Atipamezole

Research use only, not for human use.

Antipamezole (MPV-1248) is a potent, specific α2-adrenoceptor antagonist with Ki of 1.6 nM.

Antipamezole (MPV-1248) is a potent, specific α2-adrenoceptor antagonist with Ki of 1.6 nM; reverses the effects of the sedative dexmedetomidine and medetomidine as a veterinary drug.Alcoholism Phase 1 Discontinued.

The affinity of atipamezole for α2-adrenoceptors and its α2/α1 selectivity ratio are considerably higher than yohimbine.Atipamezole is not selective for subtypes of α2-adrenoceptors. It has negligible affinity for 5-HT1, 5-HT2 and I2 bindings sites.

Atipamezole is well tolerated in rodents. In anesthetized, normotensive rats, the cardiovascular effects of atipamezole (0.01–1 mg/kg, i.v.) are rather modest. Atipamezole is commonly used by veterinarians to awaken animals from sedation or anesthesia. Atipamezole increases sexual activity in rats and monkeys. In animals with sustained nociception, atipamezole increases pain-related responses by blocking the noradrenergic feedback inhibition of pain. Atipamezole at low doses has beneficial effects on alertness, selective attention, planning, learning, and recall in experimental animals, but not necessarily on short-term working memory.

MPV-1248 | MPV1248 | MPV 1248

GPCR/G Protein

Adrenergic Receptor

α2-adrenoceptor

Neurological Disease

Alcoholism

104054-27-5

212.2902

C14H16N2

>98% (HPLC)

DMSO: ≥30 mg/mL

CCC1(C2=CNC=N2)CC3=C(C=CC=C3)C1

1H-Imidazole, 5-(2-ethyl-2,3-dihydro-1H-inden-2-yl)-

(-20℃)

With Ice Pack

≥ 2 years