Bioactivity | PM226 is a selective cannabinoid CB2R agonist (Ki (CB2R)=13 nM; EC50 (CB2R)=39 nM; Ki (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo[1]. |
Invitro | PM226 binds selectively to CB2 receptor with an affinity in the nanomolar range (Ki=12.8±2.4 nM). PM226 has negligible affinity for the CB1 receptor (Ki >40000 nM) and no activity at the GPR55. PM226 was also evaluated in GTPγS binding assays specific to the CB2 receptor showing agonist activity (EC50=38.67±6.70 nM)[2]. |
In Vivo | PM226 (0.1, 1 and 10 mg/kg; administered i.p.) administration decreases the volume of the striatal lesion caused by Malonate[2]. Animal Model: |
Name | PM226 |
CAS | 1949726-13-9 |
Formula | C22H31NO3 |
Molar Mass | 357.49 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Gemma Navarro, et al. Targeting Cannabinoid CB2 Receptors in the Central Nervous System. Medicinal Chemistry Approaches with Focus on Neurodegenerative Disorders. Front Neurosci. 2016 Sep 13;10:406. [2]. M Gómez-Cañas, et al. Biological characterization of PM226, a chromenoisoxazole, as a selective CB2 receptor agonist with neuroprotective profile. Pharmacol Res. 2016 Aug;110:205-215. |