Probes for Narcotic Receptor-Mediated Phenomena. 27.1Synthesis and Pharmacological Evaluation of Selective δ-Opioid Receptor Agonists from 4-[(αR)-α-(2S,5R)-4-Substituted-2,5-dimethyl-1-piperazinyl-3-methoxybenzyl]-N,N-diethylbenzamides and Their Enantiomers

2000 ◽  
Vol 43 (16) ◽  
pp. 3193-3196 ◽  
Author(s):  
M. Scott Furness ◽  
Xiaoyan Zhang ◽  
Andrew Coop ◽  
Arthur E. Jacobson ◽  
Richard B. Rothman ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonists ◽  
Pharmacological Evaluation ◽  
Δ Opioid Receptor ◽  
Opioid Receptor Agonists

Selective δ opioid receptor agonists for inflammatory and neuropathic pain

Il Farmaco ◽  
2001 ◽  
Vol 56 (1-2) ◽  
pp. 117-119 ◽  
Author(s):  
Giulio Dondio ◽  
Silvano Ronzoni ◽  
Carlo Farina ◽  
Davide Graziani ◽  
Carlo Parini ◽  
...  
Keyword(s):  
Neuropathic Pain ◽  
Opioid Receptor ◽  
Receptor Agonists ◽  
Δ Opioid Receptor ◽  
Opioid Receptor Agonists

Homology modeling and 3D–QSAR study of benzhydrylpiperazine δ opioid receptor agonists

2019 ◽  
Vol 83 ◽  
pp. 107109 ◽  
Author(s):  
Chenling Pan ◽  
Hao Meng ◽  
Shuqun Zhang ◽  
Zhili Zuo ◽  
Yuehai Shen ◽  
...  
Keyword(s):  
Homology Modeling ◽  
Opioid Receptor ◽  
3D Qsar ◽  
Qsar Study ◽  
Receptor Agonists ◽  
Δ Opioid Receptor ◽  
Opioid Receptor Agonists

Differential Effects of μ-, δ-, and κ-Opioid Receptor Agonists on Mechanosensitive Gastric Vagal Afferent Fibers in the Rat

2000 ◽  
Vol 83 (4) ◽  
pp. 2209-2216 ◽  
Author(s):  
Noriyuki Ozaki ◽  
J. N. Sengupta ◽  
G. F. Gebhart
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonist ◽  
Dose Range ◽  
Receptor Agonists ◽  
Afferent Fibers ◽  
Opioid Receptor Agonist ◽  
Resting Activity ◽  
Vagal Afferent ◽  
Δ Opioid Receptor ◽  
Opioid Receptor Agonists

Single-fiber recordings were made from the decentralized right cervical vagus nerve (hyponodosal) of the rat. A total of 56 afferent fibers that responded to gastric distension (GD) were studied: 6 fibers were stimulated by phasic balloon GD, 50 by fluid GD. All fibers gave increasing responses to increasing pressures of GD (5–60 mmHg). The effects of μ-opioid (morphine), δ-opioid (SNC80), and κ-opioid (EMD61,753, U62,066) receptor agonists were tested on responses of afferent fibers to GD. Morphine, administered systemically over a broad dose range (10 μg to 31 mg/kg, cumulative), had no effect on either resting activity or responses of vagal afferent fibers to GD. Similarly, the δ-opioid receptor agonist SNC80 (0.05–3.2 mg/kg) did not affect resting activity or responses to GD. In contrast, cumulative intra-arterial doses of the κ-opioid receptor agonist EMD61,753 or U62,066 dose dependently attenuated afferent fiber responses to GD. Doses producing inhibition to 50% of the control response to GD of EMD61,753 (8.0 mg/kg) and U62,066 (8.8 mg/kg) did not differ. The effect of U62,066 was moderately attenuated by a nonselective dose (4 mg/kg) of naloxone hydrochloride; the κ-opioid receptor-selective antagonist nor-BNI (20 mg/kg) was ineffective. These results demonstrate that κ-, but not μ- or δ-opioid receptor agonists modulate visceral sensation conveyed by vagal afferent fibers innervating the stomach. Given that κ-opioid receptor agonists effects were only modestly antagonized by naloxone and not at all by nor-BNI, the results point to a novel site of action.

4-Piperidin-4-ylidenemethyl-benzamides as δ-opioid receptor agonists for CNS indications: Identifying clinical candidates

2012 ◽  
Vol 22 (2) ◽  
pp. 1174-1178 ◽  
Author(s):  
Cathy L. Dantzman ◽  
Megan M. King ◽  
Glen E. Ernst ◽  
Xia Wang ◽  
John P. McCauley ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonists ◽  
Δ Opioid Receptor ◽  
Opioid Receptor Agonists
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