Biochemical Characterization of the Nicotinic Cholinergic Receptors in Human Brain: Binding of (—)-[3H]Nicotine
Abstract: (−)-[3H]Nicotine was found to bind specifically to membranes of human brains obtained at autopsy. The binding was stereospecific, (−)-nicotine being 40 times more potent than (+)-nicotine in displacing labeled (−)-nicotine. Saturation binding studies revealed the presence of two binding si...
Ausführliche Beschreibung
Autor*in: |
Shimohama, Shun [verfasserIn] Taniguchi, Takashi [verfasserIn] Fujiwara, Motohatsu [verfasserIn] |
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E-Artikel |
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Erschienen: |
Oxford, UK: Blackwell Publishing Ltd ; 1985 |
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Online-Ressource |
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2006 ; Blackwell Publishing Journal Backfiles 1879-2005 |
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Übergeordnetes Werk: |
In: Journal of neurochemistry - Oxford : Wiley-Blackwell, 1956, 45(1985), 2, Seite 0 |
Übergeordnetes Werk: |
volume:45 ; year:1985 ; number:2 ; pages:0 |
Links: |
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DOI / URN: |
10.1111/j.1471-4159.1985.tb04029.x |
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520 | |a Abstract: (−)-[3H]Nicotine was found to bind specifically to membranes of human brains obtained at autopsy. The binding was stereospecific, (−)-nicotine being 40 times more potent than (+)-nicotine in displacing labeled (−)-nicotine. Saturation binding studies revealed the presence of two binding sites with dissociation constant (KD) values of 8.1 and 86 nM, and maximum binding capacity (Bmax) values of 36 and 90 fmol/mg protein, respectively. In competition studies, nicotinic agonists were 1,000 times more potent than ganglionic, neuromuscular, and muscarinic blocking drugs in displacing labeled (−)nicotine. IC50 values for cholinergic drugs of (−)[3H]nicotine binding were as follows: (−)-nicotine, 0.51 nM; acetylcholine, 12.6 nM; (+)-nicotine, 19.9 nM; cytisine, 27.3 nM; and carbachol, 527 nM. IC50 values of α-bungarotoxin, hexamethonium, d-tubocurarine, and atropine were larger than 50 μM. (−)-[3H]Nicotine binding was highest in the nucleus basalis of Meynert and thalamus and lowest in the cerebral cortex and caudate in the brain regions tested. These results suggest that nicotinic cholinergic receptors are present in human brain and that there are regional differences in the density of these receptors. | ||
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10.1111/j.1471-4159.1985.tb04029.x doi (DE-627)NLEJ24029839X DE-627 ger DE-627 rakwb Shimohama, Shun verfasserin aut Biochemical Characterization of the Nicotinic Cholinergic Receptors in Human Brain: Binding of (—)-[3H]Nicotine Oxford, UK Blackwell Publishing Ltd 1985 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract: (−)-[3H]Nicotine was found to bind specifically to membranes of human brains obtained at autopsy. The binding was stereospecific, (−)-nicotine being 40 times more potent than (+)-nicotine in displacing labeled (−)-nicotine. Saturation binding studies revealed the presence of two binding sites with dissociation constant (KD) values of 8.1 and 86 nM, and maximum binding capacity (Bmax) values of 36 and 90 fmol/mg protein, respectively. In competition studies, nicotinic agonists were 1,000 times more potent than ganglionic, neuromuscular, and muscarinic blocking drugs in displacing labeled (−)nicotine. IC50 values for cholinergic drugs of (−)[3H]nicotine binding were as follows: (−)-nicotine, 0.51 nM; acetylcholine, 12.6 nM; (+)-nicotine, 19.9 nM; cytisine, 27.3 nM; and carbachol, 527 nM. IC50 values of α-bungarotoxin, hexamethonium, d-tubocurarine, and atropine were larger than 50 μM. (−)-[3H]Nicotine binding was highest in the nucleus basalis of Meynert and thalamus and lowest in the cerebral cortex and caudate in the brain regions tested. These results suggest that nicotinic cholinergic receptors are present in human brain and that there are regional differences in the density of these receptors. 2006 Blackwell Publishing Journal Backfiles 1879-2005 |2006|||||||||| Human brain Taniguchi, Takashi verfasserin aut Fujiwara, Motohatsu verfasserin aut Kameyama, Masakuni oth In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 45(1985), 2, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:45 year:1985 number:2 pages:0 http://dx.doi.org/10.1111/j.1471-4159.1985.tb04029.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 45 1985 2 0 |
