A 5-HT2C receptor agonist
ORG 12962 is an agonist of the serotonin (5-HT) receptor subtype 5-HT2C with an EC50 value of 97.72 nM in a FLIPR-based intracellular calcium assay using CHO-K1 cells expressing the human receptor.1 It is selective for 5-HT2C over 5-HT2A and 5-HT2B receptors (EC50s = 419.87 and 524.81 nM, respectively). ORG 12962 (1 and 3.2 mg/kg) has anti-aversive effects in a rat model of panic anxiety induced by dorsolateral periaqueductal gray matter (dPAG) stimulation.2
1.Porter, R.H.P., Benwell, K.R., Lamb, H., et al.Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cellsBr. J. Pharmacol.128(1)13-20(1999) 2.Jenck, F., Moreau, J.-L., Berendsen, H.H.G., et al.Antiaversive effects of 5HT2C receptor agonists and fluoxetine in a model of panic-like anxiety in ratsEur. Neuropsychopharmacol.8(3)161-168(1998)
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