PHARMACOLOGY OF Go-1002

¹ CIBA Research Centre, Goregaon, Bombay 63, India

Go-1002 (1-(5-methyl-1-phenyl-4-pyrazole-3-[4-(o-tolyl)-1-piperazinyl]-1-propanone hydrochloride) is a potent orally active hypotensive agent, with epinephrine-, amphetamine- and tyramine-blocking properties. It produces marked antihypertensive effects in renal hypertensive rats. It produces diminution of peripheral resistance by causing vasodilatation. This has been demonstrated in the isolated perfused hind limb and by measuring femoral artery blood flow. Its vasodilator action is seen in coronary vessels as well. It blocks centrally mediated vasomotor reflexes such as the carotid sinus occlusion reflex and the pressor response to stimulation of the central end of the vagus nerve. The vasopressor response elicited by stimulation of the posterior hypothalamus and reticular formation is markedly reduced by intraarterial injection of this compound. It produces a depletion of catecholamines from the heart, brain and adrenals. It does not possess any ganglionic blocking activity. It has central sedative tranquilizing properties and shows marked antiaggressive activity in rhesus monkeys.