SB-334867 is a non-peptide selective antagonist of the orexin OX1 receptor. SB-334867 blocks orexin-A induced calcium response with a pKb of 7.23. SB-334867 blocks increases in heart rate and body temperature induced by administratin of methamphetamine, and can inhibit the development of tolerance to the analgesic properties of morphine in rodent models. SB-334867 also shows anxiolytic and sedative effects.
Lateral hypothalamic orexin neuron activation leads to the development of morphine conditioned place preference, which is preferably blocked by SB-334867.