Analogues of carbacholine: synthesis and relationship between structure and affinity for muscarinic and nicotinic acetylcholine receptors

…, S Ebdrup, P Krogsgaard??Larsen, E Falch

Index: Sokilde, Birgitte; Mikkelsen, Ivan; Stensbol, Tine B.; Andersen, Birgit; Ebdrup, Soren; Krogsgaard-Larsen, Povl; Falch, Erik Archiv der Pharmazie, 1996 , vol. 329, # 2 p. 95 - 104

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Citation Number: 11

Abstract

Abstract A series of acyclic and heterocyclic analogues of carbacholine (1) was synthesized using N-methylcarbacholine (MCC, 2), N, N-dimethylcarbacholine (DMCC, 3), and the corresponding tertiary amine (4) as leads. Whereas nicotinic acetylcholine receptor affinity was determined using [3 H] nicotine as the radioactive ligand,[3 H] oxotremorine-M ([3 H] Oxo-M) and [3 H] quinuclidinyl benzilate ([3 H] QNB), in some cases supplemented with [3 ...