Английская Википедия:Buprenorphine-3-glucuronide

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Версия от 19:32, 12 февраля 2024; EducationBot (обсуждение | вклад) (Новая страница: «{{Английская Википедия/Панель перехода}} {{Short description|Chemical compound}} {{Drugbox | IUPAC_name = (5α,6β,14β,18R)-17-(Cyclopropylmethyl)-18-[(2S)-2-hydroxy-3,3-dimethyl-2-butanyl]-6-methoxy-18,19-dihydro-4,5-epoxy-6,14-ethenomorphinan-2-yl β-D-glucopyranosiduronic acid | image = Buprenorphine-3-glucuronide.svg | CAS_number_Ref = {{cascite|correct|CAS}} | CAS_number = 101224-22-0 | UNII_Ref = {{f...»)
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Buprenorphine-3-glucuronide (B3G) is a major active metabolite of the opioid modulator buprenorphine.[1] It has affinity for the μ-opioid receptor (Ki = 4.9 (± 2.7) pM), δ-opioid receptor (Ki = 270 nM), and nociceptin receptor (Ki = 36 μM), but not for the κ-opioid receptor.[1] Whether B3G acts as an agonist or antagonist of each of the former three respective sites has yet to be determined.[2] In rats, at the doses assayed, B3G has been found to produce a small degree of antinociception, and similarly to buprenorphine in these assays, has not been found to produce sedation, reduce locomotion, or decrease respiratory rate.[1] Of all of the active metabolites of buprenorphine, B3G is thought to be the most similar to the parent drug.[1] Unlike norbuprenorphine, but similarly to buprenorphine (and norbuprenorphine-3-glucuronide), B3G is not a substrate for P-glycoprotein, and hence may cross the blood-brain-barrier significantly.[2]

See also

References

Шаблон:Reflist

Шаблон:Opioidergics


Шаблон:Analgesic-stub