Antagonist G TFA

Antagonist G TFA is a potent antagonist of vasopressin, with additional, weaker antagonistic effects on GRP and Bradykinin. This compound also promotes AP-1 transcription and enhances cellular sensitivity to chemotherapy [1] [2].

G-Protein antagonist peptide acetate is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide acetate inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis

Antagonist G is an anticancer peptide and is also a broad spectrum neuropeptide growth factor antagonist.

Substance P-related peptide that inhibits binding of G proteins to their receptors. Competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.

Ac-RYYRIK-NH2 TFA acts as both a potent partial agonist for ORL1 when transfected in CHO cells (K d = 1.5 nM) and an endogenous ligand of ORL1. Moreover, it serves as a specific antagonist that inhibits G protein activation and competitively blocks the stimulation of [35S]-GTPγS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in rat brain membranes and sections [1].