WIN 55,212-2 Mesylate

(+)-WIN 55,212-2 (mesylate) is a potent aminoalkyl indole cannabinoid (CB) receptor agonist with Ki values of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively. It shows antihyperalgesic and anti-inflammatory properties. It (0.01-100 nM) increases extracellular glutamate levels, displaying a bell-shaped concentration-response curve in primary cultures of rat cerebral cortex neurons. It also evokes CGRP release from trigeminal ganglion neurons in vitro (EC₅₀=26 μM) in a concentration- and calcium-dependent manner.