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10.1111/j.1471-4159.1985.tb04029.x doi (DE-627)NLEJ24029839X DE-627 ger DE-627 rakwb Shimohama, Shun verfasserin aut Biochemical Characterization of the Nicotinic Cholinergic Receptors in Human Brain: Binding of (—)-[3H]Nicotine Oxford, UK Blackwell Publishing Ltd 1985 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract: (−)-[3H]Nicotine was found to bind specifically to membranes of human brains obtained at autopsy. The binding was stereospecific, (−)-nicotine being 40 times more potent than (+)-nicotine in displacing labeled (−)-nicotine. Saturation binding studies revealed the presence of two binding sites with dissociation constant (KD) values of 8.1 and 86 nM, and maximum binding capacity (Bmax) values of 36 and 90 fmol/mg protein, respectively. In competition studies, nicotinic agonists were 1,000 times more potent than ganglionic, neuromuscular, and muscarinic blocking drugs in displacing labeled (−)nicotine. IC50 values for cholinergic drugs of (−)[3H]nicotine binding were as follows: (−)-nicotine, 0.51 nM; acetylcholine, 12.6 nM; (+)-nicotine, 19.9 nM; cytisine, 27.3 nM; and carbachol, 527 nM. IC50 values of α-bungarotoxin, hexamethonium, d-tubocurarine, and atropine were larger than 50 μM. (−)-[3H]Nicotine binding was highest in the nucleus basalis of Meynert and thalamus and lowest in the cerebral cortex and caudate in the brain regions tested. These results suggest that nicotinic cholinergic receptors are present in human brain and that there are regional differences in the density of these receptors. 2006 Blackwell Publishing Journal Backfiles 1879-2005 |2006|||||||||| Human brain Taniguchi, Takashi verfasserin aut Fujiwara, Motohatsu verfasserin aut Kameyama, Masakuni oth In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 45(1985), 2, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:45 year:1985 number:2 pages:0 http://dx.doi.org/10.1111/j.1471-4159.1985.tb04029.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 45 1985 2 0 |
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10.1111/j.1471-4159.1985.tb04029.x doi (DE-627)NLEJ24029839X DE-627 ger DE-627 rakwb Shimohama, Shun verfasserin aut Biochemical Characterization of the Nicotinic Cholinergic Receptors in Human Brain: Binding of (—)-[3H]Nicotine Oxford, UK Blackwell Publishing Ltd 1985 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract: (−)-[3H]Nicotine was found to bind specifically to membranes of human brains obtained at autopsy. The binding was stereospecific, (−)-nicotine being 40 times more potent than (+)-nicotine in displacing labeled (−)-nicotine. Saturation binding studies revealed the presence of two binding sites with dissociation constant (KD) values of 8.1 and 86 nM, and maximum binding capacity (Bmax) values of 36 and 90 fmol/mg protein, respectively. In competition studies, nicotinic agonists were 1,000 times more potent than ganglionic, neuromuscular, and muscarinic blocking drugs in displacing labeled (−)nicotine. IC50 values for cholinergic drugs of (−)[3H]nicotine binding were as follows: (−)-nicotine, 0.51 nM; acetylcholine, 12.6 nM; (+)-nicotine, 19.9 nM; cytisine, 27.3 nM; and carbachol, 527 nM. IC50 values of α-bungarotoxin, hexamethonium, d-tubocurarine, and atropine were larger than 50 μM. (−)-[3H]Nicotine binding was highest in the nucleus basalis of Meynert and thalamus and lowest in the cerebral cortex and caudate in the brain regions tested. These results suggest that nicotinic cholinergic receptors are present in human brain and that there are regional differences in the density of these receptors. 2006 Blackwell Publishing Journal Backfiles 1879-2005 |2006|||||||||| Human brain Taniguchi, Takashi verfasserin aut Fujiwara, Motohatsu verfasserin aut Kameyama, Masakuni oth In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 45(1985), 2, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:45 year:1985 number:2 pages:0 http://dx.doi.org/10.1111/j.1471-4159.1985.tb04029.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 45 1985 2 0 |
