Literature DB >> 26494260

Muscarinic acetylcholine receptor binding affinities of pethidine analogs.

Na-Ra Lee1, Xuan Zhang2, Mahesh Darna1, Linda P Dwoskin1, Guangrong Zheng2.   

Abstract

A series of pethidine analogs were synthesized and their affinities for the [(3)H]N-methyl-scopolamine (NMS) binding site on muscarinic acetylcholine receptors (mAChRs) were determined using M1, M3 or M5 human mAChRs expressed by Chinese hamster ovary (CHO) cell membranes. Compound 6b showed the highest binding affinities at M1, M3 and M5 mAChRs (Ki=0.67, 0.37, and 0.38 μM, respectively).
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Drug abuse; Muscarinic acetylcholine receptors; Pethidine; [(3)H]NMS binding affinity

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Year:  2015        PMID： 26494260      PMCID： PMC4629469          DOI： 10.1016/j.bmcl.2015.10.029

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


  17 in total

1.  M5 muscarinic receptors are required for prolonged accumbal dopamine release after electrical stimulation of the pons in mice.

Authors:  Gina L Forster; John S Yeomans; Junichi Takeuchi; Charles D Blaha
Journal:  J Neurosci       Date:  2002-01-01       Impact factor: 6.167

2.  Laterodorsal tegmental stimulation elicits dopamine efflux in the rat nucleus accumbens by activation of acetylcholine and glutamate receptors in the ventral tegmental area.

Authors:  G L Forster; C D Blaha
Journal:  Eur J Neurosci       Date:  2000-10       Impact factor: 3.386

3.  Localization of m5 muscarinic receptor mRNA in rat brain examined by in situ hybridization histochemistry.

Authors:  M T Vilaró; J M Palacios; G Mengod
Journal:  Neurosci Lett       Date:  1990-07-03       Impact factor: 3.046

4.  Expression of muscarinic acetylcholine and dopamine receptor mRNAs in rat basal ganglia.

Authors:  D M Weiner; A I Levey; M R Brann
Journal:  Proc Natl Acad Sci U S A       Date:  1990-09       Impact factor: 11.205

5.  Drugs abused by humans preferentially increase synaptic dopamine concentrations in the mesolimbic system of freely moving rats.

Authors:  G Di Chiara; A Imperato
Journal:  Proc Natl Acad Sci U S A       Date:  1988-07       Impact factor: 11.205

6.  Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.

Authors:  Y Cheng; W H Prusoff
Journal:  Biochem Pharmacol       Date:  1973-12-01       Impact factor: 5.858

7.  Destruction of dopaminergic nerve terminals in nucleus accumbens: effect on d-amphetamine self-administration.

Authors:  W H Lyness; N M Friedle; K E Moore
Journal:  Pharmacol Biochem Behav       Date:  1979-11       Impact factor: 3.533

8.  Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes.

Authors:  T I Bonner; A C Young; M R Brann; N J Buckley
Journal:  Neuron       Date:  1988-07       Impact factor: 17.173

9.  Role for M5 muscarinic acetylcholine receptors in cocaine addiction.

Authors:  Anders Fink-Jensen; Irina Fedorova; Gitta Wörtwein; David P D Woldbye; Thøger Rasmussen; Morgane Thomsen; Tom G Bolwig; Karen M Knitowski; David L McKinzie; Masahisa Yamada; Jürgen Wess; Anthony Basile
Journal:  J Neurosci Res       Date:  2003-10-01       Impact factor: 4.164

10.  Deletion of the M5 muscarinic acetylcholine receptor attenuates morphine reinforcement and withdrawal but not morphine analgesia.

Authors:  Anthony S Basile; Irina Fedorova; Agustin Zapata; Xiaoguang Liu; Toni Shippenberg; Alokesh Duttaroy; Masahisa Yamada; Jurgen Wess
Journal:  Proc Natl Acad Sci U S A       Date:  2002-08-01       Impact factor: 11.205
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