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An active metabolite results when a drug is metabolized by the body into a modified form which produces effects in the body. Usually these effects are similar to those of the parent drug but weaker, [citation needed] although they can still be significant (see e.g. 11-hydroxy-THC, morphine-6-glucuronide).
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Using cloned α 1 G, α 1 H, and α 1 I T-type calcium channels, Gomora's team found that ethosuximide blocked the channels with an IC 50 of 12 ± 2 mmol/L and that of N-desmethylmethsuximide (the active metabolite of mesuximide) is 1.95 ± 0.19 mmol/L for α 1 G, 1.82 ± 0.16 mmol/L for α 1 I, and 3.0 ± 0.3 mmol/L for α 1 H. It was ...
In biochemistry, a metabolite is an intermediate or end product of metabolism. [1] The term is usually used for small molecules.Metabolites have various functions, including fuel, structure, signaling, stimulatory and inhibitory effects on enzymes, catalytic activity of their own (usually as a cofactor to an enzyme), defense, and interactions with other organisms (e.g. pigments, odorants, and ...
11-Hydroxy-Δ 9-tetrahydrocannabinol (11-OH-Δ 9-THC, alternatively numbered as 7-OH-Δ 1-THC), usually referred to as 11-hydroxy-THC is the main active metabolite of tetrahydrocannabinol (THC), which is formed in the body after Δ 9-THC is consumed.
Enalaprilat is the active metabolite of enalapril. It is the first dicarboxylate-containing ACE inhibitor and was developed partly to overcome these limitations of captopril. The thiol functional group of captopril was replaced with a carboxylic acid group, but additional modifications were required to achieve a potency similar to captopril.
Nabumetone is a non-acidic NSAID prodrug that is rapidly metabolized in the liver to the active metabolite, 6-methoxy-2-naphthyl acetic acid. Nabumetone's active metabolite inhibits the cyclooxygenase enzyme and preferentially blocks COX-2 activity (which is indirectly responsible for the production of inflammation and pain during arthritis ...
Phenylethylmalonamide (PEMA) is an active metabolite of the anticonvulsant drug primidone, although it is produced in a much lower concentration than phenobarbital, the other active metabolite. [ 1 ] References