104075-48-1 Atipamezole HCl AKSci J61470
 
 
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  J61470    
Atipamezole HCl, 95%
 
1H-Imidazole, 4-(2-ethyl-2,3-dihydro-1H-inden-2-yl)-, monohydrochloride
IDENTITY
CAS Number:104075-48-1
MDL Number:MFCD06407819
MF:C14H17ClN2
MW:248.75
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:95%
Physical Form (at 20°C):Solid
Melting Point:211-225°C
Long-Term Storage:Store long-term at 2-8°C
DOT/IATA TRANSPORT INFORMATION
Not hazardous material

BIOLOGICAL INFO
Solubility:Soluble in water (100 mM) and DMSO (100 mM)
Application(s):A selective alfa2-adrenergic receptor antagonist
Form:HCl salt

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.

REFERENCES
[1]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.
[2] 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.
[3] 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.
[4] 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.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501

Current as of April 25, 2024


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CATEGORIES
 APIs and Bioactives > Alpha Blockers


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