Evidence map›Paper›PMID 21050177›Full record

ReviewCurrent topics in medicinal chemistry2011

Design, synthesis and interaction at the vesicular monoamine transporter-2 of lobeline analogs: potential pharmacotherapies for the treatment of psychostimulant abuse.

Peter A Crooks, Guangrong Zheng, Ashish P Vartak, John P Culver, Fang Zheng, David B Horton, Linda P Dwoskin

Abstract readReview
In one paragraph

Review in Current topics in medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
1.2field-weighted citation impact, top 23% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

11 citing papers in PubMed, 22 citations in OpenAlex.

  1. Article
  2. Review
  3. Review
  4. FromMolecules (Basel, Switzerland) · 2022
    Article
  5. Article
  6. Article
  7. Article
  8. Article
  9. Exploring the effect ofMedChemComm · 2013
    Article
  10. Article
  11. Synthesis of Lobeline, Lobelane and their Analogues. A Review.Organic preparations and procedures international
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

7 authors at 2 institutions in 1 country.

Peter A CrooksDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, 40536-0082, USA. pcrooks@email.uky.edu
Guangrong Zheng
Ashish P Vartak
John P Culver
Fang Zheng
David B Horton
Linda P Dwoskin
University of Kentucky · USCenter for Drug Evaluation and Research · US

Funding

Kentucky Center for Clinical and Translational ScienceUL1TR001998 · NCATS · UNIVERSITY OF KENTUCKY · PI HARTMANN, KATHERINE E, KERN, PHILIP A · 2016 to 2025
$34.2M
Kentucky Center for Clinical and Translational ScienceUL1TR000117 · NCATS · UNIVERSITY OF KENTUCKY · PI KERN, PHILIP A · 2012 to 2015
$13.3M
Development of Novel Therapies or Methamphetamine AbuseR01DA013519 · NIDA · UNIVERSITY OF KENTUCKY · PI DWOSKIN, LINDA P · 2000 to 2009
$5.1M
Training in Drug Abuse Related Research.T32DA016176 · NIDA · UNIVERSITY OF KENTUCKY · PI DWOSKIN, LINDA P · 2004 to 2020
$4.0M
KENTUCKY CENTER FOR CLINICAL AND TRANSLATIONAL SCIENCEUL1RR033173 · NCRR · UNIVERSITY OF KENTUCKY · PI KERN, PHILIP A · 2011 to 2011
$3.5M
Development of Novel Therapies or Methamphetamine AbuseU01DA013519 · NIDA · UNIVERSITY OF KENTUCKY · PI DWOSKIN, LINDA P · 2012 to 2016
$3.2M
NCATS NIH HHS UL1 TR000117NCATS NIH HHS UL1 TR001998NCRR NIH HHS UL1 RR033173NIDA NIH HHS DA013519NIDA NIH HHS R01 DA013519NIDA NIH HHS T32 DA016176NIDA NIH HHS U01 DA013519
6 · The paper itself

Abstract

The vesicular monoamine transporter-2 (VMAT2) is considered as a new target for the development of novel therapeutics to treat psychostimulant abuse. Current information on the structure, function and role of VMAT2 in psychostimulant abuse are presented. Lobeline, the major alkaloidal constituent of Lobelia inflata, interacts with nicotinic receptors and with VMAT2. Numerous studies have shown that lobeline inhibits both the neurochemical and behavioral effects of amphetamine in rodents, and behavioral studies demonstrate that lobeline has potential as a pharmacotherapy for psychostimulant abuse. Systematic structural modification of the lobeline molecule is described with the aim of improving selectivity and affinity for VMAT2 over neuronal nicotinic acetylcholine receptors and other neurotransmitter transporters. This has led to the discovery of more potent and selective ligands for VMAT2. In addition, a computational neural network analysis of the affinity of these lobeline analogs for VMAT2 has been carried out, which provides computational models that have predictive value in the rational design of VMAT2 ligands and is also useful in identifying drug candidates from virtual libraries for subsequent synthesis and evaluation.

Indexed as

LobelinePsychotropic DrugsAnimalsBehavior, AddictiveBinding SitesDrug DesignDrug TherapyHumansLibraries, DigitalLigandsLobeliaMiceMolecular Targeted TherapyNeural Networks, ComputerNeuronsRatsLigandsLobelinePsychotropic DrugsReceptors, NicotinicVesicular Monoamine Transport Proteins

Identifiers

PMID21050177
PMCPMC3725992
OpenAlexW1988318282

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.