scholarly journals Semisynthesis and Kappa-Opioid Receptor Activity of Derivatives of Columbin, a Furanolactone Diterpene

2017 ◽  
Vol 80 (7) ◽  
pp. 2094-2100 ◽  
Author(s):  
Anil Yilmaz ◽  
Rachel Saylor Crowley ◽  
Alexander M. Sherwood ◽  
Thomas E. Prisinzano
Keyword(s):  
Opioid Receptor ◽  
Kappa Opioid Receptor ◽  
Receptor Activity ◽  
Kappa Opioid ◽  
Derivatives Of

Kappa-Opioid Receptor-Mediated Antinociceptive Effects of Stereoisomers and Derivatives of (+)-Matrine in Mice

Planta Medica ◽  
1999 ◽  
Vol 65 (3) ◽  
pp. 230-233 ◽  
Author(s):  
Ping Xiao ◽  
Hajime Kubo ◽  
Masahiro Ohsawa ◽  
Kimio Higashiyama ◽  
Hiroshi Nagase ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Antinociceptive Effects ◽  
Derivatives Of

Kappa opioid receptor activity modulates memory for peck-avoidance training in the 2-day-old chick

1992 ◽  
Vol 108 (1-2) ◽  
pp. 235-240 ◽  
Author(s):  
Paul J. Colombo ◽  
Joe L. Martinez ◽  
Edward L. Bennett ◽  
Mark R. Rosenzweig
Keyword(s):  
Opioid Receptor ◽  
Avoidance Training ◽  
Kappa Opioid Receptor ◽  
Receptor Activity ◽  
Kappa Opioid

scholarly journals Dynorphin-kappa opioid receptor activity in the central amygdala modulates binge-like alcohol drinking in mice

2018 ◽  
Vol 44 (6) ◽  
pp. 1084-1092 ◽  
Author(s):  
Rachel I. Anderson ◽  
Marcelo F. Lopez ◽  
William C. Griffin ◽  
Harold L. Haun ◽  
Daniel W. Bloodgood ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Alcohol Drinking ◽  
Kappa Opioid Receptor ◽  
Receptor Activity ◽  
Central Amygdala ◽  
Kappa Opioid

EXPERIMENTAL EVALUATION OF TOXICOMETRIC INDICATORS AND ANALGESIC ACTIVITY OF KAPPA-OPIOID RECEPTOR AGONISTS

2020 ◽  
pp. 27-33
Author(s):  
S. V. Chepur ◽  
S. E. Galan ◽  
M. S. Vakhviayanen ◽  
R. N. Khromov ◽  
A. N. Semenov
Keyword(s):  
Opioid Receptor ◽  
Analgesic Activity ◽  
Phenyl Ring ◽  
Carbon Chain ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Receptor Agonists ◽  
Piperazine Derivatives ◽  
Opioid Receptor Agonists ◽  
Derivatives Of

Data on the biological activity of kappa-opioid receptor agonists - derivatives of three groups of compounds: 1,2-cyclohexylamine, 1,2,3,4-piperidine, 1,2,4-piperazine are presented. On the examples of 1,2-cyclohexylamine and 1,2,4-piperazine derivatives, it has been shown that a decrease in the length of the carbon chain in the phenylalkyl substituent at the nitrogen atom is accompanied by a decrease in the analgesic activity and toxicity of compounds. The replacement of chlorine atoms in the 3 and 4 positions of the phenyl ring with fluorine atoms, which are more electronegative, leads to an increase in the analgesic effect and a decrease in the toxicity of the compounds.

Dynorphin/Kappa Opioid Receptor Activity Within the Extended Amygdala Contributes to Stress-Enhanced Alcohol Drinking in Mice

2022 ◽  
Author(s):  
Harold L. Haun ◽  
Christina L. Lebonville ◽  
Matthew G. Solomon ◽  
William C. Griffin ◽  
Marcelo F. Lopez ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Alcohol Drinking ◽  
Kappa Opioid Receptor ◽  
Receptor Activity ◽  
Kappa Opioid ◽  
Extended Amygdala

Molecular recognition at kappa opioid receptors

2001 ◽  
Vol 73 (9) ◽  
pp. 1387-1391 ◽  
Author(s):  
Philip S. Portoghese
Keyword(s):  
Molecular Recognition ◽  
Opioid Receptor ◽  
Kappa Opioid Receptor ◽  
Site Directed Mutagenesis ◽  
Directed Mutagenesis ◽  
Kappa Opioid ◽  
Molecular Modification ◽  
Opioid Receptor Antagonists ◽  
Membrane Bound ◽  
Derivatives Of

Structure­activity relationships are rarely straightforward, and often are more complicated than they appear. For this reason, the use of site-directed mutagenesis as a complementary tool to analyze structure­activity relationships has been invaluable. Here, we illustrate how site-directed mutagenesis has led to greater insight into the molecular basis for molecular recognition of norbinaltorphimine and to the design of novel kappa antagonists. Given the paucity of high-resolution crystal structures for membrane-bound receptors, the use of a coordinated "two-dimensional" paradigm that involves molecular modification of both the ligand and the receptor, affords a useful approach to the study of molecular recognition. This paradigm has led to the design of highly potent and selective kappa opioid receptor antagonists that are derivatives of the delta opioid receptor antagonist, naltrindole.

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