CGP-35348

CGP-35348
Identifiers
	IUPAC name 3-Aminopropyl(diethoxymethyl)phosphinic acid;
CAS Number	123690-79-9 ;
PubChem CID	107699;
IUPHAR/BPS	1069;
ChemSpider	96869 ;
CompTox Dashboard (EPA)	DTXSID70154064 ;
Chemical and physical data
Formula	C8H20NO4P
Molar mass	225.225 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCOC(OCC)P(=O)(CCCN)O;
	InChI InChI=1S/C8H20NO4P/c1-3-12-8(13-4-2)14(10,11)7-5-6-9/h8H,3-7,9H2,1-2H3,(H,10,11) ; Key:QIIVUOWTHWIXFO-UHFFFAOYSA-N ;
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CGP-35348 is a compound used in scientific research which acts as an antagonist at GABA_B 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 GABA_B 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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[pmid16647701-1] 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.

[pmid17293844-2] 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.

[pmid19564487-3] 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.

[4] Maurizio Raiteri (2006). "Functional Pharmacology in Human Brain". Pharmacological Reviews. 58 (2): 162–193. doi:10.1124/pr.58.2.5. PMID 16714485.

[5] 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)