Evolution of the Dmt-Tic Pharmacophore:  N-Terminal Methylated Derivatives with Extraordinary δ Opioid Antagonist Activity

Author:

Salvadori Severo1,Balboni Gianfranco1,Guerrini Remo1,Tomatis Roberto1,Bianchi Clementina1,Bryant Sharon D.1,Cooper Peter S.1,Lazarus Lawrence H.1

Affiliation:

1. Department of Pharmaceutical Science and Biotechnology Center, University of Ferrara, Ferrara 44100, Italy, Institute of Pharmacology, University of Ferrara, Ferrara 44100, Italy, and Peptide Neurochemistry, LCBRA, National Institute of Environmental Health Sciences, Research Triangle Park, North Carolina 27709

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference95 articles.

1. Symbols and abbreviations used in this paper follows the IUPAC−IUB Commission on Biochemical Nomenclature (J. Biol. Chem.1985,260, 1442). Boc,tert-butyloxycarbonyl; DAGO, [d-Ala2,N-Me-Phe4,Gly-ol5]enkephalin; deltorphin C, [d-Ala2]deltorphin I (H-Tyr-d-Ala-Phe-Asp-Val-Val-Gly-NH2); DMSO, dimethyl sulfoxide; Dmt, 2‘,6‘-dimethyl-l-tyrosine; DPDPE, [d-Pen2,5]enkephalin; Et2O, diethyl ether; EtOAc, ethyl acetate; GPI, guinea pig ileum; HOBt, 1-hydroxybenzotriazole; HPLC, high performance liquid chromatography;Ke, the antilog of pA2in molar concentration; Me, methyl group; MeOH, methanol; MVD, mouse vas deferens; pA2, the negative log of the molar concentration necessary to double the concentration of agonist needed to elicit the original response;tBu,tert-butyl; TEA, triethylamine; TFA, trifluoroacetic acid; Tic, 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; TLC, thin-layer chromatography; WSC, 1-ethyl-3-(3‘-(dimethyl)aminopropyl)carbodiimide hydrochloride; Z, benzyloxycarbonyl.

2. The opioid peptides of the amphibian skin

3. The toad, ugly and venomous, wears yet a precious jewel in his skin

4. Opioid receptor selectivity reversal in deltorphin tetrapeptide analogues

5. The aspartic acid in deltorphin I and dermenkephalin promotes targeting to δ-opioid receptor independently of receptor binding

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