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10.1111/j.1471-4159.1985.tb04029.x doi (DE-627)NLEJ24029839X DE-627 ger DE-627 rakwb Shimohama, Shun verfasserin aut Biochemical Characterization of the Nicotinic Cholinergic Receptors in Human Brain: Binding of (—)-[3H]Nicotine Oxford, UK Blackwell Publishing Ltd 1985 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract: (−)-[3H]Nicotine was found to bind specifically to membranes of human brains obtained at autopsy. The binding was stereospecific, (−)-nicotine being 40 times more potent than (+)-nicotine in displacing labeled (−)-nicotine. Saturation binding studies revealed the presence of two binding sites with dissociation constant (KD) values of 8.1 and 86 nM, and maximum binding capacity (Bmax) values of 36 and 90 fmol/mg protein, respectively. In competition studies, nicotinic agonists were 1,000 times more potent than ganglionic, neuromuscular, and muscarinic blocking drugs in displacing labeled (−)nicotine. IC50 values for cholinergic drugs of (−)[3H]nicotine binding were as follows: (−)-nicotine, 0.51 nM; acetylcholine, 12.6 nM; (+)-nicotine, 19.9 nM; cytisine, 27.3 nM; and carbachol, 527 nM. IC50 values of α-bungarotoxin, hexamethonium, d-tubocurarine, and atropine were larger than 50 μM. (−)-[3H]Nicotine binding was highest in the nucleus basalis of Meynert and thalamus and lowest in the cerebral cortex and caudate in the brain regions tested. These results suggest that nicotinic cholinergic receptors are present in human brain and that there are regional differences in the density of these receptors. 2006 Blackwell Publishing Journal Backfiles 1879-2005 |2006|||||||||| Human brain Taniguchi, Takashi verfasserin aut Fujiwara, Motohatsu verfasserin aut Kameyama, Masakuni oth In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 45(1985), 2, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:45 year:1985 number:2 pages:0 http://dx.doi.org/10.1111/j.1471-4159.1985.tb04029.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 45 1985 2 0 |
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10.1111/j.1471-4159.1985.tb04029.x doi (DE-627)NLEJ24029839X DE-627 ger DE-627 rakwb Shimohama, Shun verfasserin aut Biochemical Characterization of the Nicotinic Cholinergic Receptors in Human Brain: Binding of (—)-[3H]Nicotine Oxford, UK Blackwell Publishing Ltd 1985 Online-Ressource nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract: (−)-[3H]Nicotine was found to bind specifically to membranes of human brains obtained at autopsy. The binding was stereospecific, (−)-nicotine being 40 times more potent than (+)-nicotine in displacing labeled (−)-nicotine. Saturation binding studies revealed the presence of two binding sites with dissociation constant (KD) values of 8.1 and 86 nM, and maximum binding capacity (Bmax) values of 36 and 90 fmol/mg protein, respectively. In competition studies, nicotinic agonists were 1,000 times more potent than ganglionic, neuromuscular, and muscarinic blocking drugs in displacing labeled (−)nicotine. IC50 values for cholinergic drugs of (−)[3H]nicotine binding were as follows: (−)-nicotine, 0.51 nM; acetylcholine, 12.6 nM; (+)-nicotine, 19.9 nM; cytisine, 27.3 nM; and carbachol, 527 nM. IC50 values of α-bungarotoxin, hexamethonium, d-tubocurarine, and atropine were larger than 50 μM. (−)-[3H]Nicotine binding was highest in the nucleus basalis of Meynert and thalamus and lowest in the cerebral cortex and caudate in the brain regions tested. These results suggest that nicotinic cholinergic receptors are present in human brain and that there are regional differences in the density of these receptors. 2006 Blackwell Publishing Journal Backfiles 1879-2005 |2006|||||||||| Human brain Taniguchi, Takashi verfasserin aut Fujiwara, Motohatsu verfasserin aut Kameyama, Masakuni oth In Journal of neurochemistry Oxford : Wiley-Blackwell, 1956 45(1985), 2, Seite 0 Online-Ressource (DE-627)NLEJ243927584 (DE-600)2020528-4 1471-4159 nnns volume:45 year:1985 number:2 pages:0 http://dx.doi.org/10.1111/j.1471-4159.1985.tb04029.x text/html Verlag Deutschlandweit zugänglich Volltext GBV_USEFLAG_U ZDB-1-DJB GBV_NL_ARTICLE AR 45 1985 2 0 |
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Biochemical Characterization of the Nicotinic Cholinergic Receptors in Human Brain: Binding of (—)-[3H]Nicotine |
abstract |
