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 Affinity of fentanyl and its derivatives for the σ1-receptor.

Literature DB >> 31391893

Affinity of fentanyl and its derivatives for the σ₁-receptor.

Piotr F J Lipiński¹, Edina Szűcs^2,3, Małgorzata Jarończyk⁴, Piotr Kosson⁵, Sándor Benyhe², Aleksandra Misicka^1,6, Ján Cz Dobrowolski⁴, Joanna Sadlej⁷.

Abstract

Fentanyl and its 11 commercially available derivatives were investigated as to their affinity for the σ1 receptor. The parent compound is a rather poor binder (IC50 = 4973 nM), but its close derivatives (benzylfentanyl or p-fluorofentanyl) have submicromolar affinities. Modelling provides a structural basis for the observed trends in activity.

Entities: Chemical

Year: 2019 PMID： 31391893 PMCID： PMC6657672 DOI： 10.1039/c9md00222g

Source DB: PubMed Journal: Medchemcomm ISSN： 2040-2503 Impact factor: 3.597

22 in total

Review 1. Sigma receptors: potential targets for a new class of antidepressant drug.

Authors: James A Fishback; Matthew J Robson; Yan-Tong Xu; Rae R Matsumoto
Journal: Pharmacol Ther Date: 2010-05-11 Impact factor: 12.310

Review 2. Early development of sigma-receptor ligands.

Authors: Sanju Narayanan; Rohit Bhat; Christophe Mesangeau; Jacques H Poupaert; Christopher R McCurdy
Journal: Future Med Chem Date: 2011-01 Impact factor: 3.808

3. AutoDock Vina: improving the speed and accuracy of docking with a new scoring function, efficient optimization, and multithreading.

Authors: Oleg Trott; Arthur J Olson
Journal: J Comput Chem Date: 2010-01-30 Impact factor: 3.376

4. Phase II trial of the Sigma-1 receptor agonist cutamesine (SA4503) for recovery enhancement after acute ischemic stroke.

Authors: Roman Urfer; Hans J Moebius; David Skoloudik; Estevo Santamarina; Wakao Sato; Shiro Mita; Keith W Muir
Journal: Stroke Date: 2014-09-30 Impact factor: 7.914

5. Uniform assessment and ranking of opioid μ receptor binding constants for selected opioid drugs.

Authors: Donna A Volpe; Grainne A McMahon Tobin; R Daniel Mellon; Aspandiar G Katki; Robert J Parker; Thomas Colatsky; Timothy J Kropp; S Leigh Verbois
Journal: Regul Toxicol Pharmacol Date: 2011-01-06 Impact factor: 3.271

6. Ether modifications to 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine (SA4503): effects on binding affinity and selectivity for sigma receptors and monoamine transporters.

Authors: Rong Xu; Sarah A Lord; Ryan M Peterson; Emily A Fergason-Cantrell; John R Lever; Susan Z Lever
Journal: Bioorg Med Chem Date: 2014-11-11 Impact factor: 3.641

7. Anti-amnesic and neuroprotective potentials of the mixed muscarinic receptor/sigma 1 (σ1) ligand ANAVEX2-73, a novel aminotetrahydrofuran derivative.

Authors: Vanessa Villard; Julie Espallergues; Emeline Keller; Alexandre Vamvakides; Tangui Maurice
Journal: J Psychopharmacol Date: 2010-09-09 Impact factor: 4.153

Affinity of fentanyl and its derivatives for the σ₁-receptor.

Review 1. Sigma receptors: potential targets for a new class of antidepressant drug.

Review 2. Early development of sigma-receptor ligands.

3. AutoDock Vina: improving the speed and accuracy of docking with a new scoring function, efficient optimization, and multithreading.

4. Phase II trial of the Sigma-1 receptor agonist cutamesine (SA4503) for recovery enhancement after acute ischemic stroke.

5. Uniform assessment and ranking of opioid μ receptor binding constants for selected opioid drugs.

6. Ether modifications to 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine (SA4503): effects on binding affinity and selectivity for sigma receptors and monoamine transporters.

7. Anti-amnesic and neuroprotective potentials of the mixed muscarinic receptor/sigma 1 (σ1) ligand ANAVEX2-73, a novel aminotetrahydrofuran derivative.

Review 8. Sigma receptor ligands: possible application as therapeutic drugs and as radiopharmaceuticals.

Review 9. The pharmacology of sigma-1 receptors.

10. Pharmacology and therapeutic potential of sigma(1) receptor ligands.

Review 1. Unique Pharmacology, Brain Dysfunction, and Therapeutic Advancements for Fentanyl Misuse and Abuse.

Review 2. Fentanyl Structure as a Scaffold for Opioid/Non-Opioid Multitarget Analgesics.