Phaclofen

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Hodoodo CAT#: H329992

CAS#: 108351-35-5

Description: Phaclofen, also known as phosphonobaclofen, is a selective antagonist for the GABAB receptor.

Chemical Structure

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Phaclofen
CAS# 108351-35-5
Instruction

Theoretical Analysis

Hodoodo Cat#: H329992
Name: Phaclofen
CAS#: 108351-35-5
Chemical Formula: C9H13ClNO3P
Exact Mass: 249.03
Molecular Weight: 249.631
Elemental Analysis: C, 43.30; H, 5.25; Cl, 14.20; N, 5.61; O, 19.23; P, 12.41

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: Phaclofen; phosphonobaclofe,

IUPAC/Chemical Name: Phosphonic acid, (3-amino-2-(4-chlorophenyl)propyl)-

InChi Key: VSGNGLJPOGUDON-UHFFFAOYSA-N

InChi Code: InChI=1S/C9H13ClNO3P/c10-9-3-1-7(2-4-9)8(5-11)6-15(12,13)14/h1-4,8H,5-6,11H2,(H2,12,13,14)

SMILES Code: ClC1=CC=C(C(CN)CP(O)(O)=O)C=C1

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 249.63 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: Park SK, An SJ, Hwang IK, Kim DW, Jung JY, Won MH, Choi SY, Kwon OS, Jeong YG, Kang TC. Altered GABAB receptor immunoreactivity in the gerbil hippocampus induced by baclofen and phaclofen, not seizure activity. Neurosci Res. 2004 Aug;49(4):405-16. PubMed PMID: 15236866.

2: Wood MD, Murkitt KL, Rice SQ, Testa T, Punia PK, Stammers M, Jenkins O, Elshourbagy NA, Shabon U, Taylor SJ, Gager TL, Minton J, Hirst WD, Price GW, Pangalos M. The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen. Br J Pharmacol. 2000 Nov;131(6):1050-4. PubMed PMID: 11082110; PubMed Central PMCID: PMC1572438.

3: Kyriazi HT, Carvell GE, Brumberg JC, Simons DJ. Effects of baclofen and phaclofen on receptive field properties of rat whisker barrel neurons. Brain Res. 1996 Mar 18;712(2):325-8. PubMed PMID: 8814908.

4: Kubota K. Delayed response deficits induced by local injection of GABA antagonists (bicuculline and phaclofen) into area 46 in infant rhesus monkeys. Neurosci Res. 1996 Feb;24(3):245-63. PubMed PMID: 8815445.

5: Caddick SJ, Stanford IM, Chad JE. 2-Hydroxy-saclofen causes a phaclofen-reversible reduction in population spike amplitude in the rat hippocampal slice. Eur J Pharmacol. 1995 Feb 14;274(1-3):41-6. PubMed PMID: 7768279.

6: Frydenvang K, Hansen JJ, Krogsgaard-Larsen P, Mitrovic A, Tran H, Drew CA, Johnston GA. GABAB antagonists: resolution, absolute stereochemistry, and pharmacology of (R)- and (S)-phaclofen. Chirality. 1994;6(7):583-9. PubMed PMID: 7986672.

7: Giuliani S, Lecci A, Santicioli P, Del Bianco E, Maggi CA. Effect of the GABAB antagonist, phaclofen, on baclofen-induced inhibition of micturition reflex in urethane-anesthetized rats. Neuroscience. 1992;48(1):217-23. PubMed PMID: 1316570.

8: Hong Y, Henry JL. Phaclofen-reversible effects of GABA in the spinal cord of the rat. Eur J Pharmacol. 1991 Aug 29;201(2-3):171-7. PubMed PMID: 1665781.

9: Hong YG, Henry JL. Effects of phaclofen and the enantiomers of baclofen on cardiovascular responses to intrathecal administration of L- and D-baclofen in the rat. Eur J Pharmacol. 1991 Apr 24;196(3):267-75. PubMed PMID: 1654254.

10: Aran S, Hammond DL. Antagonism of baclofen-induced antinociception by intrathecal administration of phaclofen or 2-hydroxy-saclofen, but not delta-aminovaleric acid in the rat. J Pharmacol Exp Ther. 1991 Apr;257(1):360-8. PubMed PMID: 1850472.

11: Blandizzi C, Bernardini MC, Natale G, Del Tacca M. Phaclofen-sensitive GABA-B receptors do not mediate excitatory effects of baclofen on gastric secretion. Pharmacology. 1991;42(3):128-34. PubMed PMID: 1647534.

12: Ikeda H, Hankins MW, Kay CD. Actions of baclofen and phaclofen upon ON- and OFF-ganglion cells in the cat retina. Eur J Pharmacol. 1990 Nov 6;190(1-2):1-9. PubMed PMID: 2076748.

13: Smith RD, Turek FW, Slater NT. Bicuculline and picrotoxin block phase advances induced by GABA agonists in the circadian rhythm of locomotor activity in the golden hamster by a phaclofen-insensitive mechanism. Brain Res. 1990 Oct 22;530(2):275-82. PubMed PMID: 2265359.

14: Williams S, Lacaille JC. Bicuculline- and Phaclofen-Resistant Hyperpolarizations Evoked by Glutamate Applications to Stratum Lacunosum-Moleculare in CA1 Pyramidal Cells of the Rat Hippocampus In Vitro. Eur J Neurosci. 1990 Oct;2(11):993-1003. PubMed PMID: 12106087.

15: Drew CA, Johnston GA, Kerr DI, Ong J. Inhibition of baclofen binding to rat cerebellar membranes by phaclofen, saclofen, 3-aminopropylphosphonic acid and related GABAB receptor antagonists. Neurosci Lett. 1990 May 18;113(1):107-10. PubMed PMID: 2164173.

16: Allan RD, Drew CA, Ong J, Tran HW. Thioether analogues of baclofen, phaclofen and saclofen. Neurosci Lett. 1990 May 4;112(2-3):223-8. PubMed PMID: 2163039.

17: Mott DD, Bragdon AC, Lewis DV. Phaclofen antagonizes post-tetanic disinhibition in the rat dentate gyrus. Neurosci Lett. 1990 Mar 2;110(1-2):131-6. PubMed PMID: 2325880.

18: Wang MY, Dun NJ. Phaclofen-insensitive presynaptic inhibitory action of (+/-)-baclofen in neonatal rat motoneurones in vitro. Br J Pharmacol. 1990 Feb;99(2):413-21. PubMed PMID: 2158378; PubMed Central PMCID: PMC1917395.

19: Malouf AT, Robbins CA, Schwartzkroin PA. Phaclofen inhibition of the slow inhibitory postsynaptic potential in hippocampal slice cultures: a possible role for the GABAB-mediated inhibitory postsynaptic potential. Neuroscience. 1990;35(1):53-61. PubMed PMID: 2359496.

20: De Luca C, Massotti M. Phaclofen antagonizes the antinociceptive but not the sedative effects of (-)-baclofen. Prog Neuropsychopharmacol Biol Psychiatry. 1990;14(4):597-607. PubMed PMID: 2173023.