PSNCBAM-1

PSNCBAM-1 is a cannabinoid 1 (CB₁) receptor negative allosteric modulator (NAM).¹ It is selective for CB₁ over CB₂ in HEK293 cells expressing the human receptors (IC₅₀s = 74.3 and >10,000 nM, respectively). PSNCBAM-1 inhibits activation of the CB₁ receptor induced by (±)-CP 55,940 (Item No. 13241), anandamide (AEA; Item No. 90050), or 2-arachidonoyl glycerol (2-AG; Item No. 62160) in yeast expressing human CB₁ (IC₅₀s = 45.2, 37 and 230.3 nM, respectively). It reduces food intake within one hour and decreases body weight in male rats when administered at a dose of 30 mg/kg. PSNCBAM-1 (10 mg/kg) reduces THC-induced increases in tail-flick latency in mice.²

WARNING This product is not for human or veterinary use.

1. Horswill, J.G., Bali, U., Shaaban, S., et al. PSNCBAM-1, a novel allosteric antagonist at cannabinoid CB₁ receptors with hypophagic effects in rats. Br. J. Pharmacol. 152(5), 805-814 (2007).

2. Gamage, T.F., Farquhar, C.E., Lefever, T.W., et al. The great divide: Separation between in vitro and in vivo effects of PSNCBAM-based CB₁ receptor allosteric modulators. Neuropharmacology 125, 365-375 (2017).