The cannabinoid agonist CB-13 produces peripherally mediated analgesia in mice but elicits tolerance and signs of CNS activity with repeated dosing

Pain ◽  
2021 ◽  
Vol Publish Ahead of Print ◽  
Author(s):  
Richard A. Slivicki ◽  
Jiwon Yi ◽  
Victoria E. Brings ◽  
Phuong Nhu Huynh ◽  
Robert W. Gereau
Keyword(s):  
Cns Activity ◽  
Repeated Dosing ◽  
Cannabinoid Agonist

Fluorinated analogues of tricyclic neuroleptics: 6,9-difluoro derivative of 10-(4-methylpiperazino)-10,11-dihydrodibenzo[b,f]thiepin

1980 ◽  
Vol 45 (10) ◽  
pp. 2688-2694 ◽  
Author(s):  
Irena Červená ◽  
Marta Hrubantová ◽  
Emil Svátek ◽  
Jiří Holubek ◽  
Miroslav Ryska ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Title Compound ◽  
Substitution Reaction ◽  
Polyphosphoric Acid ◽  
Satisfactory Yield ◽  
Chloro Derivative ◽  
Cns Activity

The acid VI, obtained from 2,5-difluorothiophenol (IV) and (2-iodophenyl)acetic acid, afforded by cyclization with polyphosphoric acid 6,9-difluorodibenzo[b,f]thiepin-10(11H)-one (VII) in a satisfactory yield. Two further steps led to the chloro derivative X giving by a substitution reaction with 1-methylpiperazine the title compound III. This substance exhibits some 10% incoordinating activity of the unsubstituted compound I and an indication of cataleptic activity, in contrast to the inactive analogous dichloro compound II. The bulky atom of chlorine in the vicinity of the methylpiperazine residue interferes evidently with the CNS activity; the influence of the atom of fluorine is much less pronounced in this line.

The Additive Antinociceptive Interaction Between WIN 55,212-2, a Cannabinoid Agonist, and Ketorolac

2006 ◽  
Vol 102 (2) ◽  
pp. 443-447 ◽  
Author(s):  
Ahmet Ulug??l ◽  
Filiz ??zyigit ◽  
??zg??r Ye??ilyurt ◽  
Ahmet Dogrul
Keyword(s):  
Cannabinoid Agonist

scholarly journals Peripheral and central sites of action for the non-selective cannabinoid agonist WIN 55,212-2 in a rat model of post-operative pain

2009 ◽  
Vol 157 (4) ◽  
pp. 645-655 ◽  
Author(s):  
CZ Zhu ◽  
JP Mikusa ◽  
Y Fan ◽  
PR Hollingsworth ◽  
M Pai ◽  
...  
Keyword(s):  
Rat Model ◽  
Post Operative Pain ◽  
Sites Of Action ◽  
Cannabinoid Agonist

ChemInform Abstract: Synthesis and CNS-Activity of cis-Pyrano(2,3-b)(1,4)dioxane Derivatives.

ChemInform ◽  
1990 ◽  
Vol 21 (52) ◽  
Author(s):  
F. EIDEN ◽  
B. WUENSCH ◽  
J. SCHUENEMANN
Keyword(s):  
Cns Activity

Comprehensive Review on Hydrogels

2021 ◽  
Vol 18 ◽  
Author(s):  
Hitesh Chopra ◽  
Inderbir Singh ◽  
Sandeep Kumar ◽  
Tanima Bhattacharya ◽  
Md. Habibur Rahman ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Wound Healing ◽  
Controlled Release ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Bone Engineering ◽  
Comprehensive Review ◽  
Therapeutic Benefits ◽  
Conventional Drug ◽  
Repeated Dosing

: The conventional drug delivery systems have a long list of issues of repeated dosing and toxicity arising due to it. The hydrogels are the answer to them and offer a result that minimizes such activities and optimizes therapeutic benefits. The hydrogels proffer tunable properties that can withstand degradation, metabolism, and controlled release moieties. Some of the areas of applications of hydrogels involve wound healing, ocular systems, vaginal gels, scaffolds for tissue, bone engineering, etc. They consist of about 90% of the water that makes them suitable bio-mimic moiety. Here, we present a birds-eye view of various perspectives of hydrogels, along with their applications.

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