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Literature DB >> 26227772

C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.

Abstract

A group of aporphine alkaloids related to (±)-nantenine (1) and bearing a C4 phenyl and various C1 or N-substituents, was synthesized and evaluated for affinity to h5-HT receptors. In general, unlike nantenine, the analogs lack affinity for the h5-HT(2A) receptor and other 5-HT receptors but bind selectively to the h5-HT(2B) receptor. With regards to 5-HT(2B) affinity, there appears to be a low tolerance for bulky C1 or N-substituents when the C4 phenyl moiety is present. Compound 5a had the highest 5-HT(2B) affinity of the compounds tested, was found to be an antagonist and is selective vs other CNS receptors.

Entities: CellLine Chemical Disease Gene Species

Keywords: 5-HT(2A); 5-HT(2B); Aporphine; CNS; Nantenine

Mesh：

Substances：

Year: 2015 PMID： 26227772 PMCID： PMC4523491 DOI： 10.1016/j.bmcl.2015.07.012

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

33 in total

1. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.

Authors: D W Bonhaus; L A Flippin; R J Greenhouse; S Jaime; C Rocha; M Dawson; K Van Natta; L K Chang; T Pulido-Rios; A Webber; E Leung; R M Eglen; G R Martin
Journal: Br J Pharmacol Date: 1999-07 Impact factor: 8.739

2. Affinity of aporphines for the human 5-HT2A receptor: insights from homology modeling and molecular docking studies.

Authors: Stevan Pecic; Pooja Makkar; Sandeep Chaudhary; Boojala V Reddy; Hernan A Navarro; Wayne W Harding
Journal: Bioorg Med Chem Date: 2010-06-20 Impact factor: 3.641

3. Evaluation of structural effects on 5-HT(2A) receptor antagonism by aporphines: identification of a new aporphine with 5-HT(2A) antagonist activity.

Authors: Shashikanth Ponnala; Junior Gonzales; Nirav Kapadia; Hernan A Navarro; Wayne W Harding
Journal: Bioorg Med Chem Lett Date: 2014-03-04 Impact factor: 2.823

4. (6aR)-11-amino-N-propyl-noraporphine, a new dopamine D2 and serotonin 5-HT1A dual agonist, elicits potent antiparkinsonian action and attenuates levodopa-induced dyskinesia in a 6-OHDA-lesioned rat model of Parkinson's disease.

Authors: Rui Zhao; Weijian Lu; Xing Fang; Lin Guo; Zhi Yang; Na Ye; Jiahao Zhao; Zhili Liu; Jia Jia; Longtai Zheng; Bin Zhao; Ao Zhang; Xuechu Zhen
Journal: Pharmacol Biochem Behav Date: 2014-06-21 Impact factor: 3.533

Review 5. Receptor targets for antidepressant therapy in bipolar disorder: an overview.

Authors: Konstantinos N Fountoulakis; John R Kelsoe; Hagop Akiskal
Journal: J Affect Disord Date: 2011-05-20 Impact factor: 4.839

6. New aporphinoid 5-HT2A and α1A antagonists via structural manipulations of nantenine.

Authors: Sandeep Chaudhary; Shashikanth Ponnala; Onica Legendre; Junior A Gonzales; Hernán A Navarro; Wayne W Harding
Journal: Bioorg Med Chem Date: 2011-08-18 Impact factor: 3.641

7. 9-(Aminomethyl)-9,10-dihydroanthracene is a novel and unlikely 5-HT2A receptor antagonist.

Authors: R B Westkaemper; S P Runyon; M L Bondarev; J E Savage; B L Roth; R A Glennon
Journal: Eur J Pharmacol Date: 1999-09-03 Impact factor: 4.432

8. 9-Aminomethyl-9,10-dihydroanthracene (AMDA) analogs as structural probes for steric tolerance in 5-HT2A and H1 receptor binding sites.

Authors: Jitesh R Shah; Philip D Mosier; Srinivas Peddi; Bryan L Roth; Richard B Westkaemper
Journal: Bioorg Med Chem Lett Date: 2009-12-23 Impact factor: 2.823