Atipamezole is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug. Atipamezole hydrochloride (MPV-1248 hydrochloride) is hydrochloride form of atipamezole.

α2-adrenoceptor antagonist:1.6 nM（Ki）.

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[1].

Atipamezole has been found to be well tolerated in rodents and displays only modest cardiovascular effects at dosages ranging from 0.01–1 mg/kg, administered intravenously, in anesthetized, normotensive rats. This compound is frequently utilized by veterinarians to reverse sedation or anesthesia in animals. Additionally, it has been observed to enhance sexual activity in both rats and monkeys. In situations of sustained nociception, atipamezole augments pain-related responses by inhibiting the noradrenergic feedback mechanism that normally suppresses pain. Furthermore, at low doses, atipamezole positively affects several cognitive functions in experimental animals, including alertness, selective attention, planning, learning, and recall, though its impact on short-term working memory remains unclear.