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Medetomidine-13C,d3 hydrochloride

MCE China：Medetomidine-13C,d3 hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-17034BS1

CAS：1216630-06-6

Synonyms：MPV785-13C,d3

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Medetomidine-13C,d3 (hydrochloride) is a deuterated labeled Medetomidine (hydrochloride). Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels.

In Vitro：Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].Medetomidine (0-1 μM, 1 h) hydrochloride inhibits aldosterone release from the adrenocortical cell suspension[8].Medetomidine (10 nM) hydrochloride activates a kicking response in Cyprids[9].Medetomidine (1 μM) hydrochloride increases cellular cAMP production by activating β-like receptors in CHO cells[9].

In Vivo：Medetomidine (200 μg/kg, p.o. or i.m.) hydrochloride induces a sedation in cats[5].Medetomidine (20 μg/kg, i.v.) hydrochloride shows sedative and analgesic effects in dogs[6].Medetomidine (0.05-0.3 mg/kg, s.c.) hydrochloride protects against Diazinon-induced toxicosis in mice[7].

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References：

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

[2]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

[3]. Kallio A, et al. Acute effects of medetomidine, a selective alpha 2-adrenoceptor agonist, on anterior pituitary hormone and cortisol secretion in man. Acta Endocrinol (Copenh). 1988 Sep;119(1):11-5.  [Content Brief]

[4]. R Virtanen, et al. Characterization of the selectivity, specificity and potency of medetomidine as an a2-adrenoceptor agonist.  [Content Brief]

[5]. O. B. Ansah, et al. Comparing oral and intramuscular administration of medetomidine in cats.

[6]. Kuo WC, et al. Comparative cardiovascular, analgesic, and sedative effects of medetomidine, medetomidine-hydromorphone, and medetomidine-butorphanol in dogs. Am J Vet Res. 2004 Jul;65(7):931-7.  [Content Brief]

[7]. Yakoub LK, et al. Medetomidine protection against diazinon-induced toxicosis in mice. Toxicol Lett. 1997 Sep 19;93(1):1-8.  [Content Brief]

[8]. Jager LP, et al. Effects of atipamezole, detomidine and medetomidine on release of steroid hormones by porcine adrenocortical cells in vitro. Eur J Pharmacol. 1998 Apr 3;346(1):71-6.  [Content Brief]

[9]. Ulrika Lind, et al. Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2-adrenoceptor agonist medetomidine.  [Content Brief]