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Curr Opin Investig Drugs. 2007 Sep;8(9):742-9.

Cardiovascular and renal effects of nociceptin/orphanin FQ: a new mediator to target?

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  • 1Doggrell Biomedical Communications, 14 Quandong Cresent, Nightcliff, NT 0810, Australia.


Nociceptin/orphanin FQ (N/OFQ) is the endogenous ligand for the N/OFQ peptide receptor. N/OFQ acts directly on blood vessels as a relaxant, and is unlikely to cross the blood-brain barrier due to its size. In anesthetized rats and conscious animals, intravenous N/OFQ produces transient hypotension and bradycardia that may involve interactions with the sympathetic and parasympathetic nervous systems. Injected intracerebro-ventricularly or directly into brain tissue, N/OFQ also affects the cardiovascular system. For example, N/OFQ causes water diuresis (aquaresis), which may represent the most immediate potential of targeting N/OFQ in the cardiovascular/ renal systems. Aquaretics are useful in the treatment of edema/hyponatremia which ultimately occurs in end-stage heart failure, liver cirrhosis and the syndrome of inappropriate secretion of antidiuretic hormone.

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