Anticholinergic activity of imipramine and some analogs at muscarinic receptors of cultured mouse neuroblastoma cells
Abstract Imipramine and some of its analogs (trimipramine, 3-chlorimipramine, desipramine, 3-chloro-2-hydroxyimipramine, 2-hydroxyimipramine, and didesmethylimipramine), were assayed for their potencies as antimuscarinic agents by their abilities to antagonize muscarinic receptor-mediated cyclic gua...
Ausführliche Beschreibung
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Englisch |
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1982 |
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3 |
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Springer Online Journal Archives 1860-2002 |
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Übergeordnetes Werk: |
in: Psychopharmacology - 1959, 76(1982) vom: Jan., Seite 26-28 |
Übergeordnetes Werk: |
volume:76 ; year:1982 ; month:01 ; pages:26-28 ; extent:3 |
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NLEJ200780735 |
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520 | |a Abstract Imipramine and some of its analogs (trimipramine, 3-chlorimipramine, desipramine, 3-chloro-2-hydroxyimipramine, 2-hydroxyimipramine, and didesmethylimipramine), were assayed for their potencies as antimuscarinic agents by their abilities to antagonize muscarinic receptor-mediated cyclic guanosine monophosphate (GMP) formation by cultured mouse neuroblastoma cells. Equilibrium dissociation constants for these compounds yielded the following rank order of potency at the muscarinic receptor: imipramine > trimipramine > 3-chlorimipramine > desipramine > 3-chloro-2-hydroxyimipramine > 2-hydroxyimipramine > didesmethylimipramine. These results indicate that didesmethylation of the side chain nitrogen or hydroxylation of the ring at the 2-position lead to marked reductions (30-fold and 12-fold, respectively) in antimuscarinic activity of imipramine. | ||
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(DE-627)NLEJ200780735 DE-627 ger DE-627 rakwb eng Anticholinergic activity of imipramine and some analogs at muscarinic receptors of cultured mouse neuroblastoma cells 1982 3 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Imipramine and some of its analogs (trimipramine, 3-chlorimipramine, desipramine, 3-chloro-2-hydroxyimipramine, 2-hydroxyimipramine, and didesmethylimipramine), were assayed for their potencies as antimuscarinic agents by their abilities to antagonize muscarinic receptor-mediated cyclic guanosine monophosphate (GMP) formation by cultured mouse neuroblastoma cells. Equilibrium dissociation constants for these compounds yielded the following rank order of potency at the muscarinic receptor: imipramine > trimipramine > 3-chlorimipramine > desipramine > 3-chloro-2-hydroxyimipramine > 2-hydroxyimipramine > didesmethylimipramine. These results indicate that didesmethylation of the side chain nitrogen or hydroxylation of the ring at the 2-position lead to marked reductions (30-fold and 12-fold, respectively) in antimuscarinic activity of imipramine. Springer Online Journal Archives 1860-2002 Petersen, Ronald C. oth Richelson, Elliott oth in Psychopharmacology 1959 76(1982) vom: Jan., Seite 26-28 (DE-627)NLEJ188990615 (DE-600)2066933-1 1432-2072 nnns volume:76 year:1982 month:01 pages:26-28 extent:3 http://dx.doi.org/10.1007/BF00430749 GBV_USEFLAG_U ZDB-1-SOJ GBV_NL_ARTICLE AR 76 1982 1 26-28 3 |
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(DE-627)NLEJ200780735 DE-627 ger DE-627 rakwb eng Anticholinergic activity of imipramine and some analogs at muscarinic receptors of cultured mouse neuroblastoma cells 1982 3 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Imipramine and some of its analogs (trimipramine, 3-chlorimipramine, desipramine, 3-chloro-2-hydroxyimipramine, 2-hydroxyimipramine, and didesmethylimipramine), were assayed for their potencies as antimuscarinic agents by their abilities to antagonize muscarinic receptor-mediated cyclic guanosine monophosphate (GMP) formation by cultured mouse neuroblastoma cells. Equilibrium dissociation