Recent advances in benzodiazepine receptor (BZR) binding studies

1995 ◽  
pp. 67-106 ◽  
Author(s):  
S. P. Gupta
Keyword(s):  
Benzodiazepine Receptor ◽  
Binding Studies ◽  
Recent Advances

scholarly journals Synthesis and Benzodiazepine Receptor Binding Studies of Pyridazino[3, 4-b]indoles

1992 ◽  
Vol 112 (11) ◽  
pp. 804-816 ◽  
Author(s):  
Yasuo SHIMOJI ◽  
Kuniyuki TOMITA ◽  
Toshio KARUBE ◽  
Toshiharu KAMIOKA
Keyword(s):  
Receptor Binding ◽  
Benzodiazepine Receptor ◽  
Binding Studies

Recent advances in affinity capillary electrophoresis for binding studies

Bioanalysis ◽  
2014 ◽  
Vol 6 (24) ◽  
pp. 3369-3392 ◽  
Author(s):  
Hassan M Albishri ◽  
Sami El Deeb ◽  
Noura AlGarabli ◽  
Raghda AlAstal ◽  
Hassan A Alhazmi ◽  
...  
Keyword(s):  
Capillary Electrophoresis ◽  
Binding Studies ◽  
Affinity Capillary Electrophoresis ◽  
Recent Advances

Ontogeny of the Benzodiazepine Receptor in Human Brain: Fluorographic, Immunochemical, and Reversible Binding Studies

1991 ◽  
Vol 57 (4) ◽  
pp. 1128-1135 ◽  
Author(s):  
Ralf Reichelt ◽  
Dietmar Hofmann ◽  
Hans-Jörg Födisch ◽  
Hanns Möhler ◽  
Michael Knapp ◽  
...  
Keyword(s):  
Human Brain ◽  
Benzodiazepine Receptor ◽  
Binding Studies ◽  
Reversible Binding

Recent advances in the synthesis of piperazine based ligands and metal complexes and their applications

2021 ◽  
Author(s):  
Rishi Kant ◽  
Suman Maji
Keyword(s):  
Metal Complexes ◽  
Metal Binding ◽  
Binding Studies ◽  
Piperazine Ring ◽  
Recent Advances ◽  
Ring Nitrogen

The piperazine ring is an indispensable part of many biomolecules and can be easily modified through substitution on the ring nitrogen for desired application in pharmacology as well as metal binding studies.

scholarly journals Pharmacology of W-18 and W-15

2016 ◽  
Author(s):  
Xi-Ping Huang ◽  
Tao Che ◽  
Thomas J Mangano ◽  
Valerie Le Rouzic ◽  
Ying-Xian Pan ◽  
...  
Keyword(s):  
Opioid Receptors ◽  
Drugs Of Abuse ◽  
Radioligand Binding ◽  
Benzodiazepine Receptor ◽  
Significant Activity ◽  
Binding Studies ◽  
Opioid Agonist ◽  
Opioid Activity ◽  
Cardiovascular Side Effects ◽  
Similarity Ensemble Approach

ABSTRACTW-18 (1-(4-Nitrophenylethyl)piperidylidene-2-(4-chlorophenyl)sulfonamide)and W-15 (4-chloro-N-[1-(2-phenylethyl)-2-piperidinylidene]-benzenesulfonamide) represent two emerging drugs of abuse chemically related to the potent opioid agonist fentanyl (N-(1-(2-phenylethyl)-4-piperidinyl)-N-phenylpropanamide). Here we describe the comprehensive pharmacological profiles of W-18 and W-15. Although W-18 and W-15 have been described as having potent anti-nociceptive activity and are presumed to interact with opioid receptors, we found them to be without detectible opioid activity at μ, δ, κ and nociception opioid receptors in a variety of assays. We also tested W-18 and W-15 for activity as allosteric modulators at opioid receptors and found them devoid of significant positive or negative allosteric modulatory activity. Comprehensive profiling at essentially all the druggable G-protein coupled receptors in the human genome using the PRESTO-Tango platform revealed no significant activity. In silico predictions using the Similarity Ensemble Approach suggested activity for W-18 only weakly at H3-histamine receptors, which was not confirmed in radioligand binding studies. Weak activity at the sigma receptors and the peripheral benzodiazepine receptor were found for W-18 (Ki=271 nM); W-15 displayed weak antagonist activity at 5-HT2-family serotonin receptors. W-18 is extensively metabolized, but its metabolites also lack opioid activity. W-18 and W-15 did inhibit hERG binding suggesting possible cardiovascular side-effects with high doses. Thus although W-18 and W-15 have been suggested to be potent opioid agonists, our results reveal no significant activity at these or other known targets for psychoactive drugs.

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