scholarly journals Structure–Activity Relationships of Peptides Incorporating a Bioactive Reverse-Turn Heterocycle at the Melanocortin Receptors: Identification of a 5800-fold Mouse Melanocortin-3 Receptor (mMC3R) Selective Antagonist/Partial Agonist versus the Mouse Melanocortin-4 Receptor (mMC4R)

2013 ◽  
Vol 56 (7) ◽  
pp. 2747-2763 ◽  
Author(s):  
Anamika Singh ◽  
Marvin Dirain ◽  
Rachel Witek ◽  
James R. Rocca ◽  
Arthur S. Edison ◽  
...  
Keyword(s):  
Partial Agonist ◽  
Melanocortin Receptors ◽  
Selective Antagonist ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Melanocortin 4 Receptor ◽  
Reverse Turn

Structure–activity relationships of bisphenol A analogs at estrogen receptors (ERs): Discovery of an ERα-selective antagonist

2013 ◽  
Vol 23 (14) ◽  
pp. 4031-4036 ◽  
Author(s):  
Keisuke Maruyama ◽  
Masaharu Nakamura ◽  
Shusuke Tomoshige ◽  
Kazuyuki Sugita ◽  
Makoto Makishima ◽  
...  
Keyword(s):  
Bisphenol A ◽  
Estrogen Receptors ◽  
Selective Antagonist ◽  
Structure Activity Relationships ◽  
Structure Activity

scholarly journals The Discovery of Novel Selective D1 Dopaminergic Agonists: A-68930, A-77636, A-86929, and ABT-413

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Yvonne Connolly Martin
Keyword(s):  
Medicinal Chemistry ◽  
Partial Agonist ◽  
Skf 38393 ◽  
The Novel ◽  
Bioactive Conformation ◽  
Dopaminergic Agonists ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
A 68930

The novel selective D1 dopaminergic full agonists A-68930, A-77636 were discovered by the synthesis of molecules to probe the bioactive conformation of the partial agonist SKF-38393, by the use of this information to add D1 affinity and selectivity to a screening hit, and by traditional medicinal chemistry exploration of structure-activity relationships. The subsequent design of A-86929 and ABT-413 capitalized on these results, recently disclosed agonists, and traditional medicinal chemistry.

Structure—Activity Relationships of 2-(Benzothiazolylthio)acetamide Class of CCR3 Selective Antagonist.

ChemInform ◽  
2003 ◽  
Vol 34 (45) ◽  
Author(s):  
Akira Naya ◽  
Kensuke Kobayashi ◽  
Makoto Ishikawa ◽  
Kenji Ohwaki ◽  
Toshihiko Saeki ◽  
...  
Keyword(s):  
Selective Antagonist ◽  
Structure Activity Relationships ◽  
Structure Activity

Nociceptin /Orphanin FQ Peptide (NOP) Receptor Modulators: An Update in Structure-Activity Relationships

2018 ◽  
Vol 25 (20) ◽  
pp. 2353-2384 ◽  
Author(s):  
Carlo Mustazza ◽  
Stefano Pieretti ◽  
Francesca Marzoli
Keyword(s):  
Partial Agonist ◽  
Orphanin Fq ◽  
Structure Activity Relationships ◽  
Airway Constriction ◽  
Structure Activity ◽  
Antinociceptive Effects ◽  
Μ Opioid Receptor ◽  
Receptor Modulators ◽  
G Protein Coupled ◽  
Higher Doses

Nociceptin /Orphanin FQ Peptide” receptor (NOPr) is a G-protein-coupled receptor with the nociceptin/orphanin FQ peptide (N/OFQ) as endogenous agonist. It is expressed in the nervous system as well as in some non-neural tissues. Its activation has pronociceptive effect at the supraspinal level, whereas at the spinal level it produces nociceptive effects at low doses and antinociceptive effects at higher doses. NOPr is also involved in mood and blood pressure regulation, immunoregulation, airway constriction, feeding, urination, bowel motility, learning and memory. Selective NOPr agonists have been tested clinically as anxiolytics and antitussives, and the antagonists as analgesics, antidepressants and in the treatment of alcohol addiction. Two NOPr radioligands have also been tested in humans as neuroimaging agents. Furthermore, the partial agonist peptide SER100 and N/OFQ have been used in clinical trials, respectively for congestive heart failure and overactive bladder. The evidence of interactions between NOP and μ-opioid receptor (MOPr) receptors has been exploited in the use of mixed NOPr/MOPr modulators as analgesics and in the treatment of drug addiction. These drugs are devoid of typical opioid liabilities. In this review, we outline the latest advances in the structure-activity relationships (SAR) of NOPr agonists and antagonists, with emphasis on affinity, activity, selectivity and pharmacokinetic features.

scholarly journals Structure–Activity Relationships of 2-(Benzothiazolylthio)acetamide Class of CCR3 Selective Antagonist

2003 ◽  
Vol 51 (6) ◽  
pp. 697-701 ◽  
Author(s):  
Akira Naya ◽  
Kensuke Kobayashi ◽  
Makoto Ishikawa ◽  
Kenji Ohwaki ◽  
Toshihiko Saeki ◽  
...  
Keyword(s):  
Selective Antagonist ◽  
Structure Activity Relationships ◽  
Structure Activity

Structure–activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor

2004 ◽  
Vol 14 (17) ◽  
pp. 4417-4423 ◽  
Author(s):  
Joseph Pontillo ◽  
Joseph A. Tran ◽  
Melissa Arellano ◽  
Beth A. Fleck ◽  
Rajesh Huntley ◽  
...  
Keyword(s):  
Structure Activity Relationships ◽  
Structure Activity ◽  
Melanocortin 4 Receptor ◽  
Selective Agonists
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