No correlation exists between antidepressant activity and the ability of 5-HT uptake inhibitors to interact with 5-HT receptors of the rat stomach fundus strip.
Several 5-HT uptake inhibitors, established and potential antidepressant drugs, were tested for their ability to counteract contractions of the rat isolated stomach fundus strip induced by 5-HT and BaCl2. Of 12 inhibitors tested, only doxepine, amitriptyline, clomipramine, imipramine, Ro 11-2465 (cyan-imipramine), citalopram and fluvoxamine antagonized the contraction induced by 10(-6) M 5-HT with IC50 values below 10(-4) M. Amitriptyline, doxepine and cyproheptadine, at concentrations inhibiting the effect of 5-HT, did not antagonize the strip contractions induced by 3 X 10(-3) M BaCl2, while the remaining compounds that antagonized 5-HT-induced contractions, also antagonized--with at least a similar potency--the contractions induced by BaCl2. From among antidepressant compounds investigated, only doxepine and amitriptyline may be regarded as antagonists of the 5-HT receptor in the rat stomach strip.
D000818:Animals; D000929:Antidepressive Agents, Tricyclic / Q000494:pharmacology*; D001464:Barium / Q000037:antagonists & inhibitors; D017609:Barium Compounds; D002712:Chlorides; D003533:Cyproheptadine / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000187:drug effects*; D012701:Serotonin / Q000378:metabolism; D012702:Serotonin Antagonists / Q000494:pharmacology*; D013270:Stomach / Q000187:drug effects
D000929:Antidepressive Agents, Tricyclic; D017609:Barium Compounds; D002712:Chlorides; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C024986:barium chloride; D001464:Barium; D003533:Cyproheptadine; D012701:Serotonin