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A Stable and Highly Potent Hexamethonium Derivative Which Modulates Muscarinic Receptors Allosterically in Guinea-Pig Hearts

A Stable and Highly Potent Hexamethonium Derivative Which Modulates Muscarinic Receptors Allosterically in Guinea-Pig Hearts

G Bejeuhr, G Blaschke, U Holzgrabe, K Mohr, U Sürig, G Terfloth

J Pharm Pharmacol. 1994 Feb;46(2):108-12.

PMID: 7912726

Abstract:

W84 (N,N,N',N'-tetramethyl-N,N'-bis-(3-phthalimidopropyl)-N,N'-hexane- 1,6- diyl-bis-ammonium dibromide) is a potent stabilizer of antagonist binding to muscarinic receptors; however, W84 hydrolyses in aqueous buffered medium. The synthesis of the stable derivative CHIN3/6 is presented containing a 2-phenyl-quinazolinone instead of the labile phthalimide substituent. This compound retarded [3H]N-methylscopolamine-dissociation in guinea-pig cardiac membranes with slightly higher potency than W84, the EC50 values amounting to 7.5 x 10(-7) and 13 x 10(-7) M, respectively. Molecular modelling revealed differences in the electron density of the substituents and in their molecular shape. It is suggested that the derivatives use partially different sites of attachment when occupying the allosteric binding site of the receptor protein.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP21093516	W-84 dibromide		21093-51-6	Price

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