Synthesis and analgesic effects of novel β2-tryptophan hexapeptide analogs

International audienceAiming to develop more potent analgesic substances a new series of hexapeptides containing b2-tryptophan analogues was synthesized. The Trp in position 4 and 5, respectively in Ac-Arg-Phe-Met-Trp-Met-Lys-NH2 (opioid receptor antagonist) and Ac-Arg-Tyr-Tyr-Arg-Trp-Lys- NH2 (highly potent and selective NOP-receptor agonist) was substituted by the (S)-2-(1-methyl-1H-indol-3-yl)propionic residue or the (S)-2-(5-methoxy-1H-indol-3-yl)propionic residue. The analgesic effect of the four newly synthesized compounds has been evaluated in male Wistar rats by PPand HP tests and compared to the native templates. Further estimation of the mechanisms of action of each compound was achieved using specific antagonists--naloxone for opioid and JTC801 for the NOP receptor. Replacement of Trp with b2-tryptophan analogues in 4th position (Ac-Arg-Phe-Met-Trp-Met-Lys-NH2) led to increased and longer lasting analgesic effect. The results obtained permit us to assume that both opioid and NOP receptors take part in the newly synthesized compounds analgesic effects

Diversification of Banking Activity and Its Importance in Building Financial Stability

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The Moderator Effect of Communication in Marketing Channels of Distribution; The Case of Car’s Industry in Canada

Communication, Dependence, Power, Cooperation, Conflict, Satisfaction, LatentVariables, Indicators, Partial Least Squares, Communication, D21, M00, O50, R10,