constants for these compounds yielded the following rank order of potency at the muscarinic receptor: imipramine > trimipramine > 3-chlorimipramine > desipramine > 3-chloro-2-hydroxyimipramine > 2-hydroxyimipramine > didesmethylimipramine. These results indicate that didesmethylation of the side chain nitrogen or hydroxylation of the ring at the 2-position lead to marked reductions (30-fold and 12-fold, respectively) in antimuscarinic activity of imipramine. Springer Online Journal Archives 1860-2002 Petersen, Ronald C. oth Richelson, Elliott oth in Psychopharmacology 1959 76(1982) vom: Jan., Seite 26-28 (DE-627)NLEJ188990615 (DE-600)2066933-1 1432-2072 nnns volume:76 year:1982 month:01 pages:26-28 extent:3 http://dx.doi.org/10.1007/BF00430749 GBV_USEFLAG_U ZDB-1-SOJ GBV_NL_ARTICLE AR 76 1982 1 26-28 3 |
allfields_unstemmed |
(DE-627)NLEJ200780735 DE-627 ger DE-627 rakwb eng Anticholinergic activity of imipramine and some analogs at muscarinic receptors of cultured mouse neuroblastoma cells 1982 3 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Imipramine and some of its analogs (trimipramine, 3-chlorimipramine, desipramine, 3-chloro-2-hydroxyimipramine, 2-hydroxyimipramine, and didesmethylimipramine), were assayed for their potencies as antimuscarinic agents by their abilities to antagonize muscarinic receptor-mediated cyclic guanosine monophosphate (GMP) formation by cultured mouse neuroblastoma cells. Equilibrium dissociation constants for these compounds yielded the following rank order of potency at the muscarinic receptor: imipramine > trimipramine > 3-chlorimipramine > desipramine > 3-chloro-2-hydroxyimipramine > 2-hydroxyimipramine > didesmethylimipramine. These results indicate that didesmethylation of the side chain nitrogen or hydroxylation of the ring at the 2-position lead to marked reductions (30-fold and 12-fold, respectively) in antimuscarinic activity of imipramine. Springer Online Journal Archives 1860-2002 Petersen, Ronald C. oth Richelson, Elliott oth in Psychopharmacology 1959 76(1982) vom: Jan., Seite 26-28 (DE-627)NLEJ188990615 (DE-600)2066933-1 1432-2072 nnns volume:76 year:1982 month:01 pages:26-28 extent:3 http://dx.doi.org/10.1007/BF00430749 GBV_USEFLAG_U ZDB-1-SOJ GBV_NL_ARTICLE AR 76 1982 1 26-28 3 |
allfieldsGer |
(DE-627)NLEJ200780735 DE-627 ger DE-627 rakwb eng Anticholinergic activity of imipramine and some analogs at muscarinic receptors of cultured mouse neuroblastoma cells 1982 3 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Imipramine and some of its analogs (trimipramine, 3-chlorimipramine, desipramine, 3-chloro-2-hydroxyimipramine, 2-hydroxyimipramine, and didesmethylimipramine), were assayed for their potencies as antimuscarinic agents by their abilities to antagonize muscarinic receptor-mediated cyclic guanosine monophosphate (GMP) formation by cultured mouse neuroblastoma cells. Equilibrium dissociation constants for these compounds yielded the following rank order of potency at the muscarinic receptor: imipramine > trimipramine > 3-chlorimipramine > desipramine > 3-chloro-2-hydroxyimipramine > 2-hydroxyimipramine > didesmethylimipramine. These results indicate that didesmethylation of the side chain nitrogen or hydroxylation of the ring at the 2-position lead to marked reductions (30-fold and 12-fold, respectively) in antimuscarinic activity of imipramine. Springer Online Journal Archives 1860-2002 Petersen, Ronald C. oth Richelson, Elliott oth in Psychopharmacology 1959 76(1982) vom: Jan., Seite 26-28 (DE-627)NLEJ188990615 (DE-600)2066933-1 1432-2072 nnns volume:76 year:1982 month:01 pages:26-28 extent:3 http://dx.doi.org/10.1007/BF00430749 GBV_USEFLAG_U ZDB-1-SOJ GBV_NL_ARTICLE AR 76 1982 1 26-28 3 |
allfieldsSound |
