1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies

Background 1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ) demonstrates significant neuroprotective activity. It can interact with agonistic conformation of dopamine (DA) receptors.1MeTIQ inhibits the formation of 3,4-dihydroxyphenylacetic acid as well as production of free radicals and shifts DA c...
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Autor*in:	Możdżeń, Edyta [verfasserIn] Babińska, Izabela Wójcikowski, Jacek Antkiewicz -Michaluk, Lucyna

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2019

Schlagwörter:	1-Methyl-1,2,3,4-tetrahydroisoquinoline Histopathology ADMET Predictor

Anmerkung:	© Maj Institute of Pharmacology Polish Academy of Sciences 2019

Übergeordnetes Werk:	Enthalten in: Pharmacological reports - Heidelberg : Springer Nature, 1998, 71(2019), 6 vom: 09. Juli, Seite 1140-1146
Übergeordnetes Werk:	volume:71 ; year:2019 ; number:6 ; day:09 ; month:07 ; pages:1140-1146

Links:	Volltext

DOI / URN:	10.1016/j.pharep.2019.06.016

Katalog-ID:	SPR038904071

Internformat


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520			\|a Background 1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ) demonstrates significant neuroprotective activity. It can interact with agonistic conformation of dopamine (DA) receptors.1MeTIQ inhibits the formation of 3,4-dihydroxyphenylacetic acid as well as production of free radicals and shifts DA catabolism toward COMT-dependent O-methylation. 1MeTIQ inhibits both MAO-A and B enzymes activity and increases neurotransmitters levels inthe brain. It shows significant antidepressant-like effect in forced swim test (FST) in rats. This compound might be effective for depression therapy in a clinical setting but its success is determined not only by good efficacy, but also by an acceptable its ADMET profile. The use of combination in silico prediction with in vivoand in vitro studies greatly simplifies the search for new, safer and effectively acting drugs. Methods The aim of this study was to investigate the degree of histopathological changes in different rats tissues after acute and chronic administration of 1MeTIQ. Additionally, prediction of its properties in terms of absorption, distribution, metabolism, elimination and toxicity in the human body was performed. Results The obtained data did not show extensive and significant toxic effects of tested substance in in vivo and in vitro studies in rats, and in silico ADMET prediction. Conclusions These results can help to discover a new effective and safe antidepressant substance and have important significance in the treatment ofdepression in clinic. Additionally, the usein the treatment of depression substance with neuroprotective, antioxidant and antidepressant-like effects in the CNS and existing endogenously might be also beneficial in controlling the adverse CNS inflammatory processes accompanying depression.
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912			\|a GBV_ILN_110
912			\|a GBV_ILN_138
912			\|a GBV_ILN_150
912			\|a GBV_ILN_151
912			\|a GBV_ILN_161
912			\|a GBV_ILN_170
912			\|a GBV_ILN_171
912			\|a GBV_ILN_187
912			\|a GBV_ILN_213
912			\|a GBV_ILN_224
912			\|a GBV_ILN_230
912			\|a GBV_ILN_250
912			\|a GBV_ILN_281
912			\|a GBV_ILN_285
912			\|a GBV_ILN_293
912			\|a GBV_ILN_370
912			\|a GBV_ILN_602
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912			\|a GBV_ILN_702
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912			\|a GBV_ILN_2006
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912			\|a GBV_ILN_2009
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912			\|a GBV_ILN_2027
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912			\|a GBV_ILN_2064
912			\|a GBV_ILN_2065
912			\|a GBV_ILN_2068
912			\|a GBV_ILN_2088
912			\|a GBV_ILN_2093
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allfields	10.1016/j.pharep.2019.06.016 doi (DE-627)SPR038904071 (SPR)j.pharep.2019.06.016-e DE-627 ger DE-627 rakwb eng Możdżeń, Edyta verfasserin aut 1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies 2019 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier © Maj Institute of Pharmacology Polish Academy of Sciences 2019 Background 1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ) demonstrates significant neuroprotective activity. It can interact with agonistic conformation of dopamine (DA) receptors.1MeTIQ inhibits the formation of 3,4-dihydroxyphenylacetic acid as well as production of free radicals and shifts DA catabolism toward COMT-dependent O-methylation. 