CGP 36742
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MedKoo CAT#: 513670

CAS#: 123690-78-8 (free)

Description: 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

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

Theoretical Analysis

MedKoo Cat#: 513670
Name: CGP 36742
CAS#: 123690-78-8 (free)
Chemical Formula: C7H18NO2P
Exact Mass: 179.11
Molecular Weight: 179.200
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 2 Weeks
10mg USD 550 2 Weeks
25mg USD 1150 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:

Biological target:
In vitro activity:
In vivo activity:

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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.