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Merck
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文件

G013

Sigma-Aldrich

R (+)-巴氯芬 盐酸盐

solid

别名:

R(+)-β-（氨甲基）-4-氯苯丙酸 盐酸盐, STX209, 巴氯芬 盐酸盐

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About This Item

经验公式（希尔记法）:
C10H12ClNO2 · HCl
CAS号:
63701-55-3
分子量:
250.12
MDL號碼:
MFCD00078579
分類程式碼代碼:
12352200
PubChem物質ID:
24895006
NACRES:
NA.32

形狀

solid

品質等級

100

光學活性

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

儲存條件

desiccated

顏色

white

溶解度

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

SMILES 字串

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

InChI 密鑰

WMNUVYYLMCMHLU-QRPNPIFTSA-N

基因資訊

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

應用

R(+)-盐酸巴氯芬已用作GABAB受体激动剂，以研究其对大鼠模型中M43068诱导的镇痛作用的影响。它还被用作GABAB受体激动剂，以研究其对鼠纹状体中安非他命诱导的行为和神经化学反应的影响。

生化／生理作用

巴氯芬是一种γ-氨基丁酸（GABA）的衍生物，可用作4-氨基丁酸受体（GABAB）激动剂。它与GABA受体立体定向相互作用并表现出抗痉挛作用。巴氯芬对三叉神经痛和脊柱痉挛的阵发性疼痛有治疗作用。R(+)-巴氯芬是一种活性更强的对映体。

其他說明

对映异构体与 R（−）-巴氯芬游离碱相同。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)

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Xia Li et al.
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)
Yuriko Watanabe et al.
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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