Detail of "19883-78-4"

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Synthesis and pharmacological activity of superagonists of the ORL1 receptor

Synthesis and pharmacological activity of superagonists of the ORL1 receptor. Salvadori, Severo; Guerrini, Remo; Tomatis, Roberto; Calo, Girolamo; Bigoni, Raffaella; Rizzi, Anna; Rizzi, Daniela; Regoli, Domenico ( Department of Pharmaceutical Sciences, University of Ferrara, Ferrara 44-100, Italy). Peptides: The Wave of the Future, Proceedings of the Second International and the Seventeenth American Peptide Symposium, San Diego, CA, United States, June 9-14, 2001, 787-788. Edited by: Lebl, Michal; Houghten, Richard A. American Peptide Society: San Diego, Calif. ISBN: 0-9715560-0-8(English) 2001.Some commonly used reagents like 19883-78-4 is used in this experiment. CODEN: 69DBAL. DOCUMENT TYPE: Conference CA Section: 1 (Pharmacology) The effect of substitutions with a halogen series of the Phe4 arom. side chain of the NC(1-13)-NH2 was examd. The new ligands, which behave as superagonists of the ORL1 receptor were identified. The peptides described were prepd. by solid-phase method on a PAL-PEG-PS-resin. All of the analogs are agonists in the mouse vas deferens assay, and their potencies depend on the type of halogen. The fluoro-analog was found to be 5-fold more potent than the ref. NC(1-13)-NH2, while other para halogenated Phe4 derivs. showed lower potencies (from 2- to 30-fold) than the ref. NC(1-13)-NH2. Analogs with fluorine in meta or ortho position, are less potent than [(pF)Phe4]NC(1-13)-NH2. The results clearly showed the importance of the Phe4 pharmacophore of NC, and led to the identification of superagonists of the ORL1 receptor. .