Pharmacological effects of 2-aminotetralins, octahydrobenzo[f]quinolines and clonidine on the isolated guinea pig ileum.
The ability of derivatives of 2-aminotetralins (2AT), cis- or trans-isomers of octahydrobenzo[f]quinolines (BfQ) and clonidine to modulate acetylcholine release was studied using field-stimulated guinea pig ilea (GPI). Antihistaminic and antiacetylcholine activities were also determined using isolated superfused segments of GPI. Hydroxylated 2AT, BfQ and clonidine inhibited field stimulation-induced contractions through alpha-adrenoceptor mechanisms which were antagonized by phentolamine. In contrast, the inhibition produced by nonhydroxylated 2AT was not attenuated by alpha-adrenoceptor antagonism. 2AT, trans-7,8-dihydro-BfQ and cis-8,9-dihydroxy-BfQ inhibited contractions induced by nicotine bitartrate using superfused GPI. Clonidine was inactive as an antinicotinic agent and there was no correlation between a compound's ability to inhibit contractions induced by field stimulation and its antinicotinic activity. Various 2AT derivatives demonstrated weak antimuscarinic and/or antihistaminic activities on superfused ileal segments. These data demonstrate that these agents possess a spectrum of pharmacological activity.
D015081:2-Naphthylamine / Q000031:analogs & derivatives / Q000494:pharmacology*; D000109:Acetylcholine / Q000378:metabolism; D000818:Animals; D003000:Clonidine / Q000494:pharmacology*; D004558:Electric Stimulation; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000494:pharmacology; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009281:Naphthalenes / Q000494:pharmacology*; D009538:Nicotine / Q000037:antagonists & inhibitors; D010276:Parasympatholytics / Q000494:pharmacology; D011188:Potassium / Q000494:pharmacology; D011804:Quinolines / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013764:Tetrahydronaphthalenes / Q000494:pharmacology*
D006634:Histamine H1 Antagonists; D009281:Naphthalenes; D010276:Parasympatholytics; D011804:Quinolines; D013764:Tetrahydronaphthalenes; C006561:2-aminotetralin; D009538:Nicotine; D015081:2-Naphthylamine; D003000:Clonidine; D000109:Acetylcholine; D011188:Potassium