Different Regulation of Human δ-Opioid Receptors by SNC-80 [(+)-4-[(αR)-α-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide] and Endogenous Enkephalins

2004 ◽  
Vol 310 (2) ◽  
pp. 666-677 ◽  
Author(s):  
I. Lecoq ◽  
N. Marie ◽  
Ph. Jauzac ◽  
S. Allouche
Keyword(s):  
Opioid Receptors ◽  
Endogenous Enkephalins

scholarly journals Analgesia linked to Nav1.7 loss of function requires μ and δ opioid receptors

2018 ◽  
Author(s):  
Vanessa Pereira ◽  
Queensta Millet ◽  
Jose Aramburu ◽  
Cristina Lopez-Rodriguez ◽  
Claire Gaveriaux Ruff ◽  
...  
Keyword(s):  
Opioid Receptors ◽  
Neurotransmitter Release ◽  
Null Mouse ◽  
Channel Blockers ◽  
Loss Of Function ◽  
Analgesic Drug ◽  
Gene Encoding ◽  
Binding Motifs ◽  
Opioid Receptor Antagonists ◽  
Endogenous Enkephalins

AbstractFunctional deletion of the SCN9A gene encoding sodium channel Nav1.7 makes humans and mice pain-free (1,2). Opioid signaling contributes to this analgesic state (3). Here we show that the pharmacological block or deletion of both μ and δ opioid receptors is required to abolish Nav1.7 null opioid-related analgesia.κ-opioid receptor antagonists were without effect. Enkephalins encoded by the Penk gene are upregulated in Nav1.7 nulls (3). Deleting Nfat5, a transcription factor with binding motifs upstream of Penk (4), induces the same level of enkephalin mRNA expression as found in Nav1.7 nulls, but without consequent analgesia. These data confirm that a combination of events linked to SCN9A gene loss is required for analgesia. Higher levels of endogenous enkephalins (3), potentiated opioid receptors (5), diminished electrical excitability (6,7) and loss of neurotransmitter release (2,1) together contribute to the analgesic phenotype found in Nav1.7 null mouse and human mutants. These observations help explain the failure of Nav1.7 channel blockers alone to produce analgesia and suggest new routes for analgesic drug development.

Involvement of δ-opioid receptors in the effects induced by endogenous enkephalins on learned helplessness model

1998 ◽  
Vol 354 (1) ◽  
pp. 1-7 ◽  
Author(s):  
Purificación Tejedor-Real ◽  
Juan A. Micó ◽  
Claire Smadja ◽  
Rafael Maldonado ◽  
Bernard P. Roques ◽  
...  
Keyword(s):  
Opioid Receptors ◽  
Learned Helplessness ◽  
Endogenous Enkephalins ◽  
Helplessness Model

In vivo occupation of mouse brain opioid receptors by endogenous enkephalins: blockade of enkephalin degrading enzymes by RB 101 inhibits [3H]diprenorphine binding

1992 ◽  
Vol 571 (2) ◽  
pp. 306-312 ◽  
Author(s):  
Mariano Ruiz-Gayo ◽  
Ana Baamonde ◽  
Serge Turcaud ◽  
Marie-Claude Fournie-Zaluski ◽  
Bernard P. Roques
Keyword(s):  
Mouse Brain ◽  
Opioid Receptors ◽  
Degrading Enzymes ◽  
Endogenous Enkephalins ◽  
Rb 101

Pain control by endogenous enkephalins is mediated by MU opioid receptors

Life Sciences ◽  
1983 ◽  
Vol 33 ◽  
pp. 685-688 ◽  
Author(s):  
P. Chaillet ◽  
A. Coulaud ◽  
M.C. Fournié-Zaluski ◽  
G. Gacel ◽  
B.P. Roques ◽  
...  
Keyword(s):  
Opioid Receptors ◽  
Pain Control ◽  
Mu Opioid Receptors ◽  
Mu Opioid ◽  
Endogenous Enkephalins

Three Technical Approaches for Cloning Opioid Receptors

1988 ◽  
Author(s):  
Curtis A. Machida ◽  
John Salon ◽  
David Grandy ◽  
James Bunzow ◽  
Paul Albert ◽  
...  
Keyword(s):  
Opioid Receptors
Sign in / Sign up

Export Citation Format

Share Document