A study of the muscarinic receptor subtype mediating mucus secretion in the cat trachea in vitro.
Mucus secretion from the cat trachea simulated by muscarinic receptor agonists has been studied by monitoring both the weight and acid glycoconjugate content of samples taken from an in vitro preparation. The nature of the receptor has been probed using a number of competitive muscarinic receptor antagonists by estimating their affinities from the degree to which the response could be blocked. Antagonist affinities have also been compared with those obtained in tracheal smooth muscle and atria from the guinea-pig. Atropine had similar affinities for all receptors investigated. 4DAMP and AF-DX116 had relatively high (pA2 = 9) and low (pA2 = 6) affinities respectively for the secretory receptor. The pA2 value of 7.5 calculated for pirenzepine suggested that the receptor was not of the M1 subtype. However, the value was higher than that for pirenzepine in both guinea-pig tissues indicating that the receptor may be an 'intermediate' between M1 and M2 subtypes. The lack of antagonists with absolute selectivity for a particular subtype of the muscarinic receptor prohibits a definitive classification.
Gater
P R
PR
Pfizer Central Research, Sandwich, Kent.
Alabaster
V A
VA
Piper
I
I
D000818:Animals; D002217:Carbachol / Q000037:antagonists & inhibitors / Q000494:pharmacology; D002415:Cats; D005260:Female; D006168:Guinea Pigs; D006325:Heart Atria / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009093:Mucus / Q000378:metabolism*; D010277:Parasympathomimetics / Q000494:pharmacology; D011976:Receptors, Muscarinic / Q000187:drug effects*; D014132:Trachea / Q000187:drug effects / Q000378:metabolism*
D010277:Parasympathomimetics; D011976:Receptors, Muscarinic; D002217:Carbachol