-type) nAChR. For nAChRs expressed in Xenopus oocytes, S- and R-mTFD-MPAB inhibited ACh-induced currents with IC50 values of 5 and 10 µM, respectively. Racemic mTFD-MPAB enhanced the equilibrium binding of [(3)H]ACh to nAChR-rich membranes (EC50 = 9 µM) and inhibited binding of the ion channel blocker [(3)H]tenocyclidine in the nAChR desensitized and resting states with IC50 values of 2 and 170 µM
that selectively binds to the open/active state of the NMDA receptor ion channel, displacing the binding of (3)H-tenocyclidine from the intrachannel binding site with an affinity of 2.4 nM. No significant binding was observed with 10 nM GE-179 at 60 other neuroreceptors, channels, or transporters. We describe the kinetic behavior of the radioligand in vivo in humans. Nine healthy participants (6 men, 3 women
of psychotomimetic effects. Abused recreational and legally controlled in most countries. * Remacemide: a low affinity antagonist also a sodium-channel blocker. * Rolicyclidine: a less potent analogue of phencyclidine, but seems to be seldom, if ever, abused. * Sevoflurane: an inhalational anesthetic. * Tenocyclidine: an analogue of phencyclidine that is more potent. * Tiletamine: an animal anesthetic.[49