Warning: Undefined array key "mm" in /www/wwwroot/www.ai-bt.com/si.php on line 10 Deprecated: trim(): Passing null to parameter #1 ($string) of type string is deprecated in /www/wwwroot/www.ai-bt.com/si.php on line 10 Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor.

Literature DB >> 11504634

Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor.

H Juteau¹, Y Gareau, M Labelle, C F Sturino, N Sawyer, N Tremblay, S Lamontagne, M C Carrière, D Denis, K M Metters.

Abstract

Potent and selective antagonists of the human EP3 receptor have been identified. The structure-activity relationship of the chemical series was conducted and we found several analogues displaying sub-nanomolar K(i) values at the EP3 receptor and micromolar activities at the EP1, EP2 and EP4 receptors. The effect of added human serum albumin (HSA) on the binding affinity at the EP3 receptor was also investigated.

Entities: Chemical Gene Species

Mesh：

Substances：

Year: 2001 PMID： 11504634 DOI： 10.1016/s0968-0896(01)00110-9

Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641

Keyword Cloud
Cited

26 in total

1. The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

Authors: Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal: Br J Pharmacol Date: 2013-12 Impact factor: 8.739

2. Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists.

Authors: Jian Jin; Angel Morales-Ramos; Patrick Eidam; John Mecom; Yue Li; Carl Brooks; Mark Hilfiker; David Zhang; Ning Wang; Dongchuan Shi; Pei-San Tseng; Karen Wheless; Brian Budzik; Karen Evans; Jon-Paul Jaworski; Jack Jugus; Lisa Leon; Charlene Wu; Mark Pullen; Bhumika Karamshi; Parvathi Rao; Emma Ward; Nicholas Laping; Christopher Evans; Colin Leach; Dennis Holt; Xin Su; Dwight Morrow; Harvey Fries; Kevin Thorneloe; Richard Edwards
Journal: ACS Med Chem Lett Date: 2010-05-14 Impact factor: 4.345

3. Fluorescent Human EP3 Receptor Antagonists.

Authors: Miriam Tomasch; J Stephan Schwed; Karina Kuczka; Sascha Meyer Dos Santos; Sebastian Harder; Rolf M Nüsing; Alexander Paulke; Holger Stark
Journal: ACS Med Chem Lett Date: 2012-08-08 Impact factor: 4.345

4. Adenosine A(1) and prostaglandin E receptor 3 receptors mediate global airway contraction after local epithelial injury.

Authors: Jian Zhou; Martha B Alvarez-Elizondo; Elliot Botvinick; Steven C George
Journal: Am J Respir Cell Mol Biol Date: 2012-12-06 Impact factor: 6.914

5. Prostaglandins of the E series inhibit monoamine release via EP3 receptors: proof with the competitive EP3 receptor antagonist L-826,266.

Authors: J Günther; K Schulte; D Wenzel; B Malinowska; E Schlicker
Journal: Naunyn Schmiedebergs Arch Pharmacol Date: 2009-12-10 Impact factor: 3.000

Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor.

1. The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

2. Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists.

3. Fluorescent Human EP3 Receptor Antagonists.

4. Adenosine A(1) and prostaglandin E receptor 3 receptors mediate global airway contraction after local epithelial injury.

5. Prostaglandins of the E series inhibit monoamine release via EP3 receptors: proof with the competitive EP3 receptor antagonist L-826,266.

Review 6. Prostanoid receptor antagonists: development strategies and therapeutic applications.

7. Prostaglandin E2 regulates melanocyte dendrite formation through activation of PKCzeta.

8. Activation of prostaglandin EP receptors by lubiprostone in rat and human stomach and colon.

9. Dual modulation of urinary bladder activity and urine flow by prostanoid EP3 receptors in the conscious rat.

10. Cross-couplings between benzylic and aryl halides "on water": synthesis of diarylmethanes.