baclofen

Baclofen (Lioresal) 是 γ-氨基丁酸 (GABA) 的亲脂性衍生物，是可口服的选择性代谢型 GABA-B 受体激动剂，具有高血脑屏障渗透率，用于治疗因脊髓损伤和多发性硬化引起的痉挛。

Baclofen hydrochloride (4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride) 是一种 GAMMA-AMINOBUTYRIC ACID 衍生物，是一种特异性 GABA-B 受体激动剂。它用于治疗肌肉痉挛，尤其是由于脊髓损伤引起的肌肉痉挛。其治疗效果来自于脊髓和脊髓上部位的作用，通常是减少兴奋性传递。

(S)-Baclofen has effects on excitation in the ascending auditory pathway leading to it a potential reagent for the treatment of hyperactive auditory disorders such as hyperacusis and tinnitus.

(R)-baclofen (STX209) 是一种选择性GABAB 受体激动剂。

(S)-baclofen（或称L-baclofen）作为baclofen的一个对映体，直接模拟GABA-B受体的作用。在治疗三叉神经痛方面，L-baclofen相较于racemic baclofen显示出显著的疗效提升。

Arbaclofen hydrochloride, a Gamma-Aminobutyric Acid derivative, is a specific agonist of GABA-B receptors, it is used to treat spasticity, especially that due to spinal cord damage. It acts at spinal and supraspinal sites, generally reduces excitatory tra

Baclofen-d4 是 Baclofen 的氘代化合物。Baclofen 的 CAS 号为 1134-47-0。Baclofen 是 γ-氨基丁酸 (GABA) 的亲脂性衍生物，是可口服的选择性代谢型 GABA-B 受体激动剂，具有高血脑屏障渗透率，用于治疗因脊髓损伤和多发性硬化引起的痉挛。

Arbaclofen placarbil( XP19986) is a GABA(B) receptor agonist.Arbaclofen Placarbil is a novel R-baclofen prodrug with improved absorption, distribution, metabolism, and elimination properties compared to R-baclofen. And it can reduce postprandial reflux in

Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。

Phaclofen (3-Amino-2-(4-chlorophenyl)propanephosphonic acid) 是一种选择性 GABAB receptor 拮抗剂，可部分拮抗（-）-巴氯芬的镇静作用，可逆地拮抗巴氯芬或GABA对豚鼠回肠和远端结肠胆碱能抽搐反应的抑制，可用于研究神进系统疾病。

4-Fluorophenibut (developmental code name CGP-11130; also known as β-(4-fluorophenyl)-γ-aminobutyric acid or β-(4-fluorophenyl)-GABA) is a GABAB receptor agonist which was never marketed. It is selective for the GABAB receptor over the GABAA receptor (IC50 = 1.70 μM and > 100 μM, respectively). The drug is a GABA analogue and is closely related to baclofen (β-(4-chlorophenyl)-GABA), tolibut (β-(4-methylphenyl)-GABA), and phenibut (β-phenyl-GABA). It is less potent as a GABAB receptor agonist than baclofen but more potent than phenibut.

3-Amino-3-phenylpropionic acid (DL-β-Phenylalanine) 作为一种GABA类似物，能够抑制巴氯芬诱导的胃酸分泌。