Characterization And Pharmacology Of Receptors For Gastrointestinal Peptides

National Institute Of Diabetes And Digestive And Kidney Diseases

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Abstract

During the year the receptor pharmacology and molecular pharmacology of primarily of the bombesin receptor family (GRPR, NMBR, BRS-3) was investigated as well as publishing a number of expert opinions of advances in this field. The molecular basis of selectivity of a newly described antagonist for the orphan receptor, BRS-3 receptor, which is a member of the Bn family of receptors, Bantag-1, was determined and published, which should help in the design of future selective ligands for this receptor. Inn collaboration with Prof M Leopolo of the f Universit degli Studi di Bari Aldo Moro, Bari, Italy. a number of potential small molecule inhibitors of Bombesin receptors were screened. Two were discovered to function as BnR antagonists, AM-37 and ST-36. In the micro molar rage each of these inhibited BB1, BB2 and BB3 activation and may be useful as templates to develop more potent antagonistic analogues. In addition, the pharmacological selectivity of newly described chiral diazepine antagonists for the BRS-3 receptor over the closely related GRPR and NBMR was determined.