![]() Phendimetrazine hydrochloride was first developed by Lilly (Itamar Pharmaceuticals, 1957, US patent # 2,891,567) for the treatment of obesity in both humans and animals. The noradrenaline transporter (NAT) is also less sensitive than the dopamine transporter to the inhibition of efflux by phendimetrazine. Catecholamine release induced by phendimetrazine is more sensitive than that caused by D-amphetamine. In animal studies, phendimetrazine is less sensitive than D-amphetamine to the antagonism of its actions by haloperidol. ![]() Phendimetrazine is also an agonist of the 5-HT2C receptor, with a degree of selectivity compared to other 5-HT2C receptor agonists. ![]() Desmethylphendimetrazine is an extremely potent sympathomimetic drug, which shows 10 to 100 times more potency than D-amphetamine. ![]() Phendimetrazine is a prodrug of D-amphetamine, which does not have a significant stimulant-like action by itself. Phendimetrazine and its metabolite desmethylphendimetrazine have been found to exert a greater degree of psychostimulant action in animals and in humans than D-amphetamine. ![]()
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