Arbaclofen Hydrochloride - CAS 63701-55-3
Catalog number: 63701-55-3
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C10H13Cl2NO2
Molecular Weight:
250.12
COA:
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Targets:
GABA Receptor
Description:
Arbaclofen, the R-enantiomer of baclofen, is a selective gamma-amino butyric acid type B receptor agonist used for autism spectrum disorder and fragile X syndrome in randomized, double blind, placebo controlled trials.
Purity:
≥98%
Appearance:
White to off-white solid
Synonyms:
(R)-Baclofen hydrochloride; STX 209 hydrochloride; D-Baclofen hydrochloride; (3R)-4-amino-3-(4-chlorophenyl)butanoic acid;hydrochloride;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
A selective gamma-amino butyric acid type B receptor agonist used for autism spectrum disorder
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
Melting Point:
220-222 °C
InChIKey:
WMNUVYYLMCMHLU-QRPNPIFTSA-N
InChI:
1S/C10H12ClNO2.ClH/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14;/h1-4,8H,5-6,12H2,(H,13,14);1H/t8-;/m0./s1
Canonical SMILES:
C1=CC(=CC=C1C(CC(=O)O)CN)Cl.Cl
Current Developer:
Seaside Therapeutics
1.Antinociception produced by systemic R(+)-baclofen hydrochloride is attenuated by CGP 35348 administered to the spinal cord or ventromedial medulla of rats.
Thomas DA;Navarrete IM;Graham BA;McGowan MK;Hammond DL Brain Res. 1996 Apr 29;718(1-2):129-37.
This study examined the sites in the central nervous system at which subcutaneously-administered R(+)-baclofen hydrochloride (baclofen), the most active isomer of this prototypic gamma-aminobutyric acid (GABA)B receptor agonist, acts to produce antinociception in the rat. To determine whether baclofen acts in the spinal cord, either saline or the GABAB receptor antagonist CGP 35348 was injected intrathecally in rats pretreated 24 min earlier with 1 or 3 mg/kg s.c. baclofen. Intrathecal (i.t.) injection of 3 or 10 micrograms of CGP 35348 antagonized the increase in tail-flick and hot-plate latency produced by either dose of baclofen. To determine whether baclofen acts at sites in the ventromedial medulla (VMM), either saline or CGP 35348 was microinjected in the nucleus raphe magnus or nucleus reticularis gigantocellularis pars alpha of rats pretreated 24 min earlier with 1 or 3 mg/kg s.c. baclofen. Microinjection of 0.5 or 3 micrograms of CGP 35348 at sites in the VMM produced at best only a very modest attenuation of the antinociceptive effects of baclofen. These data suggest that systemically-administered baclofen acts at sites in both the spinal cord and the VMM, but that its antinociceptive effects are likely to be mediated to a greater extent by a spinal, rather than medullary site of action.
2.Transition metal-catalyzed asymmetric reactions using P-chirogenic diaminophosphine oxides: DIAPHOXs.
Nemoto T Chem Pharm Bull (Tokyo). 2008 Sep;56(9):1213-28.
This review describes the development of a new class of chiral phosphorus ligands: amino acid-derived P-chirogenic diaminophosphine oxides, DIAPHOXs, and their application to several transition metal-catalyzed asymmetric allylic substitution reactions. Pd-catalyzed asymmetric allylic alkylation with cyclic beta-keto esters as prochiral nucleophiles was initially examined using P-chirogenic diaminophosphine oxide 1a, resulting in highly enantioselective construction of quaternary stereocenters. Mechanistic investigations revealed that 1a is activated by N,O-bis(trimethylsilyl)acetamide-induced tautomerization to afford a trivalent diamidophosphite species 13, which functions as the actual ligand. Pd-catalyzed asymmetric allylic substitutions of both acyclic and cyclic substrates were also examined using various nucleophiles such as malonate derivatives, nitromethane, aliphatic amines, and aromatic amines, providing a variety of chiral compounds with good to excellent enantioselectivity. In addition, Ir-catalyzed asymmetric allylic amination and alkylation of terminal allylic carbonates were examined using structurally optimized P-chirogenic diaminophosphine oxides, and the corresponding branched products were obtained in a highly regio- and enantioselective manner.
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CAS 63701-55-3 Arbaclofen Hydrochloride

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