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Vatinoxan hydrochloride (MK-467 hydrochloride) Sale

(Synonyms: MK-467 hydrochloride; L-659066 hydrochloride) 目录号 : GC30938

Vatinoxan hydrochloride (MK-467 hydrochloride) (MK-467 hydrochloride;L-659066 hydrochloride) 是一种外周 α2 肾上腺素能受体拮抗剂。

Vatinoxan hydrochloride (MK-467 hydrochloride) Chemical Structure

Cas No.:130466-38-5

规格 价格 库存 购买数量
10mM (in 1mL Water)
¥9,326.00
现货
5mg
¥8,479.00
现货
25mg
¥32,130.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

Vatinoxan hydrochloride (MK-467 hydrochloride;L-659066 hydrochloride) is a peripheral α2 adrenergic receptor antagonist.

Vatinoxan alone increases cardiac index and tissue oxygen delivery and has no deleterious adverse effects. Vatinoxan attenuates or prevents dexmedetomidine’s systemic hemodynamic effects in a dose-dependent manner when given simultaneously i.v. but has no effect on the pulmonary outcome in conscious dogs. A 50:1 dose ratio (Vatinoxan:dexmedetomidine) induces the least alterations in cardiovascular function[1]. Vatinoxan dose-dependently attenuates the bradycardia associated with dexmedetomidine, and shortens the sedative effect without altering its quality. Vatinoxan may be useful in attenuating reductions in heart rate in conscious catsadministered dexmedetomidine[2].

[1]. Honkavaara JM, et al. The effects of increasing doses of MK-467, a peripheral alpha(2)-adrenergic receptor antagonist, on the cardiopulmonary effects of intravenous dexmedetomidine in conscious dogs. J Vet Pharmacol Ther. 2011 Aug;34(4):332-7. [2]. Honkavaara J, et al. The effect of MK-467, a peripheral α2-adrenoceptor antagonist, on dexmedetomidine-inducedsedation and bradycardia after intravenous administration in conscious cats. Vet Anaesth Analg. 2017 Feb 22. pii: S1467-2987(16)31387-3.

实验参考方法

Animal experiment:

Dogs[1]Eight dogs receive either dexmedetomidine (10 μg/kg), Vatinoxan (250 μg/kg or dexmedetomidine (10 μg/kg) with increasing doses of Vatinoxan (250 μg/kg, 500 μg/kg and 750 μg/kg). Treatments are given intravenously (i.v.) in a randomized, crossover design with a 14-day ishout period. Systemic hemodynamics and arterial blood gas analyses are recorded at baseline and at intervals up to 90 min after drugs administration[1].Cats[2]Cats are administered seven IV treatments are administered at least 2 weeks apart, consisting of dexmedetomidine 12.5 μg/kg (D12.5) and 25 μg/kg (D25), Vatinoxan 300 μg/kg (M300), and D25 combined with 75, 150, 300 and 600 μg/kg of Vatinoxan (D25M 75, D25M150, D25M300 and D25M600, respectively). Heart rates (HR) are recorded via telemetry and sedation assessed with a simple descriptive score and a visual analogue scale prior to treatments and at intervals until 8 hours thereafter[2].

References:

[1]. Honkavaara JM, et al. The effects of increasing doses of MK-467, a peripheral alpha(2)-adrenergic receptor antagonist, on the cardiopulmonary effects of intravenous dexmedetomidine in conscious dogs. J Vet Pharmacol Ther. 2011 Aug;34(4):332-7.
[2]. Honkavaara J, et al. The effect of MK-467, a peripheral α2-adrenoceptor antagonist, on dexmedetomidine-inducedsedation and bradycardia after intravenous administration in conscious cats. Vet Anaesth Analg. 2017 Feb 22. pii: S1467-2987(16)31387-3.

化学性质

Cas No. 130466-38-5 SDF
别名 MK-467 hydrochloride; L-659066 hydrochloride
化学名 N-(2-((2R,12bS)-2'-oxo-1,3,4,6,7,12b-hexahydrospiro[benzofuro[2,3-a]quinolizine-2,4'-imidazolidin]-3'-yl)ethyl)methanesulfonamide hydrochloride
Canonical SMILES [H]Cl.CS(=O)(NCCN([C@]1(CN2)CCN3CCC4=C(OC5=CC=CC=C54)[C@]3([H])C1)C2=O)=O
分子式 C20H27ClN4O4S 分子量 454.97
溶解度 Water : ≥ 133 mg/mL (292.33 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.1979 mL 10.9897 mL 21.9795 mL
5 mM 0.4396 mL 2.1979 mL 4.3959 mL
10 mM 0.2198 mL 1.099 mL 2.1979 mL
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