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Chemical compound
CGP-35348 is a compound used in scientific research which acts as an
antagonist at
GABAB
receptors .
[1]
[2]
[3]
CGP-35348 was ineffective up to 100 μM to antagonize the inhibitory release of GABA elicited by baclofen, doing so selectively as a
GABAB heteroreceptor antagonist.
[4] Moreover, CGP-35348 was about threefold less potent in antagonizing
gamma-hydroxybutyrate (GHB) and
gamma-butyrolactone (GBL) than
baclofen and
SKF-97,541 .
[5]
References
^ Carter LP, Chen W, Coop A, Koek W, France CP (May 2006). "Discriminative stimulus effects of GHB and GABA(B) agonists are differentially attenuated by CGP35348". European Journal of Pharmacology . 538 (1–3): 85–93.
doi :
10.1016/j.ejphar.2006.03.039 .
PMID
16647701 .
^ Nasrallah FA, Griffin JL, Balcar VJ, Rae C (August 2007). "Understanding your inhibitions: modulation of brain cortical metabolism by GABA(B) receptors". Journal of Cerebral Blood Flow and Metabolism . 27 (8): 1510–20.
doi :
10.1038/sj.jcbfm.9600453 .
PMID
17293844 .
S2CID
16069846 .
^ Koek W, Mercer SL, Coop A, France CP (September 2009).
"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)" . The Journal of Pharmacology and Experimental Therapeutics . 330 (3): 876–83.
doi :
10.1124/jpet.109.151845 .
PMC
2729800 .
PMID
19564487 .
^ Maurizio Raiteri (2006). "Functional Pharmacology in Human Brain". Pharmacological Reviews . 58 (2): 162–193.
doi :
10.1124/pr.58.2.5 .
PMID
16714485 .
S2CID
14404544 .
^ Koek W1, Mercer SL, Coop A. (June 2007). "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". Psychopharmacology . 192 (3): 407–14.
doi :
10.1007/s00213-007-0718-y .
PMID
17277933 .
S2CID
25049526 . {{
cite journal }}
: CS1 maint: multiple names: authors list (
link ) CS1 maint: numeric names: authors list (
link )
Ionotropic
GABAA Tooltip γ-Aminobutyric acid A receptor
Positive modulators (abridged; see
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α-EMTBL
Alcohols (e.g.,
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2M2B )
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Negative modulators:
1,3M1B
3M2B
11-Ketoprogesterone
17-Phenylandrostenol
α3IA
α5IA (LS-193,268)
β-CCB
β-CCE
β-CCM
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L-655,708
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Oenanthotoxin
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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
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TETS
Thujone
U-93631
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ZK-93426
GABAA -ρ Tooltip γ-Aminobutyric acid A-rho receptor
Metabotropic
GABAB Tooltip γ-Aminobutyric acid B receptor