BPTU (BMS-646786) is a potent, highly selective and allosteric antagonist of P2Y1 receptor with Ki of 6 nM for hP2Y1.
BPTU shows no significant affinity for hP2Y2/6/11/12/14 (Ki>5 uM).
BPTU inhibits purinergic inhibitory junction potentials and inhibition of spontaneous motility induced by electrical field stimulation in the colon of rats (EC50 = 0.3 uM) and mice (EC50 = 0.06 uM).
BPTU also blocks nicotine induced relaxation, has reasonable plasma exposure, clearance and half-life with moderate oral bioavailability.
