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. 1995;56(11-12):831-6.
doi: 10.1016/0024-3205(95)00017-z.

Quinuclidin-2-ene-based muscarinic antagonists

U Hacksell  1 , B M Nilsson, G Nordvall, G Johansson, S Sundquist, L Nilvebrant
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Quinuclidin-2-ene-based muscarinic antagonists

U Hacksell et al. Life Sci. 1995.

Abstract

A series of achiral 3-heteroaryl substituted quinuclidin-2-ene derivatives and related compounds have been synthesized by facile methods. The compounds were evaluated for muscarinic and antimuscarinic properties in receptor binding studies using (-)-[3H]-QNB as the radioligand and in a functional assay using isolated guinea pig urinary bladder. 3-(2-Benzofuranyl)-quinuclidin-2-ene (15) displayed the highest M1-receptor affinity in the present series (Ki = 9.6 nM).

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