[Agonistic effects of ring opened serotonin analogs of the 3-(2-aminophenyl)-3-oxopropanamine type. Pharmacology of ring opened serotonin analogs].
Intrinsic activity and affinity of various synthesized ring-opened serotonin (5-HT) analogues including 3-(2-amino-5-hydroxy-phenyl)-3-oxo-propaneamine (I) were studied using the isolated gastric fundus of the rat. For I a relative intrinsic activity of 0.83 was measured while the affinity was nearly equal to 5-HT. For the N,N-dimethyl derivative of I (V) both intrinsic activity and affinity were identical to those of bufotenine (= N,N-dimethyl serotonin). The obtained results support the postulated three-point binding of 5-HT at its D receptor.
D000818:Animals; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects; D012701:Serotonin / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000502:physiology*
D011985:Receptors, Serotonin; D012701:Serotonin
Agonistisch wirksame ringoffene Serotonin-Analoga vom 3-(2-Aminophenyl)-3-oxo-propanamin-Typ. Pharmakologie ringoffener Serotonin-Analoga.