Agonist, Antagonist, and Inverse Agonist Characteristics of TIPP (H-Tyr-Tic-Phe-Phe-OH), a Selective δ-Opioid Receptor Ligand

2002 ◽  
Vol 301 (2) ◽  
pp. 661-671 ◽  
Author(s):  
Nancy A. Martin ◽  
Michael B. Ruckle ◽  
Stephanie L. VanHoof ◽  
Paul L. Prather
Keyword(s):  
Opioid Receptor ◽  
Inverse Agonist ◽  
Receptor Ligand ◽  
Δ Opioid Receptor

scholarly journals Effects of N-Substituents on the Functional Activities of Naltrindole Derivatives for the δ Opioid Receptor: Synthesis and Evaluation of Sulfonamide Derivatives

Molecules ◽  
2020 ◽  
Vol 25 (17) ◽  
pp. 3792
Author(s):  
Chiharu Iwamatsu ◽  
Daichi Hayakawa ◽  
Tomomi Kono ◽  
Ayaka Honjo ◽  
Saki Ishizaki ◽  
...  
Keyword(s):  
Molecular Mechanism ◽  
Opioid Receptor ◽  
Inverse Agonist ◽  
Side Chain ◽  
Agonist Activity ◽  
Inverse Agonists ◽  
Functional Activities ◽  
Δ Opioid Receptor

We have recently reported that N-alkyl and N-acyl naltrindole (NTI) derivatives showed activities for the δ opioid receptor (DOR) ranging widely from full inverse agonists to full agonists. We newly designed sulfonamide-type NTI derivatives in order to investigate the effects of the N-substituent on the functional activities because the side chain and S=O part in the sulfonamide moiety located in spatially different positions compared with those in the alkylamine and amide moieties. Among the tested compounds, cyclopropylsulfonamide 9f (SYK-839) was the most potent full inverse agonist for the DOR, whereas phenethylsulfonamide 9e (SYK-901) showed full DOR agonist activity with moderate potency. These NTI derivatives are expected to be useful compounds for investigation of the molecular mechanism inducing these functional activities.

(2S,3R)TMT-l-Tic-OH is a potent inverse agonist at the human δ-opioid receptor

1999 ◽  
Vol 380 (1) ◽  
pp. R9-R10 ◽  
Author(s):  
Keiko Hosohata ◽  
Thomas H Burkey ◽  
Josua Alfaro-Lopez ◽  
Victor J Hruby ◽  
William R Roeske ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Inverse Agonist ◽  
Δ Opioid Receptor

scholarly journals In vitro and in vivo characterization of the bifunctional μ and δ opioid receptor ligand UFP‐505

2018 ◽  
Vol 175 (14) ◽  
pp. 2881-2896 ◽  
Author(s):  
N Dietis ◽  
H Niwa ◽  
R Tose ◽  
J McDonald ◽  
V Ruggieri ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Ligand ◽  
Δ Opioid Receptor ◽  
In Vivo Characterization

scholarly journals δ-opioid receptor inverse agonist SYK-623 reversed chronic stress-induced leaning impairment in mice

2019 ◽  
Vol 92 (0) ◽  
pp. 1-P-030
Author(s):  
Rei Mishima ◽  
Takashi Iwai ◽  
Shigeto Hirayama ◽  
Misa Oyama ◽  
Shun Watanabe ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Chronic Stress ◽  
Inverse Agonist ◽  
Δ Opioid Receptor ◽  
Receptor Inverse Agonist

Development of a lanthanide-based assay for detection of receptor–ligand interactions at the δ-opioid receptor

2005 ◽  
Vol 343 (2) ◽  
pp. 299-307 ◽  
Author(s):  
Heather L. Handl ◽  
Josef Vagner ◽  
Henry I. Yamamura ◽  
Victor J. Hruby ◽  
Robert J. Gillies
Keyword(s):  
Opioid Receptor ◽  
Receptor Ligand ◽  
Ligand Interactions ◽  
Δ Opioid Receptor

A peripheral antinociceptive effects of a bifunctional μ and δ opioid receptor ligand in rat model of inflammatory bladder pain

2021 ◽  
pp. 108701
Author(s):  
Maia Terashvili ◽  
Bhavana Talluri ◽  
Watchareepohn Palangmonthip ◽  
Kenneth A. Iczkowski ◽  
Patrick Sanvanson ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Rat Model ◽  
Receptor Ligand ◽  
Bladder Pain ◽  
Antinociceptive Effects ◽  
Δ Opioid Receptor

scholarly journals δ-opioid receptor inverse agonist SYK-623 improved stress-induced learning dysfunction in mice

2018 ◽  
Vol WCP2018 (0) ◽  
pp. PO1-1-20
Author(s):  
Takashi Iwai ◽  
Toya Okonogi ◽  
Rei Mishima ◽  
Kayoko Yoshida ◽  
Misa Oyama ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Inverse Agonist ◽  
Learning Dysfunction ◽  
Δ Opioid Receptor ◽  
Receptor Inverse Agonist
Sign in / Sign up

Export Citation Format

Share Document