Pharmacological properties of two amino esters of diphenylpropanoic acid.
N, N-Diethylaminoethyl ester and 3-quinuclidinyl ester of 2, 2-diphenylpropanoic acid (compound 1 and 2, respectively) were prepared and pharmacologically evaluated in vitro and in the intact animal. Both compounds attenuated the effects of increasing doses of ACh in the isolated rat ileum (pA2 = 8.40 and 8.55, respectively). These effects were comparable to that of atropine (pA2 = 8.73). The duration of methacholine-induced salivation in male Swiss-Webster mice was significantly decreased by compound 2 but not by compound 1. Cardiorespiratory studies in adult male Sprague-Dawley rats revealed that both compounds shifted the dose-response curves to methacholine in terms of arterial blood pressure, heart rate and respiration upwards; indicative of cholinergic blockade. The observed pharmacological differences between the two compounds may be attributed to apparent in vivo hydrolysis of compound 1 by esterases.
D000109:Acetylcholine / Q000494:pharmacology; D000818:Animals; D001285:Atropine / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D006339:Heart Rate / Q000187:drug effects; D006439:Hemodynamics / Q000187:drug effects; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D008688:Methacholine Compounds / Q000494:pharmacology; D051379:Mice; D009130:Muscle, Smooth / Q000187:drug effects; D010276:Parasympatholytics / Q000494:pharmacology*; D010666:Phenylpropionates / Q000494:pharmacology*; D011812:Quinuclidines / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D012119:Respiration / Q000187:drug effects; D012472:Salivation / Q000187:drug effects
D008688:Methacholine Compounds; D010276:Parasympatholytics; D010666:Phenylpropionates; D011812:Quinuclidines; C042414:aprolidine; D001285:Atropine; D000109:Acetylcholine; C006615:aprofen