CHOLINERGIC AGENTS - EFFECT OF METHYL SUBSTITUTION IN A SERIES OF ARECOLINE DERIVATIVES ON BINDING TO MUSCARINIC ACETYLCHOLINE-RECEPTORS
Arecoline, arecaidine, and a series of derivatives, differing by the presence or absence of methyl groups at positions on the periphery of the molecule, were prepared, and their binding to muscarinic acetylcholine receptors was tested. On the basis of this study, muscarinic agonism for arecoline ser...
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| Published in | Journal of pharmaceutical sciences Vol. 81; no. 10; pp. 1015 - 1019 |
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| Main Authors | , , , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
HOBOKEN
Wiley
01.10.1992
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| Subjects | |
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| Abstract | Arecoline, arecaidine, and a series of derivatives, differing by the presence or absence of methyl groups at positions on the periphery of the molecule, were prepared, and their binding to muscarinic acetylcholine receptors was tested. On the basis of this study, muscarinic agonism for arecoline series is governed by strict structure-activity relationships, as previously observed for other agonist series. Only minor changes in nitrogen substitution were tolerated in the present series of arecoline derivatives. |
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| AbstractList | Arecoline, arecaidine, and a series of derivatives, differing by the presence or absence of methyl groups at positions on the periphery of the molecule, were prepared, and their binding to muscarinic acetylcholine receptors was tested. On the basis of this study, muscarinic agonism for arecoline series is governed by strict structure-activity relationships, as previously observed for other agonist series. Only minor changes in nitrogen substitution were tolerated in the present series of arecoline derivatives. |
| Author | MOOS, WH DAVIS, RE COUGHENOUR, LL MCKEE, JS MARRIOTT, JG BERGMEIER, SC THOMAS, AJ KESTER, JA HERSHENSON, FM TECLE, H SCHWARZ, RD |
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| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/1432612$$D View this record in MEDLINE/PubMed |
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| Issue | 10 |
| Keywords | ARECAIDINE EFFICACY ANALOGS AFFINITY CORTEX ESTERS COGNITION ENHANCERS INFUSIONS AGONIST BINDING RAT-BRAIN |
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article-title: POTENCY RATIO FOR THE INHIBITION OF H-3-QNB AND H-3 CIS-METHYLDIOXOLANE BINDING PREDICTS AGONIST OR ANTAGONIST ACTIVITY ON MUSCARINIC RECEPTORS publication-title: METHODS AND FINDINGS IN EXPERIMENTAL AND CLINICAL PHARMACOLOGY contributor: fullname: MORET, C – volume: 134 start-page: 61 year: 1987 ident: WOS:A1987F959000007 article-title: STIMULATION OF GANGLIONIC MUSCARINIC-M1 RECEPTORS BY A SERIES OF TERTIARY ARECAIDINE AND ISOARECAIDINE ESTERS IN THE PITHED RAT publication-title: EUROPEAN JOURNAL OF PHARMACOLOGY contributor: fullname: WESS, J – volume: 31 start-page: 1109 year: 1975 ident: WOS:A1975W163100037 article-title: CRYSTAL AND MOLECULAR-STRUCTURE OF ARECOLINE METHIODIDE publication-title: ACTA CRYSTALLOGRAPHICA SECTION B-STRUCTURAL SCIENCE contributor: fullname: MALLARD, DJH – volume: 193 start-page: 189 year: 1980 ident: WOS:A1980JZ86900016 article-title: ANALYSIS OF REGIONAL VARIATIONS IN THE AFFINITIES OF MUSCARINIC AGONISTS IN THE RAT-BRAIN 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AGONISTS publication-title: JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS contributor: fullname: PARKER, RB – year: 1988 ident: WOS:A1992JQ81800011.27 publication-title: 196TH NAT M AM CHEM contributor: fullname: MOOS WH – volume: 70 start-page: 485 year: 1986 ident: WOS:A1986G273000031 article-title: MUSCARINIC CHOLINERGIC AGONISTS - PHARMACOLOGICAL AND CLINICAL PERSPECTIVES publication-title: PROGRESS IN BRAIN RESEARCH contributor: fullname: PALACIOS, JM – volume: 237 start-page: 411 year: 1986 ident: WOS:A1986C323900009 article-title: [H-3] PIRENZEPINE AND (-)-[H-3]QUINUCLIDINYL BENZILATE BINDING TO RAT CEREBRAL CORTICAL AND CARDIAC MUSCARINIC CHOLINERGIC SITES .1. CHARACTERIZATION AND REGULATION OF AGONIST BINDING TO PUTATIVE MUSCARINIC SUBTYPES publication-title: JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS contributor: fullname: WATSON, M |
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| SubjectTerms | Animals Arecoline - analogs & derivatives Arecoline - metabolism Chemistry Chemistry, Medicinal Chemistry, Multidisciplinary Choline - physiology Dioxolanes - metabolism Dioxolanes - pharmacology Life Sciences & Biomedicine Muscarinic Antagonists Parasympathomimetics - metabolism Parasympathomimetics - pharmacology Pharmacology & Pharmacy Physical Sciences Quinuclidinyl Benzilate - metabolism Quinuclidinyl Benzilate - pharmacology Rats Receptors, Muscarinic - metabolism Receptors, Muscarinic - physiology Science & Technology Structure-Activity Relationship Tritium |
| Title | CHOLINERGIC AGENTS - EFFECT OF METHYL SUBSTITUTION IN A SERIES OF ARECOLINE DERIVATIVES ON BINDING TO MUSCARINIC ACETYLCHOLINE-RECEPTORS |
| URI | http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=Summon&SrcAuth=ProQuest&DestApp=WOS&DestLinkType=FullRecord&UT=A1992JQ81800011 https://www.ncbi.nlm.nih.gov/pubmed/1432612 |
| Volume | 81 |
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