1MeTIQ inhibits both MAO-A and B enzymes activity and increases neurotransmitters levels inthe brain. It shows significant antidepressant-like effect in forced swim test (FST) in rats. This compound might be effective for depression therapy in a clinical setting but its success is determined not only by good efficacy, but also by an acceptable its ADMET profile. The use of combination in silico prediction with in vivoand in vitro studies greatly simplifies the search for new, safer and effectively acting drugs. Methods The aim of this study was to investigate the degree of histopathological changes in different rats tissues after acute and chronic administration of 1MeTIQ. Additionally, prediction of its properties in terms of absorption, distribution, metabolism, elimination and toxicity in the human body was performed. Results The obtained data did not show extensive and significant toxic effects of tested substance in in vivo and in vitro studies in rats, and in silico ADMET prediction. Conclusions These results can help to discover a new effective and safe antidepressant substance and have important significance in the treatment ofdepression in clinic. Additionally, the usein the treatment of depression substance with neuroprotective, antioxidant and antidepressant-like effects in the CNS and existing endogenously might be also beneficial in controlling the adverse CNS inflammatory processes accompanying depression. 1-Methyl-1,2,3,4-tetrahydroisoquinoline (dpeaa)DE-He213 Histopathology (dpeaa)DE-He213 ADMET Predictor (dpeaa)DE-He213 Babińska, Izabela aut Wójcikowski, Jacek aut Antkiewicz -Michaluk, Lucyna aut Enthalten in Pharmacological reports Heidelberg : Springer Nature, 1998 71(2019), 6 vom: 09. Juli, Seite 1140-1146 (DE-627)375964215 (DE-600)2129019-2 2299-5684 nnns volume:71 year:2019 number:6 day:09 month:07 pages:1140-1146 https://dx.doi.org/10.1016/j.pharep.2019.06.016 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_647 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 AR 71 2019 6 09 07 1140-1146
spelling	10.1016/j.pharep.2019.06.016 doi (DE-627)SPR038904071 (SPR)j.pharep.2019.06.016-e DE-627 ger DE-627 rakwb eng Możdżeń, Edyta verfasserin aut 1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies 2019 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier © Maj Institute of Pharmacology Polish Academy of Sciences 2019 Background 1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ) demonstrates significant neuroprotective activity. It can interact with agonistic conformation of dopamine (DA) receptors.1MeTIQ inhibits the formation of 3,4-dihydroxyphenylacetic acid as well as production of free radicals and shifts DA catabolism toward COMT-dependent O-methylation. 1MeTIQ inhibits both MAO-A and B enzymes activity and increases neurotransmitters levels inthe brain. It shows significant antidepressant-like effect in forced swim test (FST) in rats. This compound might be effective for depression therapy in a clinical setting but its success is determined not only by good efficacy, but also by an acceptable its ADMET profile. The use of combination in silico prediction with in vivoand in vitro studies greatly simplifies the search for new, safer and effectively acting drugs. Methods The aim of this study was to investigate the degree of histopathological changes in different rats tissues after acute and chronic administration of 1MeTIQ. Additionally, prediction of its properties in terms of absorption, distribution, metabolism, elimination and toxicity in the human body was performed. Results The obtained data did not show extensive and significant toxic effects of tested substance in in vivo and in vitro studies in rats, and in silico ADMET prediction. Conclusions These results can help to discover a new effective and safe antidepressant substance and have important significance in the treatment ofdepression in clinic. Additionally, the usein the treatment of depression substance with neuroprotective, antioxidant and antidepressant-like effects in the CNS and existing endogenously might be also beneficial in controlling the adverse CNS inflammatory processes accompanying depression. 1-Methyl-1,2,3,4-tetrahydroisoquinoline (dpeaa)DE-He213 Histopathology (dpeaa)DE-He213 ADMET Predictor (dpeaa)DE-He213 Babińska, Izabela aut Wójcikowski, Jacek aut Antkiewicz -Michaluk, Lucyna aut Enthalten in Pharmacological reports Heidelberg : Springer Nature, 1998 71(2019), 6 vom: 09. Juli, Seite 1140-1146 (DE-627)375964215 (DE-600)2129019-2 2299-5684 nnns volume:71 year:2019 number:6 day:09 month:07 pages:1140-1146 https://dx.doi.org/10.1016/j.pharep.2019.06.016 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_647 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 AR 71 2019 6 09 07 1140-1146
