Evidence that an atypical beta-adrenoceptor mediates the inhibition of spontaneous rhythmical contractions of rabbit isolated jejunum induced by ritodrine and salbutamol.
1. The nature of the adrenoceptors mediating the inhibitory action of noradrenaline, ritodrine and salbutamol on the spontaneous activity of longitudinal muscle of the rabbit jejunum in vitro was investigated by use of a range of adrenoceptor antagonists. 2. The actions of ritodrine and salbutamol were antagonized competitively by propranolol. The pA2 values of 6.4 and 6.6 respectively were smaller than those found elsewhere for beta 1- and beta 2-adrenoceptors. 3. In contrast, the responses to ritodrine and salbutamol were antagonized only by high concentrations (greater than 2.7 microM) of phentolamine and were unaffected by yohimbine (2.6 microM), mepyramine (2.5 microM) or cimetidine (4.0 microM). 4. Ritodrine which is less potent than salbutamol in tissues with typical beta 2-adrenoceptors was found to be 8 times more potent than salbutamol in the rabbit jejunum. 5. It is suggested that in the rabbit jejunum ritodrine and salbutamol may act at an atypical beta-adrenoceptor, at which propranolol is a competitive but not very potent antagonist.
Norman
B J
BJ
Department of Pharmacology, Charing Cross and Westminster Medical School, London.
Leathard
H L
HL
D000420:Albuterol / Q000494:pharmacology*; D000818:Animals; D002927:Cimetidine / Q000494:pharmacology; D005260:Female; D066298:In Vitro Techniques; D007583:Jejunum / Q000187:drug effects; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology*; D009638:Norepinephrine / Q000494:pharmacology; D011738:Pyrilamine / Q000494:pharmacology; D011817:Rabbits; D011943:Receptors, Adrenergic, beta / Q000187:drug effects / Q000378:metabolism*; D012312:Ritodrine / Q000494:pharmacology*; D015016:Yohimbine / Q000494:pharmacology
D011943:Receptors, Adrenergic, beta; D015016:Yohimbine; D002927:Cimetidine; D011738:Pyrilamine; D012312:Ritodrine; D000420:Albuterol; D009638:Norepinephrine