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Key Documents

G013

Sigma-Aldrich

R(+)-Baclofen hydrochloride

solid

Sinonimo/i:

Arbaclofen hydrochloride, R(+)-β-(Aminomethyl)-4-chlorobenzenepropanoic acid hydrochloride, STX209

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About This Item

Formula empirica (notazione di Hill):
C10H12ClNO2 · HCl
Numero CAS:
Peso molecolare:
250.12
Numero MDL:
Codice UNSPSC:
12352200
ID PubChem:
NACRES:
NA.32

Forma fisica

solid

Livello qualitativo

Attività ottica

[α]28/D +3.8°, c = 0.9 in methanol(lit.)

Condizioni di stoccaggio

desiccated

Colore

white

Solubilità

DMSO: >20 mg/mL
H2O: 26 mg/mL (Solutions may be stored for several weeks at 4 °C.)

Stringa SMILE

Cl[H].NC[C@H](CC(O)=O)c1ccc(Cl)cc1

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
WMNUVYYLMCMHLU-QRPNPIFTSA-N

Informazioni sul gene

human ... GABBR1(2550)
mouse ... GABBR1(54393)
rat ... GABBR1(81657)

Applicazioni

R(+)-Baclofen hydrochloride has been used as a GABAB receptor agonist to study its effects on M43068-induced antinociception in rat models. It has also been used as a GABAB receptor agonist to study its effects on amphetamine-induced behavior and neurochemical responses in rat striatum.

Azioni biochim/fisiol

Baclofen is a derivative of γ-aminobutyric acid (GABA) and acts as a 4-aminobutanoic acid receptor (GABAB) agonist. It interacts stereospecifically with the GABA receptor and exhibits antispastic effects.Baclofen shows therapeutic effects against paroxysmal pain of trigeminal neuralgia and spinal spasticity. R(+)-Baclofen is a more active enantiomer.

Altre note

Same enantiomer as R(−)-baclofen free base.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Dispositivi di protezione individuale

Eyeshields, Gloves, type N95 (US)


Certificati d'analisi (COA)

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Neuropharmacology, 97, 357-364 (2015-05-24)
GABAB (γ-aminobutyric acid B) receptors may be a therapeutic target for anxiety disorders. Here we characterized the effects of the GABAB receptor positive allosteric modulator (PAM) BHF177 on conditioned and unconditioned physiological responses to threat in the light-enhanced startle (LES)
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European journal of pharmacology, 837, 88-95 (2018-08-08)
The nucleus accumbens contains delta-opioid receptors that may decrease inhibitory neurotransmission. As GABAB receptors inhibit dopamine release, decrease in activation of GABAB receptors may be a mediator of delta-opioid receptor-induced accumbal dopamine efflux. If so, accumbal dopamine efflux induced by
Synthesis of both enantiomers of baclofen using (R)-and (S)-N-phenylpantolactam as chiral auxiliaries
Camps P, et al.
Tetrahedron Asymmetry, 15(13) (2004)
Reagan L Pennock et al.
The Journal of physiology, 592(19), 4247-4256 (2014-08-03)
It has recently been shown that dynorphin A (Dyn A), an endogenous agonist of the κ-opioid receptor (KOR), directly inhibits proopiomelanocortin (POMC) neurons in the hypothalamus through activation of G-protein-coupled inwardly rectifying K(+) channels (GIRKs). This effect has been proposed
Y G Hong et al.
European journal of pharmacology, 196(3), 267-275 (1991-04-24)
In a previous study it was found that i.t. administration of L-baclofen decreased arterial pressure and heart rate while D-baclofen differentially increased arterial pressure. The objective of the present study was to determine which of these effects was blocked by

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