[Effects of the partial dopamine receptor agonist, terguride, on the field-stimulated vas deferens in the mouse].
Transdihydrolisuride (terguride), a 9,10-dihydrogenated analogue of the ergot dopamine agonist lisuride, is characterized as partial dopamine receptor agonist at CNS level. This compound was investigated for its effects on peripheral neurotransmission in the attempt to delineate its pharmacological profile. The contractile responses of field-stimulated mouse vas deferens were slightly inhibited by terguride at very high concentrations (10(-5)-10(-2) M); the selective antagonists for alpha 2-adrenergic and dopamine receptors failed to counteract this effect. Terguride was very effective in blocking the inhibitory effects of LY 171555 (selective DA2 agonist), SK&F 38393 (selective DA1 agonist) and clonidine (selective alpha 2 agonist). In no case the antagonism was competitive: the control dose-response curves were not shifted in a parallel and dose-dependent manner. Therefore terguride displays a mixed DA1, DA2 and alpha 2 antagonistic activity.
Carratù
M R
MR
Istituto di Farmacologia, Università di Bari.
De Serio
A
A
Lagioia
R
R
Conte-Camerino
D
D
Ferrari
E
E
Mitolo-Chieppa
D
D
D000818:Animals; D015259:Dopamine Agents / Q000494:pharmacology*; D004558:Electric Stimulation; D004873:Ergolines / Q000494:pharmacology*; D066298:In Vitro Techniques; D008090:Lisuride / Q000031:analogs & derivatives / Q000494:pharmacology*; D008297:Male; D051379:Mice; D009130:Muscle, Smooth / Q000187:drug effects*; D014649:Vas Deferens / Q000187:drug effects
D015259:Dopamine Agents; D004873:Ergolines; C006208:dironyl; D008090:Lisuride
Effetti di un agonista dopaminergico parziale, terguride, sul dotto deferente elettrostimolato di topo.