From Wikipedia, the free encyclopedia
Chemical compound
GS-39783 is a compound used in scientific research which acts as a
positive allosteric modulator at the
GABAB
receptor .
[1]
[2] It has been shown to produce
anxiolytic effects in animal studies,
[3]
[4]
[5] and reduces self-administration of
alcohol ,
[6]
[7]
cocaine
[8]
[9]
[10] and
nicotine .
[11]
References
^ Urwyler S, Pozza MF, Lingenhoehl K, Mosbacher J, Lampert C, Froestl W, et al. (October 2003). "N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function". The Journal of Pharmacology and Experimental Therapeutics . 307 (1): 322–30.
doi :
10.1124/jpet.103.053074 .
PMID
12954816 .
^ Guery S, Floersheim P, Kaupmann K, Froestl W (November 2007).
"Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors" . Bioorganic & Medicinal Chemistry Letters . 17 (22): 6206–11.
doi :
10.1016/j.bmcl.2007.09.023 .
PMC
2278029 .
PMID
17884493 .
^ Mombereau C, Kaupmann K, Froestl W, Sansig G, van der Putten H, Cryan JF (June 2004).
"Genetic and pharmacological evidence of a role for GABA(B) receptors in the modulation of anxiety- and antidepressant-like behavior" . Neuropsychopharmacology . 29 (6): 1050–62.
doi :
10.1038/sj.npp.1300413 .
PMID
15039762 .
^ Cryan JF, Kelly PH, Chaperon F, Gentsch C, Mombereau C, Lingenhoehl K, et al. (September 2004). "Behavioral characterization of the novel GABAB receptor-positive modulator GS39783 (N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine): anxiolytic-like activity without side effects associated with baclofen or benzodiazepines". The Journal of Pharmacology and Experimental Therapeutics . 310 (3): 952–63.
doi :
10.1124/jpet.104.066753 .
PMID
15113848 .
^ Jacobson LH, Cryan JF (April 2008). "Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents". Neuropharmacology . 54 (5): 854–62.
doi :
10.1016/j.neuropharm.2008.01.004 .
PMID
18328507 .
^ Orrù A, Lai P, Lobina C, Maccioni P, Piras P, Scanu L, et al. (November 2005). "Reducing effect of the positive allosteric modulators of the GABA(B) receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats". European Journal of Pharmacology . 525 (1–3): 105–11.
doi :
10.1016/j.ejphar.2005.10.005 .
PMID
16289452 .
^ Maccioni P, Pes D, Orrù A, Froestl W, Gessa GL, Carai MA, Colombo G (August 2007). "Reducing effect of the positive allosteric modulator of the GABA(B) receptor, GS39,783, on alcohol self-administration in alcohol-preferring rats". Psychopharmacology . 193 (2): 171–8.
doi :
10.1007/s00213-007-0776-1 .
PMID
17393141 .
^ Smith MA, Yancey DL, Morgan D, Liu Y, Froestl W, Roberts DC (April 2004). "Effects of positive allosteric modulators of the GABAB receptor on cocaine self-administration in rats". Psychopharmacology . 173 (1–2): 105–11.
doi :
10.1007/s00213-003-1706-5 .
PMID
14712341 .
^ Slattery DA, Markou A, Froestl W, Cryan JF (November 2005).
"The GABAB receptor-positive modulator GS39783 and the GABAB receptor agonist baclofen attenuate the reward-facilitating effects of cocaine: intracranial self-stimulation studies in the rat" . Neuropsychopharmacology . 30 (11): 2065–72.
doi :
10.1038/sj.npp.1300734 .
PMID
15841108 .
^ Lhuillier L, Mombereau C, Cryan JF, Kaupmann K (February 2007).
"GABA(B) receptor-positive modulation decreases selective molecular and behavioral effects of cocaine" . Neuropsychopharmacology . 32 (2): 388–98.
doi :
10.1038/sj.npp.1301102 .
PMC
1774586 .
PMID
16710312 .
^ Paterson NE, Vlachou S, Guery S, Kaupmann K, Froestl W, Markou A (July 2008).
"Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats" . The Journal of Pharmacology and Experimental Therapeutics . 326 (1): 306–14.
doi :
10.1124/jpet.108.139204 .
PMC
2574924 .
PMID
18445779 .
