REVIEW Atipamezole (brand name Antisedan, Pfizer) is a synthetic alpha2-adrenergic antagonist with an imidazole structure, indicated for the reversal of the sedative and analgesic effects of dexmedetomidine and medetomidine in dogs. It has also been researched in humans as a potential anti-Parkinsonian drug. Receptor binding studies indicate that its affinity for alpha2-adrenoceptors and its alpha2/alpha1 selectivity ratio are considerably higher than those of yohimbine, the prototype alpha2-adrenoceptor antagonist. Atipamezole is not selective for subtypes of alpha2-adrenoceptors. Unlike many other alpha2-adrenoceptor antagonists, it has negligible affinity for 5-HT1A and I2 binding sites.
Karjalainen, Arto Johannes; Virtanen, Raimo Einari; Karjalainen, Arja Leena; Kurkela, Kauko Oiva Antero Substituted imidazole derivatives and their use Eur. Pat. Appl. (1986), EP 183492 A1 19860604.
Honkavaara, Juhana M.; Raekallio, Marja R.; Kuusela, Erja K.; Hyvarinen, Esko A.; Vainio, Outi M. The effects of L-659,066, a peripheral alpha2-adrenoceptor antagonist, on dexmedetomidine-induced sedation and bradycardia in dogs Veterinary Anaesthesia and Analgesia (2008), 35(5), 409-413.
Talukder, Md. Hasanuzzaman; Hikasa, Yoshiaki; Takahashi, Hajime; Sato, Kanako; Matsuu, Aya Antagonistic effects of atipamezole and yohimbine on medetomidine-induced diuresis in healthy dogs. Canadian Journal of Veterinary Research (2009), 73(4), 260-270.
Pertovaara A, Haapalinna A, Sirviö J, Virtanen R. Pharmacological properties, central nervous system effects, and potential therapeutic applications of atipamezole, a selective alpha2-adrenoceptor antagonist. CNS Drug Rev. 2005 Autumn;11(3):273-88.
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