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