MEDI 238 |
| The nociceptin receptor, NOP, is a G protein-coupled receptor that was cloned in 1994. It bears high homology to the classic opioid receptors, but has little cross reactivity with their native ligands. Nociceptin, the endogeneous ligand to NOP, was discovered in 1995 and shown to be a peptide ligand that activates the NOP receptor, but not the classic opioid receptors. Intensive pharmacological studies with the nociceptin receptor and its peptide ligand and analogs over the past several years have resulted in significant advances in understanding the interaction of nociceptin with biological systems. In our in-house studies, either central (ICV) or peripheral (IV) administration of nociceptin in conscious guinea pigs produces inhibition of capsaicin induced cough. In this presentation, we will disclose part of our studies in the nociceptin receptor area as an effort to identify a small molecule nociceptin receptor agonist for the management of cough. The synthesis, SAR development of 1, PK and in vivo activity of selected compounds will be presented.
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General Oral Session
1:30 PM-4:50 PM, Tuesday, August 21, 2007 BCEC -- 210A, Oral
Division of Medicinal Chemistry |
