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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]
^ 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 here for a full list): α-EMTBL
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α3IA
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PWZ-029
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Ro 15-4513
Ro 19-4603
RO4882224
RO4938581
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TB-21007
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TCS-1105
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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