PM 226

Names

[ CAS No. ]:
1949726-13-9

[ Name ]:
PM 226

Biological Activity

[Description]:

PM226 is a selective cannabinoid CB2R agonist (Ki (CB2)=13 nM; EC50 (CB2)=39 nM; Ki (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo[1].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor

[Target]

CB2:13 nM (Ki)

CB2:39 nM (EC50)

[In Vitro]

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: Malonate-lesioned adult (12 week old; 350-400 g) male Wistar rats[2] Dosage: 0.1, 1 and 10 mg/kg Administration: Administered i.p. Result: Reduced the volume of edema observed in Malonate-lesioned rats at the dose of 1 mg/kg.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₃₁NO₃

[ Molecular Weight ]:
357.49

PM 226

Names

Biological Activity

Chemical & Physical Properties

Related Compounds