Selective antagonist of vasopressin V1A receptor that inhibits vasopressin and oxytocin-induced increases in intracellular calcium concentrations in vitro (IC50 values are 5 and 30 nM respectively). Exhibits potent and prolonged antivasopressor activity and induces anxiolytic-like effects in the dorsal, but not ventral, hippocampus in vivo.
CAT No: R1081
CAS No:73168-24-8
Synonyms/Alias:Manning Compound, [Pmp1, Tyr(OMe)2, Arg8] Vasopressin; β-Mercapto-β,β-cyclopentamethylene-propionyl-Tyr(Me)-Phe-Gln-Asn-Cys-Pro-Arg-Gly-NH2 trifluoroacetate salt (Disulfide bond)
(d(CH2)51,Tyr(Me)2,Arg8)-Vasopressin is a synthetic peptide analog of the neurohypophyseal hormone vasopressin, engineered with specific amino acid modifications to confer altered receptor selectivity and enhanced metabolic stability. As a member of the vasopressin peptide family, this compound is distinguished by its substitution of the disulfide bridge with a methylene thioether linkage, methylation of tyrosine residues, and an arginine substitution at position 8. These structural features make it a valuable molecular tool for dissecting vasopressin receptor pharmacology, investigating signaling pathways, and developing novel approaches to peptide-based research in neuroendocrinology and receptor biology.
Receptor Selectivity Studies: Researchers employ this vasopressin analog to explore the binding affinities and functional selectivity among vasopressin receptor subtypes, such as V1a, V1b, and V2 receptors. The unique structural modifications in the peptide confer distinct interaction profiles compared to native vasopressin, enabling the precise mapping of receptor-ligand interactions and downstream signaling events. Such studies are fundamental for elucidating the molecular determinants of receptor specificity and for designing future ligands with targeted pharmacological properties.
Signal Transduction Research: The compound is frequently utilized to probe intracellular signaling cascades initiated by vasopressin receptor activation. Its metabolic stability and receptor selectivity facilitate detailed investigations into G protein-coupled receptor (GPCR) signaling mechanisms, including second messenger generation, kinase activation, and gene expression modulation. These insights are instrumental for understanding the physiological and pathophysiological roles of vasopressin systems in various tissues.
Peptide Structure-Activity Relationship (SAR) Analysis: The modified peptide serves as a benchmark in structure-activity relationship studies aimed at correlating specific amino acid substitutions with changes in biological activity, stability, and receptor interaction. By systematically comparing analogs with native and engineered sequences, researchers can delineate the contributions of individual residues and backbone modifications to overall peptide function, informing the rational design of new bioactive peptides.
Neuroendocrine Function Investigation: With its tailored receptor activity, the analog is widely used in basic research to dissect the central and peripheral roles of vasopressin in neuroendocrine regulation. Experimental paradigms often include the study of hormone secretion, osmoregulation, and behavioral responses in in vitro and in vivo models. These investigations provide valuable insights into the physiological mechanisms governed by vasopressinergic signaling.
Peptide Stability and Degradation Studies: The presence of non-native linkages and methylated residues in this analog makes it a preferred model for evaluating peptide degradation pathways and metabolic resistance in biological matrices. By assessing its stability relative to unmodified peptides, scientists can better understand proteolytic processing, identify key enzymes involved in peptide turnover, and develop strategies to enhance the pharmacokinetic properties of peptide-based research tools.
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