AM-251An inverse agonist of the CB1 receptor

AM-251 (CAS 183232-66-8)

AM-251 | CAS 183232-66-8 is rated 5.0 out of 5 by 1.
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Synonym: 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide
Application: An inverse agonist of the CB1 receptor
CAS Number: 183232-66-8
Purity: 98%
Molecular Weight: 555.24
Molecular Formula: C22H21Cl2IN4O
* Refer to Certificate of Analysis for lot specific data (including water content).
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AM-251 is a 123I radioisotope and potent CB1 receptor antagonist derivative of the CB1 cannabinoid receptor inverse agonist SR141716A, presenting a radioprobe for in vivo binding studies at the CB1 receptor with a higher affinity (Ki = 7.49 nM) for CB1 than the parent compound (Ki = 11.5 nM). AM-251 has been employed in competitive binding studies to identify CB1 affinity of different cannabimimetic agonists in vivo. Characterization of AM-251-CB1 association with SPECT (single photon emission computed tomography) has been described. AM-251 is also a potent activator of the GPR55 receptor.


References

1. Gatley, S.J., et al. 1997. Life Sci. 61: PL 191-PL 197. PMID: 9335234
2. Lan, R., et al. 1999. J. Med. Chem. 42: 769-776. PMID: 10052983
3. McLaughlin, P.J., et al. 2003. Behav Pharmacol. 14: 583-588. PMID: 14665975
4. Fong, T.M. and Heymsfield, S.B. 2009. Int J Obes. 33: 947-955. PMID: 19597516

Physical State :
Solid
Solubility :
Soluble in DMSO (~10 mg/ml), ethanol (~10 mg/ml), DMF (~10 mg/ml), and 1:3 DMSO:PBS (pH 7.2) (~14 mg/ml). Insoluble in water.
Storage :
Store at room temperature
Melting Point :
196-198° C
Density :
~1.7 g/cm3 (Predicted)
Refractive Index :
n20D 1.70 (Predicted)
IC50 :
Cannabinoid CB1 receptor: IC50 = 0.32 nM (human); [3H]SR-141716: IC50 = 0.59 nM (human CBR1 S383A mutant expressed in CHO cells); GPR55: EC5050 = 39 nM
Ki Data :
CB1 receptor: Ki= 7.5 nM
pK Values :
pKa: 11.31 (Predicted), pKb: 3.22 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
2125
MDL Number :
MFCD01861181
SMILES :
CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)I

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Certificate of Analysis

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AM-251  Product Citations

See how others have used AM-251. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 30620895  Askari, VR.|Shafiee-Nick, R.| et al. 2019. Life Sci. 219: 40-73.

PMID: # 23315130  Pai, WY. et al. 2013. Transgenic Res. 22: 823-38.

PMID: # 23251393  Chen, SW. et al. 2012. PLoS ONE. 7: e50850.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from McLaughlin et al McLaughlin et al. (PubMed ID 14665975) found that CB1 antagonist AM-251 suppressed appetite in rats. -SCBT Publication Review
Date published: 2015-07-04
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