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Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects.

Abstract：

:We have recently reported that the elaboration of the N-substituent in the δ opioid receptor (DOR) antagonist naltrindole (NTI) enabled the regulation of the DOR activities from full inverse agonists to weak partial agonists. The investigations of amide-type NTI derivatives revealed that N-phenylacetyl and N-dihydrocinnamoyl derivatives 3a and 3b were DOR full agonists. The same transformations were applied to a DOR agonist KNT-127 to provide the more potent DOR agonists 6a and 6b. Among the tested compounds, the most efficacious compound 6a showed dose-dependent antidepressant-like effects in the mouse forced swim test. The antidepressant-like effects by 6a seemed to be more potent than those of KNT-127, which is a more potent DOR agonist in in vitro assays. The amide-type compound like 6a may more fully penetrate into the central nervous system.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Fujii H,Uchida Y,Shibasaki M,Nishida M,Yoshioka T,Kobayashi R,Honjo A,Itoh K,Yamada D,Hirayama S,Saitoh A

doi

10.1016/j.bmcl.2020.127176

subject

Has Abstract

pub_date

2020-06-15 00:00:00

pages

127176

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(20)30273-0

journal_volume

30

pub_type

杂志文章

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