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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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Like other 11-OH cannabinoid metabolites, 11-OH-9β-HHC retains activity comparable to HHC itself while the 9α-isomer is significantly less active. [5] However, upon formation it is rapidly metabolized further to the inactive 11-carboxylates, producing a shortened half-life within the body and lowering its bioavailability considerably through ...
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 ...
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.
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This analgesic activity of M6G (in animals) was first noted by Yoshimura. [5]Subsequent work at St Bartholomew's Hospital, London in the 1980s, [6] using a sensitive and specific high-performance liquid chromatography assay, [7] accurately defined for the first time the metabolism of morphine, and the abundance of this metabolite (along with morphine-3-glucuronide, [8] considered an inactive ...
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