Analysis of the muscarinic receptor subtype mediating inhibition of the neurogenic contractions in rabbit isolated vas deferens by a series of polymethylene tetra-amines

British Journal of Pharmacology
R BudriesiC Melchiorre

Abstract

The pharmacological characteristics of the presynaptic muscarinic receptor subtype, which mediates inhibition of the neurogenic contractions in the prostatic portion of rabbit vas deferens, have been investigated by using a series of polymethylene tetra-amines, which were selected for their ability to differentiate among muscarinic receptor subtypes. It was found that all tetra-amines antagonized McN-A-343-induced inhibition in electrically stimulated rabbit vas deferens in a competitive manner and with affinity values (pA:(2)) ranging between 6.27+/-0.09 (spirotramine) and 8.51+/-0.02 (AM170). Competition radioligand binding studies, using native muscarinic receptors from rat tissues (M(1), cortex; M(2), heart; M(3), submaxillary gland) or from NG 108-15 cells (M(4)) and human cloned muscarinic M(1)-M(4) receptors expressed in CHO-K1 cells, were undertaken with the same tetra-amines employed in functional assays. All antagonists indicated a one-site fit. The affinity estimates (pK:(i)) of tetra-amines calculated in binding assays using native receptors were similar to those obtained using cloned receptors. Among these compounds some displayed selectivity between muscarinic receptor subtypes, indicating that they may be valuabl...Continue Reading

References

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Citations

Sep 19, 2003·Il Farmaco·Marco De AmiciCarlo De Micheli
May 31, 2012·Pharmacology & Therapeutics·F Mitchelson
Jan 31, 2006·British Journal of Pharmacology·Virginia Andrea Pujol LereisRodolfo Pedro Rothlin

Related Concepts

Tripitramine
Dipitramine
Benzodiazepines
Dose-Response Relationship, Drug
McN-A-343
Inotropism
Polyamines
Muscarinic Acetylcholine Receptor
Vas Deferens Structure
Rats, Wistar

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