阿替美唑，Atipamezole；≥98% (HPLC)

Atipamezole has an imidazole structure and gets localized in the central nervous system on administration.[1]

 

Atipamezole has been used as a α2-adrenoceptor antagonist in mesencephalic trigeminal nucleus (MTN) neurons,[2] CD4+ T-lymphocyte[3] and human embryonic kidney (HEK293) membrane preparation.[4]

 

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.[1] Atipamezole shows no affinity towards muscarinic[1] and dopamine or neurotransmitter receptors.[5] Atipamezole when used along with morphine elicits antinociceptive effects.[6]

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.

 

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