allfields_unstemmed	10.1016/j.pharep.2019.06.016 doi (DE-627)SPR038904071 (SPR)j.pharep.2019.06.016-e DE-627 ger DE-627 rakwb eng Możdżeń, Edyta verfasserin aut 1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies 2019 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier © Maj Institute of Pharmacology Polish Academy of Sciences 2019 Background 1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ) demonstrates significant neuroprotective activity. It can interact with agonistic conformation of dopamine (DA) receptors.1MeTIQ inhibits the formation of 3,4-dihydroxyphenylacetic acid as well as production of free radicals and shifts DA catabolism toward COMT-dependent O-methylation. 1MeTIQ inhibits both MAO-A and B enzymes activity and increases neurotransmitters levels inthe brain. It shows significant antidepressant-like effect in forced swim test (FST) in rats. This compound might be effective for depression therapy in a clinical setting but its success is determined not only by good efficacy, but also by an acceptable its ADMET profile. The use of combination in silico prediction with in vivoand in vitro studies greatly simplifies the search for new, safer and effectively acting drugs. Methods The aim of this study was to investigate the degree of histopathological changes in different rats tissues after acute and chronic administration of 1MeTIQ. Additionally, prediction of its properties in terms of absorption, distribution, metabolism, elimination and toxicity in the human body was performed. Results The obtained data did not show extensive and significant toxic effects of tested substance in in vivo and in vitro studies in rats, and in silico ADMET prediction. Conclusions These results can help to discover a new effective and safe antidepressant substance and have important significance in the treatment ofdepression in clinic. Additionally, the usein the treatment of depression substance with neuroprotective, antioxidant and antidepressant-like effects in the CNS and existing endogenously might be also beneficial in controlling the adverse CNS inflammatory processes accompanying depression. 1-Methyl-1,2,3,4-tetrahydroisoquinoline (dpeaa)DE-He213 Histopathology (dpeaa)DE-He213 ADMET Predictor (dpeaa)DE-He213 Babińska, Izabela aut Wójcikowski, Jacek aut Antkiewicz -Michaluk, Lucyna aut Enthalten in Pharmacological reports Heidelberg : Springer Nature, 1998 71(2019), 6 vom: 09. Juli, Seite 1140-1146 (DE-627)375964215 (DE-600)2129019-2 2299-5684 nnns volume:71 year:2019 number:6 day:09 month:07 pages:1140-1146 https://dx.doi.org/10.1016/j.pharep.2019.06.016 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_647 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 AR 71 2019 6 09 07 1140-1146
allfieldsGer	10.1016/j.pharep.2019.06.016 doi (DE-627)SPR038904071 (SPR)j.pharep.2019.06.016-e DE-627 ger DE-627 rakwb eng Możdżeń, Edyta verfasserin aut 1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies 2019 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier © Maj Institute of Pharmacology Polish Academy of Sciences 2019 Background 1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ) demonstrates significant neuroprotective activity. It can interact with agonistic conformation of dopamine (DA) receptors.1MeTIQ inhibits the formation of 3,4-dihydroxyphenylacetic acid as well as production of free radicals and shifts DA catabolism toward COMT-dependent O-methylation. 1MeTIQ inhibits both MAO-A and B enzymes activity and increases neurotransmitters levels inthe brain. It shows significant antidepressant-like effect in forced swim test (FST) in rats. This compound might be effective for depression therapy in a clinical setting but its success is determined not only by good efficacy, but also by an acceptable its ADMET profile. The use of combination in silico prediction with in vivoand in vitro studies greatly simplifies the search for new, safer and effectively acting drugs. Methods The aim of this study was to investigate the degree of histopathological changes in different rats tissues after acute and chronic administration of 1MeTIQ. Additionally, prediction of its properties in terms of absorption, distribution, metabolism, elimination and toxicity in the human body was performed. Results The obtained data did not show extensive and significant toxic effects of tested substance in in vivo and in vitro studies in rats, and in silico ADMET prediction. Conclusions These results can help to discover a new effective and safe antidepressant substance and have important significance in the treatment ofdepression in clinic. Additionally, the usein the treatment of depression substance with neuroprotective, antioxidant and antidepressant-like effects in the CNS and existing endogenously might be also beneficial in controlling the adverse CNS inflammatory processes accompanying depression. 