5.04275
CB1 antagonist AM251
别名:
CB1 antagonist AM251, N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide, AM 251
form
solid
InChI
1S/C22H21Cl2IN4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-7-16(23)13-18(19)24)21(14)15-5-8-17(25)9-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30)
InChI key
BUZAJRPLUGXRAB-UHFFFAOYSA-N
assay
≥98% (HPLC)
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 10 mg/mL
storage temp.
10-30°C
Quality Level
Biochem/physiol Actions
Primary Target
CB₁ Receptor
CB₁ Receptor
Disclaimer
Toxicity: Standard Handling (A)
General description
A potent and highly selective antagonist for cannabinoid subtyre 1 (CB1) receptor. Affinity for CB1 (IC50 = 8 nM, Ki = 7.49 nM) is more than 306-fold higher than that for CB2 receptors. Has been used in a study to determine its interaction with hippocampal neurons to enhance spatial memory in mice.
Other Notes
Gatley, S., et al. 1996. Eur. J. Pharmacol.307, 331.
Gatley, S., et al. 1997. Life Sci.61, 191.
Lan, R., et al. 1999. J. Med. Chem.42, 769.
Pertwee, R., 2005. Life Sci.76, 1307.
Ryberg, E., et al. 2007. Br. J. Pharmacol.152, 1092.
Assini, F., et al. 2012. Behav. Pharmacol.23, 292.
Gatley, S., et al. 1997. Life Sci.61, 191.
Lan, R., et al. 1999. J. Med. Chem.42, 769.
Pertwee, R., 2005. Life Sci.76, 1307.
Ryberg, E., et al. 2007. Br. J. Pharmacol.152, 1092.
Assini, F., et al. 2012. Behav. Pharmacol.23, 292.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_c
Not applicable
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