Melanocortin receptor subtypes

Lapinsh, M., Prusis, P., Mutule, L, Mutulis, F., and Wikberg, J.E.S. QSAR and proteo-chemometric analysis of the interaction of a series of organic compounds with melanocortin receptor subtypes./. Med. Chem. 2003, 46, 2572-2579. 

Interaction of Organic Compounds with Melanocortin Receptor Subtypes... 

Figure 4 Selective nonpeptide modulators of melanocortin receptor subtypes. The MC4 R selective compound seems to affect sexual function, and the MCI R selective compound possess anti-inflammatory activity.

Other more recent examples of new receptor subt)rpes include neurokinin, melanocortin and somatostatin receptor subt)q)es. Neurokinins (substance P, neurokinin A and neurokinin B) act at three receptor subtypes NK, NK2 and NK3. Selective ligands are being... 

Numerous examples exist where variant-selective ligands have been used to dissect complex hormone signaling pathways, but one of the best examples of the use of selective ligands to uncover the function of very disparate receptor variants is the case of the melanocortin receptor. The melanocortin receptor family is a group of five receptor subtypes that belong to... 

Richardson TI, Qmstein PL, Briner K, et al. Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor. / Med Chem 2004 47 744-55. 

Scheme 52 Synthesis of W-functionalised sultams as selective human melanocortin subtype-4 receptor ligands...

Addition of Aldehydes. Secondary alcohols are formed via addition of 2-lithio-l-methylimidazole to benzaldehydes, providing access to bioactive substrates such as selective angiotensin IIAT2 receptor antagonists, and melanocortin subtype-4 receptors (eqs... 

Figure 13.24 Chemoenzymatic access to methyl (R)-4-fluorophenylalanine hydrochloride used for the preparation of a melanocortin subtype-4 receptor partial agonist to combat obesity.

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