1-Methyl-1,2,3,4-tetrahydroisoquinoline (dpeaa)DE-He213 Histopathology (dpeaa)DE-He213 ADMET Predictor (dpeaa)DE-He213 Babińska, Izabela aut Wójcikowski, Jacek aut Antkiewicz -Michaluk, Lucyna aut Enthalten in Pharmacological reports Heidelberg : Springer Nature, 1998 71(2019), 6 vom: 09. Juli, Seite 1140-1146 (DE-627)375964215 (DE-600)2129019-2 2299-5684 nnns volume:71 year:2019 number:6 day:09 month:07 pages:1140-1146 https://dx.doi.org/10.1016/j.pharep.2019.06.016 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_647 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 AR 71 2019 6 09 07 1140-1146
allfieldsSound	10.1016/j.pharep.2019.06.016 doi (DE-627)SPR038904071 (SPR)j.pharep.2019.06.016-e DE-627 ger DE-627 rakwb eng Możdżeń, Edyta verfasserin aut 1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies 2019 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier © Maj Institute of Pharmacology Polish Academy of Sciences 2019 Background 1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ) demonstrates significant neuroprotective activity. It can interact with agonistic conformation of dopamine (DA) receptors.1MeTIQ inhibits the formation of 3,4-dihydroxyphenylacetic acid as well as production of free radicals and shifts DA catabolism toward COMT-dependent O-methylation. 1MeTIQ inhibits both MAO-A and B enzymes activity and increases neurotransmitters levels inthe brain. It shows significant antidepressant-like effect in forced swim test (FST) in rats. This compound might be effective for depression therapy in a clinical setting but its success is determined not only by good efficacy, but also by an acceptable its ADMET profile. The use of combination in silico prediction with in vivoand in vitro studies greatly simplifies the search for new, safer and effectively acting drugs. Methods The aim of this study was to investigate the degree of histopathological changes in different rats tissues after acute and chronic administration of 1MeTIQ. Additionally, prediction of its properties in terms of absorption, distribution, metabolism, elimination and toxicity in the human body was performed. Results The obtained data did not show extensive and significant toxic effects of tested substance in in vivo and in vitro studies in rats, and in silico ADMET prediction. Conclusions These results can help to discover a new effective and safe antidepressant substance and have important significance in the treatment ofdepression in clinic. Additionally, the usein the treatment of depression substance with neuroprotective, antioxidant and antidepressant-like effects in the CNS and existing endogenously might be also beneficial in controlling the adverse CNS inflammatory processes accompanying depression. 1-Methyl-1,2,3,4-tetrahydroisoquinoline (dpeaa)DE-He213 Histopathology (dpeaa)DE-He213 ADMET Predictor (dpeaa)DE-He213 Babińska, Izabela aut Wójcikowski, Jacek aut Antkiewicz -Michaluk, Lucyna aut Enthalten in Pharmacological reports Heidelberg : Springer Nature, 1998 71(2019), 6 vom: 09. Juli, Seite 1140-1146 (DE-627)375964215 (DE-600)2129019-2 2299-5684 nnns volume:71 year:2019 number:6 day:09 month:07 pages:1140-1146 https://dx.doi.org/10.1016/j.pharep.2019.06.016 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_647 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 AR 71 2019 6 09 07 1140-1146
language	English
source	Enthalten in Pharmacological reports 71(2019), 6 vom: 09. Juli, Seite 1140-1146 volume:71 year:2019 number:6 day:09 month:07 pages:1140-1146
sourceStr	Enthalten in Pharmacological reports 71(2019), 6 vom: 09. Juli, Seite 1140-1146 volume:71 year:2019 number:6 day:09 month:07 pages:1140-1146
format_phy_str_mv	Article
institution	findex.gbv.de
topic_facet	1-Methyl-1,2,3,4-tetrahydroisoquinoline Histopathology ADMET Predictor
isfreeaccess_bool	false
container_title	Pharmacological reports
authorswithroles_txt_mv	Możdżeń, Edyta @@aut@@ Babińska, Izabela @@aut@@ Wójcikowski, Jacek @@aut@@ Antkiewicz -Michaluk, Lucyna @@aut@@
publishDateDaySort_date	2019-07-09T00:00:00Z
hierarchy_top_id	375964215
id	SPR038904071
language_de	englisch
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author	Możdżeń, Edyta
