From Wikipedia, the free encyclopedia
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 it selective as GABAB heteroreceptor antagonist.
[4] Moreover, CGP-35348 was about threefold less potent to antagonize 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 .
^ 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 .
^ 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 . CS1 maint: multiple names: authors list (link )
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α5IA (LS-193,268)
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L-655,708
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MRK-016
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PWZ-029
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Ro 15-4513
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TB-21007
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ZK-93426
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See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators
Categories :
GABAB receptor antagonists Phosphinic acids Nervous system drug stubs Hidden categories:
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