▽ E Phe4‐enkephalin analogs Delta receptors in rat brain are different from those in mouse vas deferens

FEBS Letters

Pfeiffer, Andreas³  Herz, Albert³  Stammer, Charles H.²  Costa, Tommaso³  Shimohigashi, Yasuyuki¹  Kimura, Hitoshi² 

[1] Laboratory of Biochemistry, Faculty of Science, Kyushu University 33, Fukuoka 812, Japan;Department of Chemistry, School of Chemical Sciences, University of Georgia, Athens, GA 30602, USA;Laboratory of Neuropharmacology, Max Planck Institute for Psychiatry, D-8033 Martinsried FRG

关键词: Enkephalin analog;    Conformational restriction;    Opiate receptor;    Receptor heterogeneity;   

DOI  :  10.1016/0014-5793(87)80193-X

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Conformationally restricted enkephalin analogs containing E-cyclopropylphenylalanine (▽ ^E Phe), [D-Ala², (2R,3S)-▽ ^E Phe⁴,Leu⁵]enkephalin and its (2S,3R) isomer, were evaluated in receptor-binding assays using rat brain and in assays using muscle preparations. The (2S,3R) isomer was almost completely inactive in all assays. In contrast, the (2R,3S) isomer showed a very high affinity for the δ and a very weak affinity for the μ receptors in rat brain. The extent of δ affinity and the selectivity of this isomer were almost equal to those of [D-Pen²,D-Pen⁵]enkephalin. However, the (2R,3S) isomer was inactive in both the mouse vas deferens and guinea pig ileum assays, and showed no antagonistic activity in these tissues. These results indicate that the (2R,3S) isomer interacts with the δ receptors in rat brain, but not with those in the mouse vas deferens, and they suggest that the δ receptors in the central and peripheral nervous systems are different from each other.

【 授权许可】

Unknown