spellingShingle	Możdżeń, Edyta misc 1-Methyl-1,2,3,4-tetrahydroisoquinoline misc Histopathology misc ADMET Predictor 1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies
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topic_title	1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies 1-Methyl-1,2,3,4-tetrahydroisoquinoline (dpeaa)DE-He213 Histopathology (dpeaa)DE-He213 ADMET Predictor (dpeaa)DE-He213
topic	misc 1-Methyl-1,2,3,4-tetrahydroisoquinoline misc Histopathology misc ADMET Predictor
topic_unstemmed	misc 1-Methyl-1,2,3,4-tetrahydroisoquinoline misc Histopathology misc ADMET Predictor
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title	1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies
ctrlnum	(DE-627)SPR038904071 (SPR)j.pharep.2019.06.016-e
title_full	1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies
author_sort	Możdżeń, Edyta
journal	Pharmacological reports
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author_browse	Możdżeń, Edyta Babińska, Izabela Wójcikowski, Jacek Antkiewicz -Michaluk, Lucyna
container_volume	71
format_se	Elektronische Aufsätze
author-letter	Możdżeń, Edyta
doi_str_mv	10.1016/j.pharep.2019.06.016
title_sort	1-methyl-1,2,3,4-tetrahydroisoquinoline — the toxicological research on an exo/endogenous amine with antidepressant-like activity — in vivo, in vitro and in silico studies
title_auth	1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies
abstract	Background 1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ) demonstrates significant neuroprotective activity. It can interact with agonistic conformation of dopamine (DA) receptors.1MeTIQ inhibits the formation of 3,4-dihydroxyphenylacetic acid as well as production of free radicals and shifts DA catabolism toward COMT-dependent O-methylation. 1MeTIQ inhibits both MAO-A and B enzymes activity and increases neurotransmitters levels inthe brain. It shows significant antidepressant-like effect in forced swim test (FST) in rats. This compound might be effective for depression therapy in a clinical setting but its success is determined not only by good efficacy, but also by an acceptable its ADMET profile. The use of combination in silico prediction with in vivoand in vitro studies greatly simplifies the search for new, safer and effectively acting drugs. Methods The aim of this study was to investigate the degree of histopathological changes in different rats tissues after acute and chronic administration of 1MeTIQ. Additionally, prediction of its properties in terms of absorption, distribution, metabolism, elimination and toxicity in the human body was performed. Results The obtained data did not show extensive and significant toxic effects of tested substance in in vivo and in vitro studies in rats, and in silico ADMET prediction. Conclusions These results can help to discover a new effective and safe antidepressant substance and have important significance in the treatment ofdepression in clinic. Additionally, the usein the treatment of depression substance with neuroprotective, antioxidant and antidepressant-like effects in the CNS and existing endogenously might be also beneficial in controlling the adverse CNS inflammatory processes accompanying depression. © Maj Institute of Pharmacology Polish Academy of Sciences 2019
abstractGer	Background 1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ) demonstrates significant neuroprotective activity. It can interact with agonistic conformation of dopamine (DA) receptors.1MeTIQ inhibits the formation of 3,4-dihydroxyphenylacetic acid as well as production of free radicals and shifts DA catabolism toward COMT-dependent O-methylation. 1MeTIQ inhibits both MAO-A and B enzymes activity and increases neurotransmitters levels inthe brain. It shows significant antidepressant-like effect in forced swim test (FST) in rats. This compound might be effective for depression therapy in a clinical setting but its success is determined not only by good efficacy, but also by an acceptable its ADMET profile. The use of combination in silico prediction with in vivoand in vitro studies greatly simplifies the search for new, safer and effectively acting drugs. Methods The aim of this study was to investigate the degree of histopathological changes in different rats tissues after acute and chronic administration of 1MeTIQ. Additionally, prediction of its properties in terms of absorption, distribution, metabolism, elimination and toxicity in the human body was performed. Results The obtained data did not show extensive and significant toxic effects of tested substance in in vivo and in vitro studies in rats, and in silico ADMET prediction. Conclusions These results can help to discover a new effective and safe antidepressant substance and have important significance in the treatment ofdepression in clinic. Additionally, the usein the treatment of depression substance with neuroprotective, antioxidant and antidepressant-like effects in the CNS and existing endogenously might be also beneficial in controlling the adverse CNS inflammatory processes accompanying depression. © Maj Institute of Pharmacology Polish Academy of Sciences 2019
