Atipamezole has an imidazole structure and gets localized in the central nervous system on administration.

Atipamezole has been used as a α2-adrenoceptor antagonist in mesencephalic trigeminal nucleus (MTN) neurons, CD4+ T-lymphocyte and human embryonic kidney (HEK293) membrane preparation.

Atipamezole elicits affinity towards adrenoreceptor subtypes namely α2A, α2B and α2C. High levels of atipamezole impairs cognitive functions. It also reverses the adrenoreceptor agonist functionalities. Atipamezole shows no affinity towards muscarinic and dopamine or neurotransmitter receptors. Atipamezole when used along with morphine elicits antinociceptive effects.

Atipamezole is a selective α₂ adrenergic blocker. Atipamezole is more potent than yohimbine; it is very selective for α₂ adrenergic vs α₁ sites, but not selelctive for α₂ subtypes.

Atipamezole is a selective α₂ adrenergic blocker; neutral antagonist

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