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MedKoo Cat#: 513670 | Name: CGP 36742
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

CGP36742 is the first orally active GABAB-selective antagonist. CGP 36742's IC50 for blocking GABAergic transmission is 36 μM. CGP36742 in rats blocks baclofen-induced neuronal depression, and reduces learning deficit and passive avoidance in an olfactory bulbectomy depression model.

Chemical Structure

CGP 36742
CGP 36742
CAS#123690-78-8 (free)

Theoretical Analysis

MedKoo Cat#: 513670

Name: CGP 36742

CAS#: 123690-78-8 (free)

Chemical Formula: C7H18NO2P

Exact Mass: 179.1075

Molecular Weight: 179.20

Elemental Analysis: C, 46.92; H, 10.13; N, 7.82; O, 17.86; P, 17.28

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
10mg USD 625.00 2 Weeks
25mg USD 1,150.00 2 Weeks
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Related CAS #
168910-15-4 (HCl) 123690-78-8 (free)
Synonym
CGP 36742; CGP36742; CGP-36742.
IUPAC/Chemical Name
3-aminopropyl-butylphosphinic acid
InChi Key
ONNMDRQRSGKZCN-UHFFFAOYSA-N
InChi Code
InChI=1S/C7H18NO2P/c1-2-3-6-11(9,10)7-4-5-8/h2-8H2,1H3,(H,9,10)
SMILES Code
O=P(CCCC)(CCCN)O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 179.20 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Nowak G, Partyka A, Pałucha A, Szewczyk B, Wierońska JM, Dybała M, Metz M, Librowski T, Froestl W, Papp M, Pilc A. Antidepressant-like activity of CGP 36742 and CGP 51176, selective GABAB receptor antagonists, in rodents. Br J Pharmacol. 2006 Nov;149(5):581-90. PubMed PMID: 16921399; PubMed Central PMCID: PMC2014666. 2: Nyitrai G, Kékesi KA, Emri Z, Szárics E, Juhász G, Kardos J. GABA(B) receptor antagonist CGP-36742 enhances somatostatin release in the rat hippocampus in vivo and in vitro. Eur J Pharmacol. 2003 Oct 8;478(2-3):111-9. PubMed PMID: 14575795. 3: Genkova-Papazova MG, Petkova B, Shishkova N, Lazarova-Bakarova M. The GABA-B antagonist CGP 36742 prevent PTZ-kindling-provoked amnesia in rats. Eur Neuropsychopharmacol. 2000 Jul;10(4):273-8. PubMed PMID: 10871709. 4: Nyitrai G, Szárics E, Kovács I, Kékesi KA, Juhász G, Kardos J. Effect of CGP 36742 on the extracellular level of neurotransmitter amino acids in the thalamus. Neurochem Int. 1999 May;34(5):391-8. PubMed PMID: 10397367. 5: Andrén PE, Emmett MR, DaGue BB, Steulet AF, Waldmeier P, Caprioli RM. Blood-brain barrier penetration of 3-aminopropyl-n-butylphosphinic acid (CGP 36742) in rat brain by microdialysis/mass spectrometry. J Mass Spectrom. 1998 Mar;33(3):281-7. PubMed PMID: 9538527. 6: Steulet AF, Mobius HJ, Mickel SJ, Stocklin K, Waldmeier PC. Determination of rat brain and plasma levels of the orally active GABAB antagonist 3-amino-propyl-n-butyl-phosphinic acid (CGP 36742) by a new GC/MS method. Biochem Pharmacol. 1996 Mar 8;51(5):613-9. PubMed PMID: 8615897. 7: Malcangio M, Libri V, Teoh H, Constanti A, Bowery NG. Chronic (-)baclofen or CGP 36742 alters GABAB receptor sensitivity in rat brain and spinal cord. Neuroreport. 1995 Jan 26;6(2):399-403. PubMed PMID: 7538812. 8: Pratt GD, Bowery NG. Repeated administration of desipramine and a GABAB receptor antagonist, CGP 36742, discretely up-regulates GABAB receptor binding sites in rat frontal cortex. Br J Pharmacol. 1993 Oct;110(2):724-35. PubMed PMID: 8242244; PubMed Central PMCID: PMC2175914. 9: Mondadori C, Jaekel J, Preiswerk G. CGP 36742: the first orally active GABAB blocker improves the cognitive performance of mice, rats, and rhesus monkeys. Behav Neural Biol. 1993 Jul;60(1):62-8. PubMed PMID: 8216160.