(DE-627)NLEJ200780735 DE-627 ger DE-627 rakwb eng Anticholinergic activity of imipramine and some analogs at muscarinic receptors of cultured mouse neuroblastoma cells 1982 3 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Imipramine and some of its analogs (trimipramine, 3-chlorimipramine, desipramine, 3-chloro-2-hydroxyimipramine, 2-hydroxyimipramine, and didesmethylimipramine), were assayed for their potencies as antimuscarinic agents by their abilities to antagonize muscarinic receptor-mediated cyclic guanosine monophosphate (GMP) formation by cultured mouse neuroblastoma cells. Equilibrium dissociation constants for these compounds yielded the following rank order of potency at the muscarinic receptor: imipramine > trimipramine > 3-chlorimipramine > desipramine > 3-chloro-2-hydroxyimipramine > 2-hydroxyimipramine > didesmethylimipramine. These results indicate that didesmethylation of the side chain nitrogen or hydroxylation of the ring at the 2-position lead to marked reductions (30-fold and 12-fold, respectively) in antimuscarinic activity of imipramine. Springer Online Journal Archives 1860-2002 Petersen, Ronald C. oth Richelson, Elliott oth in Psychopharmacology 1959 76(1982) vom: Jan., Seite 26-28 (DE-627)NLEJ188990615 (DE-600)2066933-1 1432-2072 nnns volume:76 year:1982 month:01 pages:26-28 extent:3 http://dx.doi.org/10.1007/BF00430749 GBV_USEFLAG_U ZDB-1-SOJ GBV_NL_ARTICLE AR 76 1982 1 26-28 3 |
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anticholinergic activity of imipramine and some analogs at muscarinic receptors of cultured mouse neuroblastoma cells |
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Anticholinergic activity of imipramine and some analogs at muscarinic receptors of cultured mouse neuroblastoma cells |
abstract |
Abstract Imipramine and some of its analogs (trimipramine, 3-chlorimipramine, desipramine, 3-chloro-2-hydroxyimipramine, 2-hydroxyimipramine, and didesmethylimipramine), were assayed for their potencies as antimuscarinic agents by their abilities to antagonize muscarinic receptor-mediated cyclic guanosine monophosphate (GMP) formation by cultured mouse neuroblastoma cells. Equilibrium dissociation constants for these compounds yielded the following rank order of potency at the muscarinic receptor: imipramine > trimipramine > 3-chlorimipramine > desipramine > 3-chloro-2-hydroxyimipramine > 2-hydroxyimipramine > didesmethylimipramine. These results indicate that didesmethylation of the side chain nitrogen or hydroxylation of the ring at the 2-position lead to marked reductions (30-fold and 12-fold, respectively) in antimuscarinic activity of imipramine. |
abstractGer |
Abstract Imipramine and some of its analogs (trimipramine, 3-chlorimipramine, desipramine, 3-chloro-2-hydroxyimipramine, 2-hydroxyimipramine, and didesmethylimipramine), were assayed for their potencies as antimuscarinic agents by their abilities to antagonize muscarinic receptor-mediated cyclic guanosine monophosphate (GMP) formation by cultured mouse neuroblastoma cells. Equilibrium dissociation constants for these compounds yielded the following rank order of potency at the muscarinic receptor: imipramine > trimipramine > 3-chlorimipramine > desipramine > 3-chloro-2-hydroxyimipramine > 2-hydroxyimipramine > didesmethylimipramine. These results indicate that didesmethylation of the side chain nitrogen or hydroxylation of the ring at the 2-position lead to marked reductions (30-fold and 12-fold, respectively) in antimuscarinic activity of imipramine. |
abstract_unstemmed |
Abstract Imipramine and some of its analogs (trimipramine, 3-chlorimipramine, desipramine, 3-chloro-2-hydroxyimipramine, 2-hydroxyimipramine, and didesmethylimipramine), were assayed for their potencies as antimuscarinic agents by their abilities to antagonize muscarinic receptor-mediated cyclic guanosine monophosphate (GMP) formation by cultured mouse neuroblastoma cells. Equilibrium dissociation constants for these compounds yielded the following rank order of potency at the muscarinic receptor: imipramine > trimipramine > 3-chlorimipramine > desipramine > 3-chloro-2-hydroxyimipramine > 2-hydroxyimipramine > didesmethylimipramine. These results indicate that didesmethylation of the side chain nitrogen or hydroxylation of the ring at the 2-position lead to marked reductions (30-fold and 12-fold, respectively) in antimuscarinic activity of imipramine. |
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