Comparison of the muscarinic receptors of the guinea-pig oesophageal muscularis mucosae and trachea in vitro.
1. The muscarinic receptor profile of the guinea-pig oesophageal muscularis mucosae has been compared to that of the trachea in vitro. There was no significant difference in the potency of the following muscarinic agonists at muscarinic receptors in the two tissues: carbachol, RS-86, ethoxyethyltrimethyl-ammonium, bethanechol and pilocarpine. RS-86 was 6-fold more potent at receptors in the muscularis mucosae in comparison to the trachea. There was no difference in the affinity of either carbachol or RS 86 at receptors in the two tissues. 2. The affinities (pA2) of the majority of antagonists (atropine, 4 diphenylacetoxy-N-methylpiperidine methiodide, AF-DX 116, silabenzhexol, methoctramine and gallamine) were similar at receptors in the muscularis mucosae and trachea. In contrast, the affinity of pirenzepine was approximately 5-fold greater at receptors in the muscularis mucosae (pA2 = 7.4) in comparison to receptors in the trachea (pA2 = 6.8). 3. It is concluded that the muscarinic receptor profile of the oesophageal muscularis and trachea are similar and only differ slightly with respect to the affinity of pirenzepine. Consequently, it is difficult to justify receptor heterogeneity in these two tissues.
Eglen
R M
RM
Syntex Research Institute of Pharmacology, Palo Alto, CA 94304.
Whiting
R L
RL
D000818:Animals; D004947:Esophagus / Q000187:drug effects / Q000378:metabolism*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D010276:Parasympatholytics / Q000378:metabolism / Q000494:pharmacology; D010277:Parasympathomimetics / Q000378:metabolism / Q000494:pharmacology; D011976:Receptors, Muscarinic / Q000187:drug effects / Q000378:metabolism*; D014018:Tissue Distribution; D014132:Trachea / Q000187:drug effects / Q000378:metabolism*
D010276:Parasympatholytics; D010277:Parasympathomimetics; D011976:Receptors, Muscarinic