A novel super-potent neurokinin A receptor antagonist containing dehydroalanine(600 views) Lombardi A, D'Agostino B, Nastri F, D'Andrea LD, Filippelli A, Falciani M, Rossi F, Pavone V
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894xprint, 0960-894xlinking), 1998 May 19; 8(10): 1153-1156.
Keywords: Alanine, Analogs, Derivatives, Amino Acid Sequence, Animals, Models, Molecular, Molecular Structure, Peptides, Cyclic, Chemical Synthesis, Chemistry, Pharmacology, Protein Conformation, Rats, Receptors, Neurokinin-2, Antagonists, Inhibitors, Structure-Activity Relationship, Vas Deferens, Drug Effects, Physiology, Cyclopeptide, Dehydroalanine, Hexapeptide, Men 10627, Neurokinin 1 Receptor, Neurokinin 2 Receptor Antagonist, Neurokinin 3 Receptor, Animal Tissue, Article, Controlled Study, Drug Design, Drug Potency, Drug Selectivity, Drug Synthesis, Molecular Dynamics, Nonhuman, Nuclear Magnetic Resonance Spectroscopy, Structure Activity Relation,
Affiliations: Centro Interuniveristario di Ricerca su Peptidi Bioattivi, Universita di Napoli Federico II, Italy.,
Ctro. Interuniveristario di R., Ctro. di Stud. di Biocristallografia, Universite di Napoli Federico II, via Mezzocannone 4, 80134 Napoli, Italy
Ist. di Farmacologia e Tossicologia, Seconda Universitè di Napoli, via Costantinopoli 16, 80100 Napoli, Italy
References: Not available.
A novel super-potent neurokinin A receptor antagonist containing dehydroalanine
We report here the synthesis and preliminary pharmacological characterization of a novel Neurokinin A receptor antagonist. This molecule contains a dehydroalanine residue. It displays a high conformational rigidity and possesses very high activity. Its pharmacological properties as a neurokinin A receptor antagonist were assessed in in vitro experiments on rat vas deferens and were compared to those of Neuronorm and MEN10627.
A novel super-potent neurokinin A receptor antagonist containing dehydroalanine
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