Description
CTEP, also known as RO4956371, is a potent, long-acting, orally bioavailable allosteric antagonist ofmglu5 receptor with IC50 of 2.2nM. CTEP bindsmglu5 with low nanomolar affinity and shows >1000-fold selectivity when tested against 103 targets, including all knownmglu receptors. CTEP penetrates the brain with a brain/plasma ratio of 2.6 and displaces the tracer ABP688 in vivo in mice from brain regions expressingmglu5 with an average ED (50) equivalent to a drug concentration of 77.5 ng/g in brain tissue