Design and Synthesis of Highly Specific and Selective Enkephalin Analog Containing S-Npys-Cysteine for δ Opioid Receptors

Autor:	Teruo Yasunaga, Yasuyuki Shimohigashi, Tommaso Costa, Rei Matsueda, Hiroaki Kodama, Michiko Kondo
Rok vydání:	1992
Předmět:	chemistry.chemical_classification Enkephalin Stereochemistry Biological activity General Chemistry chemistry Opioid Covalent bond Thiol medicine Receptor Selectivity Cysteine medicine.drug
Zdroj:	Chemistry Letters. 21:1259-1262
ISSN:	1348-0715 0366-7022
DOI:	10.1246/cl.1992.1259
Popis:	Enkephalin analogs containing S-(3-nitro-2-pyridinesulfenyl)cysteine at positions of 1,5, or 6 were synthesized for searching possible thiol groups in the opioid receptors. In the radio-ligand receptor assay and biological assays, [D-Ala2, Leu5]enkephalyl-Cys(Npys)6 exhibited a very high affinity and selectivity for δ over μ receptors, and its covalent attachment to δ receptors through the disulfide bonding was evidenced.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::9bd39ed1bc2ff1db3f4e41e942cd3360 https://doi.org/10.1246/cl.1992.1259 Zobrazit plný text záznamu