Analgesic activity and selectivity of isothiocyanate derivatives of fentanyl analogs for opioid receptors

Life Sciences ◽  
1999 ◽  
Vol 65 (15) ◽  
pp. 1589-1595 ◽  
Author(s):  
Chen Bi-Yi ◽  
Jin Wen-Qiao ◽  
Chen Jie ◽  
Chen Xin-Jian ◽  
Zhu You-Cheng ◽  
...  
Keyword(s):  
Opioid Receptors ◽  
Analgesic Activity ◽  
Fentanyl Analogs ◽  
Derivatives Of

Synthesis and Analgesic Activity of 3,7-dimethylpurine-2,6-dion-1-yl Derivatives of Acetic and Butanoic Acid

2014 ◽  
Vol 11 (10) ◽  
pp. 1204-1213 ◽  
Author(s):  
Mal.gorzata Zygmunt ◽  
Pawe.l Zmudzki ◽  
Graz.yna Chl.on.-Rzepa ◽  
Jacek Sapa ◽  
Maciej Pawl.owski
Keyword(s):  
Analgesic Activity ◽  
Butanoic Acid ◽  
Derivatives Of

Copper Complexes Have Potent Analgesic Activity and They May Activate Opioid Receptors

1987 ◽  
pp. 301-313 ◽  
Author(s):  
Shigeru Okuyama ◽  
Sanae Hashimoto ◽  
Hironaka Aihara ◽  
William M. Willingham ◽  
John R. J. Sorenson
Keyword(s):  
Opioid Receptors ◽  
Analgesic Activity ◽  
Copper Complexes

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 Evaluation of Analgesic Activity ofPapaver libanoticumExtract in Mice: Involvement of Opioids Receptors

2017 ◽  
Vol 2017 ◽  
pp. 1-13 ◽  
Author(s):  
Mohamad Ali Hijazi ◽  
Ahmed El-Mallah ◽  
Maha Aboul-Ela ◽  
Abdalla Ellakany
Keyword(s):  
Opioid Receptors ◽  
Analgesic Activity ◽  
Time Course ◽  
Ethanolic Extract ◽  
Maximum Activity ◽  
Tail Flick ◽  
Endemic Plant ◽  
Hot Plate ◽  
The Central Nervous System ◽  
Opioid Withdrawal Syndrome

Papaver libanoticumis an endemic plant to Lebanese region (family Papaveraceae) that has not been investigated before. The present study aimed to explore the analgesic activity of dried ethanolic extract ofPapaver libanoticum(PLE) using tail flick, hot plate, and acetic acid induced writhing models in mice. The involvement of opioid receptors in the analgesic mechanism was investigated using naloxone antagonism. Results demonstrated that PLE exhibited a potent dose dependent analgesic activity in all tested models for analgesia. The analgesic effect involved activation of opioid receptors in the central nervous system, where both spinal and supraspinal components might be involved. The time course for analgesia revealed maximum activity after three hours in both tail flick and hot plate methods, which was prolonged to 24 hours. Metabolites of PLE could be responsible for activation of opioid receptors. The EC50 of PLE was 79 and 50 mg/kg in tail flick and hot plate tests, respectively. The total coverage of analgesia by PLE was double that of morphine in both tests. In conclusion, PLE proved to have opioid agonistic activity with a novel feature of slow and prolonged effect. The present study could add a potential tool in the armaments of opioid drugs as a natural potent analgesic and for treatment of opioid withdrawal syndrome.

Synthesis and evaluation of derivatives of leucine enkephalin as potential affinity labels for δ opioid receptors

Biopolymers ◽  
2003 ◽  
Vol 71 (5) ◽  
pp. 552-557 ◽  
Author(s):  
Heekyung Choi ◽  
Thomas F. Murray ◽  
Jane V. Aldrich
Keyword(s):  
Opioid Receptors ◽  
Affinity Labels ◽  
Leucine Enkephalin ◽  
Derivatives Of

ChemInform Abstract: Synthesis and Analgesic Activity of Nitrogen-Heterocyclic Derivatives of Embelin.

ChemInform ◽  
1990 ◽  
Vol 21 (4) ◽  
Author(s):  
S. M. JAIN ◽  
R. KANT ◽  
A. N. SARIN ◽  
S. K. DHAR ◽  
K. L. DHAR
Keyword(s):  
Analgesic Activity ◽  
Heterocyclic Derivatives ◽  
Derivatives Of ◽  
Nitrogen Heterocyclic

Evidence against the Participation of μ- and κ-Opioid Receptors in the Analgesic Activity of Ketorolac in Rats

1995 ◽  
Vol 47 (6) ◽  
pp. 514-517 ◽  
Author(s):  
VINICIO GRANADOS-SOTO ◽  
FRANCISCO J. FLORES-MURRIETA ◽  
GILBERTO CASTAÑEDA-HERNÁNDEZ ◽  
ENRIQUE HONG ◽  
FRANCISCO J. LÓPEZ-MUÑOZ
Keyword(s):  
Opioid Receptors ◽  
Analgesic Activity

scholarly journals Syntheses of N-Acyl Derivatives of α-Methyl-3, 4-methylenedioxyphenethylamine and their Analgesic Activity.

1963 ◽  
Vol 11 (5) ◽  
pp. 654-657 ◽  
Author(s):  
Keijiro Takagi ◽  
Yutaka Kasuya ◽  
Kyo Fujie ◽  
Minoru Watanabe ◽  
Setsuko Kayaoka
Keyword(s):  
Analgesic Activity ◽  
Derivatives Of ◽  
Acyl Derivatives

Synthesis and Analgesic Activity of Some Deaza Derivatives of Anpirtoline

1999 ◽  
Vol 332 (1) ◽  
pp. 13-18 ◽  
Author(s):  
Stanislav Rádl ◽  
Petr Hezky ◽  
Jan Proška ◽  
Ivan Krejcí
Keyword(s):  
Analgesic Activity ◽  
Derivatives Of

Potential Irreversible Ligands for Opioid Receptors. Cinnamoyl Derivatives of β-Naltrexamine

1996 ◽  
Vol 48 (2) ◽  
pp. 192-196 ◽  
Author(s):  
IAN DERRICK ◽  
JOHN W. LEWIS ◽  
HUMPHREY A. MOYNIHAN ◽  
JILLIAN BROADBEAR ◽  
JAMES H. WOODS
Keyword(s):  
Opioid Receptors ◽  
Derivatives Of
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