Literature DB >> 28129534

A Receptor on Acid.

Qiuyan Chen1, John J G Tesmer2.   

Abstract

Wacker et al. report the crystal structure of LSD in complex with one of its major targets in the brain, the 5-HT2B receptor, the first such structure for any psychedelic drug. The results shed light on the molecular mechanisms underlying its ability to induce hallucinations with greater duration and potency than closely related compounds.
Copyright © 2017 Elsevier Inc. All rights reserved.

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Year:  2017        PMID： 28129534      PMCID： PMC5520807          DOI： 10.1016/j.cell.2017.01.012

Source DB:  PubMed          Journal:  Cell        ISSN： 0092-8674            Impact factor:   41.582


  8 in total

1.  Serotonin, but not N-methyltryptamines, activates the serotonin 2A receptor via a ß-arrestin2/Src/Akt signaling complex in vivo.

Authors:  Cullen L Schmid; Laura M Bohn
Journal:  J Neurosci       Date:  2010-10-06       Impact factor: 6.167

Review 2.  Functional selectivity and classical concepts of quantitative pharmacology.

Authors:  Jonathan D Urban; William P Clarke; Mark von Zastrow; David E Nichols; Brian Kobilka; Harel Weinstein; Jonathan A Javitch; Bryan L Roth; Arthur Christopoulos; Patrick M Sexton; Keith J Miller; Michael Spedding; Richard B Mailman
Journal:  J Pharmacol Exp Ther       Date:  2006-06-27       Impact factor: 4.030

Review 3.  Beta-arrestin-biased ligands at seven-transmembrane receptors.

Authors:  Jonathan D Violin; Robert J Lefkowitz
Journal:  Trends Pharmacol Sci       Date:  2007-07-20       Impact factor: 14.819

4.  How LSD originated.

Authors:  A Hofmann
Journal:  J Psychedelic Drugs       Date:  1979 Jan-Jun

5.  Agonist-directed signaling of the serotonin 2A receptor depends on beta-arrestin-2 interactions in vivo.

Authors:  Cullen L Schmid; Kirsten M Raehal; Laura M Bohn
Journal:  Proc Natl Acad Sci U S A       Date:  2008-01-14       Impact factor: 11.205

6.  Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD).

Authors:  David E Nichols; Stewart Frescas; Danuta Marona-Lewicka; Deborah M Kurrasch-Orbaugh
Journal:  J Med Chem       Date:  2002-09-12       Impact factor: 7.446

7.  Structural features for functional selectivity at serotonin receptors.

Authors:  Daniel Wacker; Chong Wang; Vsevolod Katritch; Gye Won Han; Xi-Ping Huang; Eyal Vardy; John D McCorvy; Yi Jiang; Meihua Chu; Fai Yiu Siu; Wei Liu; H Eric Xu; Vadim Cherezov; Bryan L Roth; Raymond C Stevens
Journal:  Science       Date:  2013-03-21       Impact factor: 47.728

8.  Radioligand binding evidence implicates the brain 5-HT2 receptor as a site of action for LSD and phenylisopropylamine hallucinogens.

Authors:  M Titeler; R A Lyon; R A Glennon
Journal:  Psychopharmacology (Berl)       Date:  1988       Impact factor: 4.530
  8 in total
  3 in total

Review 1.  Arresting the Development of Addiction: The Role of β-Arrestin 2 in Drug Abuse.

Authors:  Kirsten A Porter-Stransky; David Weinshenker
Journal:  J Pharmacol Exp Ther       Date:  2017-03-16       Impact factor: 4.030

2.  Free energy calculations of the functional selectivity of 5-HT2B G protein-coupled receptor.

Authors:  Brandon L Peters; Jinxia Deng; Andrew L Ferguson
Journal:  PLoS One       Date:  2020-12-09       Impact factor: 3.240

Review 3.  1H Nuclear Magnetic Resonance: A Future Approach to the Metabolic Profiling of Psychedelics in Human Biofluids?

Authors:  Sylvana Vilca-Melendez; Malin V Uthaug; Julian L Griffin
Journal:  Front Psychiatry       Date:  2021-12-13       Impact factor: 4.157
  3 in total

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