Nociceptin/orphanin phenylalanine glutamine (FQ) receptor and cardiovascular disease.

Nociceptin/Orphanin FQ (N/OFQ) is the endogenous ligand for the N/OFQ receptor. N/OFQ acts directly on blood vessels to elicit vasodilation. This review will describe the peripheral cardiovascular effects of N/OFQ observed in studies conducted in vitro and in vivo, along with those designed to characterize systemic cardiovascular effects resulting from direct injection into brain tissue. Emphasis is placed on the cerebrovascular action of N/OFQ and its function considered in the setting of central nervous system (CNS) pathology. Although N/OFQ is unlikely to cross the blood-brain barrier because of its size, use of N/OFQ antagonists to alleviate the potentially deleterious action of centrally released N/OFQ may be of therapeutic importance in treatment of cerebral ischemia of diverse origin, such as stroke and traumatic brain injury. Targeting N/OFQ may also be of therapeutic importance in alleviating the hyperemia and pain associated with joint inflammation.