Ionotropic
GABAA Tooltip γ-Aminobutyric acid A receptor
Positive modulators (abridged; see
here for a full list):
α-EMTBL
Alcohols (e.g.,
drinking alcohol ,
2M2B )
Anabolic steroids
Avermectins (e.g.,
ivermectin )
Barbiturates (e.g.,
phenobarbital )
Benzodiazepines (e.g.,
diazepam )
Bromide compounds (e.g.,
potassium bromide )
Carbamates (e.g.,
meprobamate )
Carbamazepine
Chloralose
Chlormezanone
Clomethiazole
Dihydroergolines (e.g.,
ergoloid (dihydroergotoxine) )
Etazepine
Etifoxine
Fenamates (e.g.,
mefenamic acid )
Flavonoids (e.g.,
apigenin ,
hispidulin )
Fluoxetine
Flupirtine
Imidazoles (e.g.,
etomidate )
Kava constituents (e.g.,
kavain )
Lanthanum
Loreclezole
Monastrol
Neuroactive steroids (e.g.,
allopregnanolone ,
cholesterol ,
THDOC )
Niacin
Niacinamide
Nonbenzodiazepines (e.g.,
β-carbolines (e.g.,
abecarnil ),
cyclopyrrolones (e.g.,
zopiclone ),
imidazopyridines (e.g.,
zolpidem ),
pyrazolopyrimidines (e.g.,
zaleplon ))
Norfluoxetine
Petrichloral
Phenols (e.g.,
propofol )
Phenytoin
Piperidinediones (e.g.,
glutethimide )
Propanidid
Pyrazolopyridines (e.g.,
etazolate )
Quinazolinones (e.g.,
methaqualone )
Retigabine (ezogabine)
ROD-188
Skullcap constituents (e.g.,
baicalin )
Stiripentol
Sulfonylalkanes (e.g.,
sulfonmethane (sulfonal) )
Topiramate
Valerian constituents (e.g.,
valerenic acid )
Volatiles /
gases (e.g.,
chloral hydrate ,
chloroform ,
diethyl ether ,
paraldehyde ,
sevoflurane )
Negative modulators:
1,3M1B
3M2B
11-Ketoprogesterone
17-Phenylandrostenol
α3IA
α5IA (LS-193,268)
β-CCB
β-CCE
β-CCM
β-CCP
β-EMGBL
Anabolic steroids
Amiloride
Anisatin
β-Lactams (e.g.,
penicillins ,
cephalosporins ,
carbapenems )
Basmisanil
Bemegride
Bicyclic phosphates (
TBPS ,
TBPO ,
IPTBO )
BIDN
Bilobalide
Bupropion
CHEB
Chlorophenylsilatrane
Cicutoxin
Cloflubicyne
Cyclothiazide
DHEA
DHEA-S
Dieldrin
(+)-DMBB
DMCM
DMPC
EBOB
Etbicyphat
FG-7142 (ZK-31906)
Fiproles (e.g.,
fipronil )
Flavonoids (e.g.,
amentoflavone ,
oroxylin A )
Flumazenil
Fluoroquinolones (e.g.,
ciprofloxacin )
Flurothyl
Furosemide
Golexanolone
Iomazenil (123 I)
IPTBO
Isopregnanolone (sepranolone)
L-655,708
Laudanosine
Lindane
MaxiPost
Morphine
Morphine-3-glucuronide
MRK-016
Naloxone
Naltrexone
Nicardipine
Nonsteroidal antiandrogens (e.g.,
apalutamide ,
bicalutamide ,
enzalutamide ,
flutamide ,
nilutamide )
Oenanthotoxin
Pentylenetetrazol (pentetrazol)
Phenylsilatrane
Picrotoxin (i.e.,
picrotin ,
picrotoxinin and
dihydropicrotoxinin )
Pregnenolone sulfate
Propybicyphat
PWZ-029
Radequinil
Ro 15-4513
Ro 19-4603
RO4882224
RO4938581
Sarmazenil
SCS
Suritozole
TB-21007
TBOB
TBPS
TCS-1105
Terbequinil
TETS
Thujone
U-93631
Zinc
ZK-93426
GABAA -ρ Tooltip γ-Aminobutyric acid A-rho receptor
Metabotropic
GABAB Tooltip γ-Aminobutyric acid B receptor