Design of Potent and Selective Agonists for the Human Vasopressin V1b Receptor Based on Modifications of [Deamino-Cys]arginine Vasopressin at Position 4
| Autor: | Maurice Manning, Stoytcho Stoev, Ana Pena, Ling Ling Cheng, Gilles Guillon, Mohamed Ben Mimoun, Sylvain Derick |
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| Rok vydání: | 2004 |
| Předmět: |
Arginine vasopressin receptor 1B
chemistry.chemical_classification Agonist medicine.medical_specialty Vasopressin Arginine Chemistry Stereochemistry medicine.drug_class Peptide chemistry.chemical_compound Endocrinology Oxytocin Internal medicine Drug Discovery medicine Peptide synthesis Molecular Medicine Receptor medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry. 47:2375-2388 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | The glutamine4 residue in [deamino-Cys1]arginine vasopressin (dAVP) was replaced by a broad series of aliphatic, aromatic, polar, and charged amino acids to give the following peptides: d[Gly4]AVP (1), d[Ala4]AVP (2), d[Abu4]AVP (3), d[Nva4]AVP (4), d[Nle4]AVP (5), d[Leu4]AVP (6), d[Ile4]AVP (7), d[Thi4]AVP (8), d[Phe4]AVP (9), d[Tyr4]AVP (10), d[Trp4]AVP (11), d[Asn4]AVP (12), d[Ser4]AVP (13), d[Thr4]AVP (14), d[Dap4]AVP (15), d[Dab4]AVP (16), d[Orn4]AVP (17), d[Lys4]AVP (18), d[Arg4]AVP (19), d[Har4]AVP (20), and d[Glu4]AVP (21). All peptides were synthesized by solid-phase methods using BOC chemistry for all but one peptide (8), which required the use of Fmoc chemistry. The binding and functional properties of these position 4 substituted analogues of dAVP (d[X4]AVP) and the previously reported d[Cha4]AVP (Derick et al. Endocrinology 2002, 143, 4655−4664) were evaluated on human arginine vasopressin (AVP) V1a, V1b, and V2 receptors and on the human oxytocin (OT) receptor expressed in living Chinese ha... |
| Databáze: | OpenAIRE |
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