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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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6β-Hydroxy-7α-thiomethylspironolactone (6β-OH-7α-TMS) is a steroidal antimineralocorticoid of the spirolactone group and a major active metabolite of spironolactone. [1] [2] [3] Other important metabolites of spironolactone include 7α-thiospironolactone (7α-TS; SC-24813), 7α-thiomethylspironolactone (7α-TMS; SC-26519), and canrenone (SC-9376).
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 ...
Norbuprenorphine-3-glucuronide (N3G) is a major active metabolite of the opioid modulator buprenorphine. [1] It has affinity for the κ-opioid receptor (K i = 300 nM) and the nociceptin receptor (K i = 18 μM), but not for the μ-or δ-opioid receptors. [1]
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.
3-Monoacetylmorphine (3-MAM) or 3-acetylmorphine is a less active metabolite of heroin (diacetylmorphine), the other two being morphine and more active 6-monoacetylmorphine (6-MAM). Because of the acetyl-group in 3-position, 3-MAM has relatively weak affinity to μ-opioid receptors .
Noroxycodone is the major metabolite of the opioid analgesic oxycodone. [1] [2] [3] It is formed from oxycodone in the liver via N-demethylation predominantly by CYP3A4.[1] [2] [3] Noroxycodone binds to and activates the μ-opioid receptor (MOR) similarly to oxycodone, although with one-third of the affinity of oxycodone and 5- to 10-fold lower activational potency.