abstract_unstemmed	Background 1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ) demonstrates significant neuroprotective activity. It can interact with agonistic conformation of dopamine (DA) receptors.1MeTIQ inhibits the formation of 3,4-dihydroxyphenylacetic acid as well as production of free radicals and shifts DA catabolism toward COMT-dependent O-methylation. 1MeTIQ inhibits both MAO-A and B enzymes activity and increases neurotransmitters levels inthe brain. It shows significant antidepressant-like effect in forced swim test (FST) in rats. This compound might be effective for depression therapy in a clinical setting but its success is determined not only by good efficacy, but also by an acceptable its ADMET profile. The use of combination in silico prediction with in vivoand in vitro studies greatly simplifies the search for new, safer and effectively acting drugs. Methods The aim of this study was to investigate the degree of histopathological changes in different rats tissues after acute and chronic administration of 1MeTIQ. Additionally, prediction of its properties in terms of absorption, distribution, metabolism, elimination and toxicity in the human body was performed. Results The obtained data did not show extensive and significant toxic effects of tested substance in in vivo and in vitro studies in rats, and in silico ADMET prediction. Conclusions These results can help to discover a new effective and safe antidepressant substance and have important significance in the treatment ofdepression in clinic. Additionally, the usein the treatment of depression substance with neuroprotective, antioxidant and antidepressant-like effects in the CNS and existing endogenously might be also beneficial in controlling the adverse CNS inflammatory processes accompanying depression. © Maj Institute of Pharmacology Polish Academy of Sciences 2019
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title_short	1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies
url	https://dx.doi.org/10.1016/j.pharep.2019.06.016
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author2	Babińska, Izabela Wójcikowski, Jacek Antkiewicz -Michaluk, Lucyna
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doi_str	10.1016/j.pharep.2019.06.016
up_date	2024-07-03T20:39:42.860Z
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It can interact with agonistic conformation of dopamine (DA) receptors.1MeTIQ inhibits the formation of 3,4-dihydroxyphenylacetic acid as well as production of free radicals and shifts DA catabolism toward COMT-dependent O-methylation. 1MeTIQ inhibits both MAO-A and B enzymes activity and increases neurotransmitters levels inthe brain. It shows significant antidepressant-like effect in forced swim test (FST) in rats. This compound might be effective for depression therapy in a clinical setting but its success is determined not only by good efficacy, but also by an acceptable its ADMET profile. The use of combination in silico prediction with in vivoand in vitro studies greatly simplifies the search for new, safer and effectively acting drugs. Methods The aim of this study was to investigate the degree of histopathological changes in different rats tissues after acute and chronic administration of 1MeTIQ. Additionally, prediction of its properties in terms of absorption, distribution, metabolism, elimination and toxicity in the human body was performed. Results The obtained data did not show extensive and significant toxic effects of tested substance in in vivo and in vitro studies in rats, and in silico ADMET prediction. Conclusions These results can help to discover a new effective and safe antidepressant substance and have important significance in the treatment ofdepression in clinic. 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1-Methyl-1,2,3,4-tetrahydroisoquinoline — The toxicological research on an exo/endogenous amine with antidepressant-like activity — In vivo, in vitro and in silico studies

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