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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).
This page was last edited on 16 October 2013, at 12:38 (UTC).; Text is available under the Creative Commons Attribution-ShareAlike 4.0 License; additional terms may apply.
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.
Metabolism (/ m ə ˈ t æ b ə l ɪ z ə m /, from Greek: μεταβολή metabolē, "change") is the set of life-sustaining chemical reactions in organisms.The three main functions of metabolism are: the conversion of the energy in food to energy available to run cellular processes; the conversion of food to building blocks of proteins, lipids, nucleic acids, and some carbohydrates; and the ...
This page was last edited on 28 December 2023, at 09:37 (UTC).; Text is available under the Creative Commons Attribution-ShareAlike 4.0 License; additional terms may apply.
The active metabolites in humans: 67M-1, 67M-2 and 67M-4 (top to bottom) Febuxostat has three active metabolites in humans, which are formed mainly by a number of cytochrome P450 liver enzymes (CYP1A1, 1A2, 2C8, 2C9). One of them is a dicarboxylic acid, the other two are hydroxylated derivatives.
Selexipag, sold under the brand name Uptravi, is a medication developed by Actelion for the treatment of pulmonary arterial hypertension (PAH). [3] [4] Selexipag and its active metabolite, ACT-333679 (or MRE-269, the free carboxylic acid), are agonists of the prostacyclin receptor, which leads to vasodilation in the pulmonary circulation. [5]