Opioid receptor agonists in the rabbit colon: Comparison of in vivo and in vitro studies

Life Sciences ◽  
1984 ◽  
Vol 35 (16) ◽  
pp. 1653-1658 ◽  
Author(s):  
M. Pairet ◽  
Y. Ruckebusch
Keyword(s):  
Opioid Receptor ◽  
In Vitro Studies ◽  
Receptor Agonists ◽  
Rabbit Colon ◽  
Opioid Receptor Agonists

scholarly journals 6,5-Fused Ring, C2-Salvinorin Ester, Dual Kappa and Mu Opioid Receptor Agonists as Analgesics Devoid of Anxiogenic Effects

2021 ◽  
Author(s):  
Nicholas S. Akins ◽  
Nisha Mishra ◽  
Hannah M. Harris ◽  
Narendar Dudhipala ◽  
Seong Jong Kim ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Opioid Receptors ◽  
Analgesic Activity ◽  
Mu Opioid Receptor ◽  
Kappa Opioid Receptor ◽  
Mu Opioid ◽  
Receptor Agonists ◽  
Opioid Receptor Agonists

Analgesia is commonly mediated through the mu or kappa opioid receptor agonism. Unfortunately, selective mu or kappa receptor agonists often cause harmful side effects. Recently, ligands exhibiting dual agonism to the opioid receptors, such as to mu and kappa, or to mu and delta, have been suggested to temper undesirable adverse effects while retaining analgesic activity. Herein we report an introduction of various 6,5-fused rings to C2 of the salvinorin scaffold <i>via</i> an ester linker. <i>In vitro</i> studies showed that some of these compounds have dual agonism on kappa and mu opioid receptors, while some have triple agonism on kappa, mu, and delta. <i>In vivo </i>studies on the lead dual kappa and mu opioid receptor agonist, compound <b>10</b>, showed that it<b> </b>produced analgesic activity while avoiding anxiogenic effects in murine models, thus providing further strong evidence for the therapeutic advantages of dual opioid receptor agonists over selective opioid receptor agonists.

scholarly journals 6,5-Fused Ring, C2-Salvinorin Ester, Dual Kappa and Mu Opioid Receptor Agonists as Analgesics Devoid of Anxiogenic Effects

2021 ◽  
Author(s):  
Nicholas S. Akins ◽  
Nisha Mishra ◽  
Hannah M. Harris ◽  
Narendar Dudhipala ◽  
Seong Jong Kim ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Opioid Receptors ◽  
Analgesic Activity ◽  
Mu Opioid Receptor ◽  
Kappa Opioid Receptor ◽  
Mu Opioid ◽  
Receptor Agonists ◽  
Opioid Receptor Agonists

Analgesia is commonly mediated through the mu or kappa opioid receptor agonism. Unfortunately, selective mu or kappa receptor agonists often cause harmful side effects. Recently, ligands exhibiting dual agonism to the opioid receptors, such as to mu and kappa, or to mu and delta, have been suggested to temper undesirable adverse effects while retaining analgesic activity. Herein we report an introduction of various 6,5-fused rings to C2 of the salvinorin scaffold <i>via</i> an ester linker. <i>In vitro</i> studies showed that some of these compounds have dual agonism on kappa and mu opioid receptors, while some have triple agonism on kappa, mu, and delta. <i>In vivo </i>studies on the lead dual kappa and mu opioid receptor agonist, compound <b>10</b>, showed that it<b> </b>produced analgesic activity while avoiding anxiogenic effects in murine models, thus providing further strong evidence for the therapeutic advantages of dual opioid receptor agonists over selective opioid receptor agonists.

Chemical Characterization and in vitro Metabolism of a Novel Class of Delta Opioid Receptor Agonists, Analogs of SNC-80

2019 ◽  
Vol 4 (7) ◽  
pp. 2109-2115
Author(s):  
Elisabetta Maria Usai ◽  
Ilaria Manca ◽  
Francesca Pettinau ◽  
Antonio Mastino ◽  
Barbara Pittau
Keyword(s):  
Opioid Receptor ◽  
Chemical Characterization ◽  
In Vitro Metabolism ◽  
Delta Opioid Receptor ◽  
Receptor Agonists ◽  
Opioid Receptor Agonists

Comparative analysis of infarct-limiting activity of δ-opioid receptor agonists in heart reperfusion in vivo

2020 ◽  
Vol 170 (11) ◽  
pp. 559-562
Author(s):  
A. V. Mukhomedzyanov ◽  
◽  
S. Yu. Tsibulnikov ◽  
A. V. Krylatov ◽  
L. N. Maslov ◽  
...  
Keyword(s):  
Comparative Analysis ◽  
Opioid Receptor ◽  
Receptor Agonists ◽  
Δ Opioid Receptor ◽  
Opioid Receptor Agonists
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