European journal of medicinal chemistry

Allosteric effect on muscarinic M 2-receptors of derivatives of the alkane-bis-ammonium compound W84. Comparison with bispyridinium-type allosteric modulators

E Kostenis, U Holzgrabe, K Mohr

Index: Kostenis, E.; Holzgrabe, U.; Mohr, K. European Journal of Medicinal Chemistry, 1994 , vol. 29, # 12 p. 947 - 954

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Citation Number: 30

Abstract

Abstract The symmetrically shaped W84= N, N, N′, N′-tetramethyl-N, N′-bis-(3- phthalimido-propyl)-N, N′-hexane-1, 6-diyl-bis-ammonium dibromide is a potent allosteric stabilizer of antagonist-binding to cardiac muscarinic M 2-receptors. The ability of unilaterally shortened W84 derivatives to allosterically retard the dissociation of [3 H] N- methylscopolamine ([3 H] NMS) from M 2-receptors was determined in porcine cardiac ...