Pharmacological characterization of muscarinic receptor subtypes in rabbit isolated tissue preparations.
1 The affinity of some muscarinic antagonists for muscarinic receptors was determined in functional isolated tissue studies in order to compare the muscarinic receptor subtypes in the rabbit. 2 Our attention was specially focused on the question of whether the muscarinic receptors mediating vasodilatation in the aorta resemble or not the ones present on the jejunum of the gastrointestinal tract. 3 Isolated aorta, jejunum, stimulated left atrium and vas deferens preparations of rabbit were investigated with the following muscarinic antagonists: atropine, pirenzepine, methoctramine (N,N'-bis[6-92-methoxybenzyl)amino hexyl]-1,8-octane-diamine tetrahydrochloride) and 4-DAMP (4-diphenylacetoxy-N-methylpiperidine methiodide). 4 The results demonstrate that the receptors on aorta are unlike those on the other rabbit tissues: pirenzepine pA2 was 6.4 on aorta but 8.1 on vas deferens; methoctramine pA2 was 5.9 on aorta but 7.1 on heart; 4-DAMP pA2 was 8.7 on aorta and 8.0 on jejunum. This raises the question: what subtype might be involved?
Angeli
P
P
Department of Chemical Sciences, University of Camerino, Italy.
Brasili
L
L
Cingolani
M L
ML
Marucci
G
G
Pigini
P
P
Tonnini
M C
MC
D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects; D001285:Atropine / Q000494:pharmacology; D003959:Diamines / Q000494:pharmacology; D007583:Jejunum / Q000737:chemistry / Q000187:drug effects; D008297:Male; D018727:Muscarinic Antagonists; D009119:Muscle Contraction / Q000187:drug effects; D009206:Myocardium / Q000737:chemistry; D010276:Parasympatholytics / Q000494:pharmacology*; D010880:Piperidines / Q000494:pharmacology; D010890:Pirenzepine / Q000494:pharmacology; D011817:Rabbits; D011976:Receptors, Muscarinic / Q000737:chemistry* / Q000378:metabolism; D014649:Vas Deferens / Q000737:chemistry / Q000187:drug effects; D014664:Vasodilation / Q000187:drug effects* / Q000502:physiology
D003959:Diamines; D018727:Muscarinic Antagonists; D010276:Parasympatholytics; D010880:Piperidines; D011976:Receptors, Muscarinic; D010890:Pirenzepine; D001285:Atropine; C042375:4-diphenylacetoxy-1,1-dimethylpiperidinium; C054938:methoctramine