| Bioactivity | Medetomidine is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine has sedative and analgesic effects. Medetomidine can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels[1][2][3][4]. | ||||||||||||
| Invitro | Medetomidine (0-1 µM, 1 h) inhibits aldosterone release from the adrenocortical cell suspension[7].Medetomidine (10 nM) activates a kicking response in Cyprids[8].Medetomidine (1 µM) increases cellular cAMP production by activating β-like receptors in CHO cells[8]. | ||||||||||||
| In Vivo | Medetomidine (200 μg/kg, p.o. or i.m.) induces a sedation in cats[4].Medetomidine (20 µg/kg, i.v.) shows sedative and analgesic effects in dogs[5].Medetomidine (0.05-0.3 mg/kg, s.c.) protects against Diazinon-induced toxicosis in mice[6]. Animal Model: | ||||||||||||
| Name | Medetomidine | ||||||||||||
| CAS | 86347-14-0 | ||||||||||||
| Formula | C13H16N2 | ||||||||||||
| Molar Mass | 200.28 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. 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. [3]. R Virtanen, et al. Characterization of the selectivity, specificity and potency of medetomidine as an a2-adrenoceptor agonist. [4]. O. B. Ansah, et al. Comparing oral and intramuscular administration of medetomidine in cats. [5]. 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. [6]. Yakoub LK, et al. Medetomidine protection against diazinon-induced toxicosis in mice. Toxicol Lett. 1997 Sep 19;93(1):1-8. [7]. 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. [8]. Ulrika Lind, et al. Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2-adrenoceptor agonist medetomidine. |