Harper's Illustrated Biochemistry, 33e.

Phendimetrazine Phendimetrazine and its metabolite desmethylphendimetrazine have been found to exert a greater degree of psychostimulant action in animals and in humans than Damphetamine. Phendimetrazine is a prodrug of D-amphetamine, which does not have a significant stimulant-like action by itself. Desmethylphendimetrazine is an extremely potent
sympathomimetic drug, which shows 10 to 100 times more potency than D-amphetamine. Phendimetrazine is also an agonist of the 5-HT2C receptor, with a degree of selectivity
compared to other 5-HT2C receptor agonists. In animal studies, phendimetrazine is less sensitive than D-amphetamine to the antagonism of its actions by haloperidol. Catecholamine
release induced by phendimetrazine is more sensitive than that caused by D-amphetamine. The noradrenaline transporter (NAT) is also less sensitive than the dopamine transporter to theinhibition of efflux by phendimetrazine. Contents Phendimetrazine hydrochloride was first developed by Lilly (Itamar Pharmaceuticals, 1957, US patent # 2,891,567) for the treatmentof obesity in both humans and animals. Phendimetrazine is marketed under the brand name Phendimetrazine Hydrochloride in the US and under the brand name Phendimetrazine inCanada. Phendimetrazine appeared on the market in the United States in 1968, in Canada in 1981, in the UK in 1982, and in Australia in 1987. In Russia, Sintez was the first drug
containing phendimetrazine. Phendimetrazine has been marketed as a diet pill for several decades in Russia, the former Soviet republics, and India. Phendimetrazine is one of the twomost-commonly used amphetamine stimulants in the US. Other common amphetamines include amphetamine, dextroamphetamine, and methamphetamine (meth). Only phendimetrazine
and its primary metabolite, desmethylphendimetrazine, are not classified as Schedule I controlled substances in the United States. Compared to other amphetamines, phendimetrazine hasa slightly longer duration of activity and a weaker subjective effect. However, this difference in the relative potency of phendimetrazine compared to other amphetamines has not been

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