130466-38-5

130466-38-5 structure

Name: Vatinoxan hydrochloride
Chemical Name: N-[2-[(2R,12bS)-2'-oxospiro[1,3,4,6,7,12b-hexahydro-[1]benzofuro[2,3-a]quinolizine-2,5'-imidazolidine]-1'-yl]ethyl]methanesulfonamide,hydrochloride
CAS Number: 130466-38-5
Molecular Formula: C₂₀H₂₇ClN₄O₄S
Molecular Weight: 454.97100
Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
Create Date: 2017-05-31 23:21:05
Modify Date: 2024-01-08 11:42:05
Vatinoxan hydrochloride (MK-467 hydrochloride;L-659066 hydrochloride) is a peripheral α2 adrenergic receptor antagonist.

Name	N-[2-[(2R,12bS)-2'-oxospiro[1,3,4,6,7,12b-hexahydro-[1]benzofuro[2,3-a]quinolizine-2,5'-imidazolidine]-1'-yl]ethyl]methanesulfonamide,hydrochloride
Synonyms	Vatinoxan hydrochloride

Description	Vatinoxan hydrochloride (MK-467 hydrochloride;L-659066 hydrochloride) is a peripheral α2 adrenergic receptor antagonist.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Neurological Disease
Target	α2 adrenergic receptor[1]
In Vivo	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].
Animal Admin	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.

Molecular Formula	C₂₀H₂₇ClN₄O₄S
Molecular Weight	454.97100
Exact Mass	454.14400
PSA	106.76000
LogP	3.22850
Storage condition	2-8℃

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