G protein-coupled receptors (GPCRs) are the largest family of membrane receptors that activate intracellular signaling cascades and undergo endocytosis, recycling, or degradation upon stimulation. The (mu) m-, delta (d) and kappa (k) opioid receptors are GPCRs of the nervous system, which control pain, stress, and addictive behaviors. The kappa opioid receptor (KOR-1) plays a role in arousal and regulation of autonomic and neuroendocrine functions and is the receptor for dynorphins. KOR-1 inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance.