Targeting GABAB receptors for anti-Abuse drug discovery

Tamara Phillips, Cheryl Reed

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

Introduction: There is increasing evidence encouraging the development of drugs that positively modulate the γ-Aminobutyric acid type B (GABAB) receptor for combating addiction. Compounds that target GABAB receptors are unique as anti-Abuse therapies because of their impact against multiple addictive drugs.Areas covered: The authors present the basic information concerning the drug actions of GABA and GABAB receptor orthosteric agonists and positive allosteric modulators (PAM). Furthermore, they discuss several recent excellent reviews and newer results pertaining to GABAB receptor drug effects on responses to and self-Administration of: alcohol (ethanol), nicotine, cocaine, (meth)amphetamine, and opioids. Preclinical and clinical data are considered.Expert opinion: Clinical data exist only for baclofen and mostly for alcohol use disorders. Additional trials are needed, but effects are promising. Whether PAMs, given alone or in combination with a direct GABAB receptor agonist, will be clinically effective and have fewer side effects requires investigation. The sedative effects of baclofen, a Food and Drug Administration (FDA)-Approved drug, become less severe over time. Based on existing data, baclofen is well-tolerated. However, genetic and physiological differences are likely to contribute to individual responses to different therapeutic agents. The more immediate development of baclofen as a therapeutic for alcohol use disorders may be of significant benefit to some individuals.

Original languageEnglish (US)
Pages (from-to)1307-1317
Number of pages11
JournalExpert Opinion on Drug Discovery
Volume9
Issue number11
DOIs
StatePublished - Nov 1 2014

Fingerprint

Baclofen
Drug Discovery
Alcohols
Pharmaceutical Preparations
Aminobutyrates
Drug Receptors
GABA Receptors
Self Administration
Expert Testimony
Therapeutic Uses
Amphetamine
United States Food and Drug Administration
Hypnotics and Sedatives
Nicotine
Cocaine
Opioid Analgesics
Ethanol
Therapeutics

Keywords

  • Addiction
  • Alcohol
  • Amphetamine
  • Baclofen
  • Cocaine
  • Ethanol
  • Methamphetamine
  • Nicotine
  • Opioid
  • Positive allosteric modulator

ASJC Scopus subject areas

  • Drug Discovery
  • Medicine(all)

Cite this

Targeting GABAB receptors for anti-Abuse drug discovery. / Phillips, Tamara; Reed, Cheryl.

In: Expert Opinion on Drug Discovery, Vol. 9, No. 11, 01.11.2014, p. 1307-1317.

Research output: Contribution to journalArticle

@article{6d8669f04fd741c9af2cdea61a21f40e,
title = "Targeting GABAB receptors for anti-Abuse drug discovery",
abstract = "Introduction: There is increasing evidence encouraging the development of drugs that positively modulate the γ-Aminobutyric acid type B (GABAB) receptor for combating addiction. Compounds that target GABAB receptors are unique as anti-Abuse therapies because of their impact against multiple addictive drugs.Areas covered: The authors present the basic information concerning the drug actions of GABA and GABAB receptor orthosteric agonists and positive allosteric modulators (PAM). Furthermore, they discuss several recent excellent reviews and newer results pertaining to GABAB receptor drug effects on responses to and self-Administration of: alcohol (ethanol), nicotine, cocaine, (meth)amphetamine, and opioids. Preclinical and clinical data are considered.Expert opinion: Clinical data exist only for baclofen and mostly for alcohol use disorders. Additional trials are needed, but effects are promising. Whether PAMs, given alone or in combination with a direct GABAB receptor agonist, will be clinically effective and have fewer side effects requires investigation. The sedative effects of baclofen, a Food and Drug Administration (FDA)-Approved drug, become less severe over time. Based on existing data, baclofen is well-tolerated. However, genetic and physiological differences are likely to contribute to individual responses to different therapeutic agents. The more immediate development of baclofen as a therapeutic for alcohol use disorders may be of significant benefit to some individuals.",
keywords = "Addiction, Alcohol, Amphetamine, Baclofen, Cocaine, Ethanol, Methamphetamine, Nicotine, Opioid, Positive allosteric modulator",
author = "Tamara Phillips and Cheryl Reed",
year = "2014",
month = "11",
day = "1",
doi = "10.1517/17460441.2014.956076",
language = "English (US)",
volume = "9",
pages = "1307--1317",
journal = "Expert Opinion on Drug Discovery",
issn = "1746-0441",
publisher = "Informa Healthcare",
number = "11",

}

TY - JOUR

T1 - Targeting GABAB receptors for anti-Abuse drug discovery

AU - Phillips, Tamara

AU - Reed, Cheryl

PY - 2014/11/1

Y1 - 2014/11/1

N2 - Introduction: There is increasing evidence encouraging the development of drugs that positively modulate the γ-Aminobutyric acid type B (GABAB) receptor for combating addiction. Compounds that target GABAB receptors are unique as anti-Abuse therapies because of their impact against multiple addictive drugs.Areas covered: The authors present the basic information concerning the drug actions of GABA and GABAB receptor orthosteric agonists and positive allosteric modulators (PAM). Furthermore, they discuss several recent excellent reviews and newer results pertaining to GABAB receptor drug effects on responses to and self-Administration of: alcohol (ethanol), nicotine, cocaine, (meth)amphetamine, and opioids. Preclinical and clinical data are considered.Expert opinion: Clinical data exist only for baclofen and mostly for alcohol use disorders. Additional trials are needed, but effects are promising. Whether PAMs, given alone or in combination with a direct GABAB receptor agonist, will be clinically effective and have fewer side effects requires investigation. The sedative effects of baclofen, a Food and Drug Administration (FDA)-Approved drug, become less severe over time. Based on existing data, baclofen is well-tolerated. However, genetic and physiological differences are likely to contribute to individual responses to different therapeutic agents. The more immediate development of baclofen as a therapeutic for alcohol use disorders may be of significant benefit to some individuals.

AB - Introduction: There is increasing evidence encouraging the development of drugs that positively modulate the γ-Aminobutyric acid type B (GABAB) receptor for combating addiction. Compounds that target GABAB receptors are unique as anti-Abuse therapies because of their impact against multiple addictive drugs.Areas covered: The authors present the basic information concerning the drug actions of GABA and GABAB receptor orthosteric agonists and positive allosteric modulators (PAM). Furthermore, they discuss several recent excellent reviews and newer results pertaining to GABAB receptor drug effects on responses to and self-Administration of: alcohol (ethanol), nicotine, cocaine, (meth)amphetamine, and opioids. Preclinical and clinical data are considered.Expert opinion: Clinical data exist only for baclofen and mostly for alcohol use disorders. Additional trials are needed, but effects are promising. Whether PAMs, given alone or in combination with a direct GABAB receptor agonist, will be clinically effective and have fewer side effects requires investigation. The sedative effects of baclofen, a Food and Drug Administration (FDA)-Approved drug, become less severe over time. Based on existing data, baclofen is well-tolerated. However, genetic and physiological differences are likely to contribute to individual responses to different therapeutic agents. The more immediate development of baclofen as a therapeutic for alcohol use disorders may be of significant benefit to some individuals.

KW - Addiction

KW - Alcohol

KW - Amphetamine

KW - Baclofen

KW - Cocaine

KW - Ethanol

KW - Methamphetamine

KW - Nicotine

KW - Opioid

KW - Positive allosteric modulator

UR - http://www.scopus.com/inward/record.url?scp=84911493202&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84911493202&partnerID=8YFLogxK

U2 - 10.1517/17460441.2014.956076

DO - 10.1517/17460441.2014.956076

M3 - Article

C2 - 25195620

AN - SCOPUS:84911493202

VL - 9

SP - 1307

EP - 1317

JO - Expert Opinion on Drug Discovery

JF - Expert Opinion on Drug Discovery

SN - 1746-0441

IS - 11

ER -