Page last updated: 2024-11-07

cgp 35348

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

CGP 35348: antagonizes both GABA-A and GABA-B receptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID107699
CHEMBL ID40157
SCHEMBL ID195698
MeSH IDM0182296

Synonyms (44)

Synonym
123690-79-9
(3-amino-propyl)-diethoxymethyl-phosphinic acid
bdbm50033003
cgp35348
3-aminopropyl-(diethoxymethyl)phosphinic acid
gtpl1069
BIOMOL-NT_000237
NCGC00025074-01
tocris-1245
PDSP1_000410
PDSP2_000408
cgp 35348
BPBIO1_000508
NCGC00025074-02
c8h20no4p
cgp-35348
phosphinic acid, (3-aminopropyl)(diethoxymethyl)-
p-(3-aminopropyl)-p-diethoxymethylphosphinic acid
CHEMBL40157 ,
L000168
3-aminopropyl(diethoxymethyl)phosphinic acid
unii-87ti61875h
87ti61875h ,
cgp 35348 hydrate
SCHEMBL195698
QIIVUOWTHWIXFO-UHFFFAOYSA-N
(3-aminopropyl)(diethoxymethyl)phosphinic acid
AKOS024456485
DTXSID70154064
J-004972
SR-01000597421-1
sr-01000597421
2BW ,
(s)-(3-aminopropyl)(diethoxymethyl)phosphinic acid
HB0955
Q5010979
phosphinic acid, p-(3-aminopropyl)-p-(diethoxymethyl)-
F81715
YEA69079
HY-103530
CS-0028030
SY325909
mfcd00882736
(3-aminopropyl)(diethoxymethyl)phos phinic acid

Research Excerpts

Treatment

ExcerptReferenceRelevance
"CGP 35348 treated females demonstrated poor exploratory behavior during open filed for several parameters (time mobile (P=0.04), time immobile (P=0.04), rotations (P=0.04), and anticlockwise rotations (P=0.038))."( Effect of GABAB receptor antagonist (CGP35348) on learning and memory in albino mice.
Akbar, A; Ali, M; Arfa, F; Gillani, Q; Iqbal, F; Iqbal, S; Khakwani, S; Ullah, A, 2014
)
1.12

Dosage Studied

ExcerptRelevanceReference
" During horizontal acceleratory/deceleratory stimulation in darkness baclofen caused a biphasic pattern in the dose-response curves."( Effects of GABAB activation and inhibition on vestibulo-ocular and optokinetic responses in the pigmented rat.
Eriksson, B; Larsby, B; Niklasson, M; Tham, R, 1994
)
0.29
" Non-REM sleep and total sleep duration increased and an s-shaped dose-response relationship was found."( Effects of the GABAB antagonist CGP 35348 on sleep-wake states, behaviour, and spike-wave discharges in old rats.
Coenen, AL; Drinkenburg, WH; Puigcerver, A; van Luijtelaar, EL, 1996
)
0.58
" The hyperpolarization was dose-dependent, and the GABA(B) receptor antagonist CGP 35,348 produced a rightward shift in the agonist dose-response curve."( A powerful GABA(B) receptor-mediated inhibition of GABAergic neurons in the arcuate nucleus.
Bosch, MA; Kelly, MJ; Rønnekleiv, K; Wagner, EJ, 1998
)
0.3
" To test the relevance of the two sets of LTP results, we performed behavioral studies examining the effect of different dosages of antagonist on spatial retention and found that memory was enhanced at intermediate dosages but not at very low and high concentrations, reminiscent of the bell-shaped dose-response curve obtained for TBS-induced LTP."( GABAB receptor antagonism: facilitatory effects on memory parallel those on LTP induced by TBS but not HFS.
Chun, D; Scafidi, J; Stäubli, U, 1999
)
0.3
" The hyperpolarization was dose dependent, and the GABA(B) receptor antagonist CGP 35,348 produced a rightward shift in the agonist dose-response curve."( A powerful GABA(B) receptor-mediated inhibition of GABAergic neurons in arcuate nucleus.
Bosch, MA; Kelly, MJ; Rønnekleiv, OK; Wagner, EJ, 1999
)
0.3
" In a first dose-response study, baclofen (0."( The GABAB receptor and recognition memory: possible modulation of its behavioral effects by the nitrergic system.
Cella, SG; Muller, EE; Pitsikas, N; Rigamonti, AE, 2003
)
0.32
" Baclofen shifted the flumazenil dose-response curve to the right and down, possibly involving perceptual masking of the discriminative stimulus effects of flumazenil by agonist activity at GABAB receptors."( Discriminative stimulus effects of flumazenil: perceptual masking by baclofen, and lack of substitution with gamma-hydroxybutyrate and its precursors 1,4-butanediol and gamma-butyrolactone.
Carter, LP; Coop, A; France, CP; Koek, W; Wu, H, 2006
)
0.33
" However, dose-response studies showed that lower doses of CGP35348 that failed to influence atypical absence seizure activity, completely reversed the spatial working memory deficit."( GABAB receptor antagonism abolishes the learning impairments in rats with chronic atypical absence seizures.
Burnham, WM; Chan, KF; Cortez, MA; Jia, Z; Snead, OC, 2006
)
0.33
" At 100 mg/kg, CGP35348 shifted the dose-response curves of baclofen and SKF97541 to the right but not those of GHB and GBL; at 320 mg/kg, CGP35348 shifted the curves of all four compounds to the right."( Cataleptic effects of gamma-hydroxybutyrate (GHB), its precursor gamma-butyrolactone (GBL), and GABAB receptor agonists in mice: differential antagonism by the GABAB receptor antagonist CGP35348.
Coop, A; Koek, W; Mercer, SL, 2007
)
0.34
" Dose-response functions determined with both training compounds revealed a clear dissociation between the discriminative stimulus effects of these drugs."( Differentiating the discriminative stimulus effects of gamma-hydroxybutyrate and ethanol in a three-choice drug discrimination procedure in rats.
Baker, LE; Poling, A; Pynnonen, DM; Searcy, GD, 2008
)
0.35
" CGP35348 shifted the dose-response curve of each agonist to the right, but the magnitude of the shift differed among the agonists."( Behavioral effects of gamma-hydroxybutyrate, its precursor gamma-butyrolactone, and GABA(B) receptor agonists: time course and differential antagonism by the GABA(B) receptor antagonist 3-aminopropyl(diethoxymethyl)phosphinic acid (CGP35348).
Coop, A; France, CP; Koek, W; Mercer, SL, 2009
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
lethal factor (plasmid)Bacillus anthracis str. A2012Potency0.12590.020010.786931.6228AID912
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid type B receptor subunit 2Rattus norvegicus (Norway rat)IC50 (µMol)27.00000.00001.01016.8100AID71394
Gamma-aminobutyric acid type B receptor subunit 1Rattus norvegicus (Norway rat)IC50 (µMol)27.00000.00001.05326.8100AID71394
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1346001Rat GABAB1 (GABAB receptors)1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists.
AID1346001Rat GABAB1 (GABAB receptors)1997Nature, Mar-20, Volume: 386, Issue:6622
Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors.
AID71394Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists.
AID175287The compound was tested for enhancement of electrically induced release of [3H]GABA from rat cortical slices.1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (364)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's215 (59.07)18.2507
2000's112 (30.77)29.6817
2010's31 (8.52)24.3611
2020's6 (1.65)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.92

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index19.92 (24.57)
Research Supply Index5.92 (2.92)
Research Growth Index4.21 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.92)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (0.54%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other371 (99.46%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]