Abstract: (−)-[3H]Nicotine was found to bind specifically to membranes of human brains obtained at autopsy. The binding was stereospecific, (−)-nicotine being 40 times more potent than (+)-nicotine in displacing labeled (−)-nicotine. Saturation binding studies revealed the presence of two binding sites with dissociation constant (KD) values of 8.1 and 86 nM, and maximum binding capacity (Bmax) values of 36 and 90 fmol/mg protein, respectively. In competition studies, nicotinic agonists were 1,000 times more potent than ganglionic, neuromuscular, and muscarinic blocking drugs in displacing labeled (−)nicotine. IC50 values for cholinergic drugs of (−)[3H]nicotine binding were as follows: (−)-nicotine, 0.51 nM; acetylcholine, 12.6 nM; (+)-nicotine, 19.9 nM; cytisine, 27.3 nM; and carbachol, 527 nM. IC50 values of α-bungarotoxin, hexamethonium, d-tubocurarine, and atropine were larger than 50 μM. (−)-[3H]Nicotine binding was highest in the nucleus basalis of Meynert and thalamus and lowest in the cerebral cortex and caudate in the brain regions tested. These results suggest that nicotinic cholinergic receptors are present in human brain and that there are regional differences in the density of these receptors. |
abstractGer |
Abstract: (−)-[3H]Nicotine was found to bind specifically to membranes of human brains obtained at autopsy. The binding was stereospecific, (−)-nicotine being 40 times more potent than (+)-nicotine in displacing labeled (−)-nicotine. Saturation binding studies revealed the presence of two binding sites with dissociation constant (KD) values of 8.1 and 86 nM, and maximum binding capacity (Bmax) values of 36 and 90 fmol/mg protein, respectively. In competition studies, nicotinic agonists were 1,000 times more potent than ganglionic, neuromuscular, and muscarinic blocking drugs in displacing labeled (−)nicotine. IC50 values for cholinergic drugs of (−)[3H]nicotine binding were as follows: (−)-nicotine, 0.51 nM; acetylcholine, 12.6 nM; (+)-nicotine, 19.9 nM; cytisine, 27.3 nM; and carbachol, 527 nM. IC50 values of α-bungarotoxin, hexamethonium, d-tubocurarine, and atropine were larger than 50 μM. (−)-[3H]Nicotine binding was highest in the nucleus basalis of Meynert and thalamus and lowest in the cerebral cortex and caudate in the brain regions tested. These results suggest that nicotinic cholinergic receptors are present in human brain and that there are regional differences in the density of these receptors. |
abstract_unstemmed |
Abstract: (−)-[3H]Nicotine was found to bind specifically to membranes of human brains obtained at autopsy. The binding was stereospecific, (−)-nicotine being 40 times more potent than (+)-nicotine in displacing labeled (−)-nicotine. Saturation binding studies revealed the presence of two binding sites with dissociation constant (KD) values of 8.1 and 86 nM, and maximum binding capacity (Bmax) values of 36 and 90 fmol/mg protein, respectively. In competition studies, nicotinic agonists were 1,000 times more potent than ganglionic, neuromuscular, and muscarinic blocking drugs in displacing labeled (−)nicotine. IC50 values for cholinergic drugs of (−)[3H]nicotine binding were as follows: (−)-nicotine, 0.51 nM; acetylcholine, 12.6 nM; (+)-nicotine, 19.9 nM; cytisine, 27.3 nM; and carbachol, 527 nM. IC50 values of α-bungarotoxin, hexamethonium, d-tubocurarine, and atropine were larger than 50 μM. (−)-[3H]Nicotine binding was highest in the nucleus basalis of Meynert and thalamus and lowest in the cerebral cortex and caudate in the brain regions tested. These results suggest that nicotinic cholinergic receptors are present in human brain and that there are regional differences in the density of these receptors. |
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title_short |
Biochemical Characterization of the Nicotinic Cholinergic Receptors in Human Brain: Binding of (—)-[3H]Nicotine |
url |
http://dx.doi.org/10.1111/j.1471-4159.1985.tb04029.x |
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author2 |
Taniguchi, Takashi Fujiwara, Motohatsu Kameyama, Masakuni |
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Taniguchi, Takashi Fujiwara, Motohatsu Kameyama, Masakuni |
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doi_str |
10.1111/j.1471-4159.1985.tb04029.x |
up_date |
2024-07-06T09:37:53.141Z |
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