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Search Results for " gabab "

41

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11137	(E)-GABAB receptor antagonist 1	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	(E)-GABAB receptor antagonist 1 是 GABAB receptor antagonist 1 的反式结构。(E)-GABAB receptor antagonist 1 降低 GABA 诱导的 IP3 (三磷酸肌醇) 产生，IC50 为 37.9 μM。GABAB receptor antagonist 1是选择性的 GABAB (γ-氨基丁酸) 受体的负变构调节剂。
T11350	GABAB receptor antagonist 1	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	(E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.GABAB receptor antagonist 1 is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.
T21793	CGP 35348	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	CGP 35348 是 GABAB 受体的选择性拮抗剂 (EC50 = 34 μM)。 CGP 35348 可用于研究白化新生小鼠脑损伤后的神经肌肉协调和空间学习。
T4363	CGP52432 4-苄氧基苯基异硫氰酸酯,CGP 52432	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	CGP52432 是一种GABAB 受体拮抗剂，IC50值为 85 nM。
T4440	Saclofen	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Saclofen 是竞争性GABAB 受体拮抗剂(IC50:7.8 μM)。它可研究 GABAB 受体调节大脑中缓慢抑制性突触后电位的功能。
T4522	SSD114 HCl	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	SSD114 is a novel GABAB receptor positive allosteric modulator.
T38205	3-Aminopropylphosphonic Acid	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	3-Aminopropylphosphonic Acid 是与膦酸的磷相连的氢被3-氨基丙基取代的膦酸，是 GABAB 受体（GABABR）的部分激动剂和基础催乳素分泌拮抗剂。
T68087	Inaperisone	Others	Others
	Inaperisone 是一种新型的中枢作用的肌肉松弛剂，对排尿反射有抑制作用。Inaperisone 可能通过间接作用于脑干的GABAB 受体来抑制排尿反射。
T36520	COR659	Cannabinoid Receptor; GABA Receptor	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	COR659 是一种有效的 GABAB 的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。
T6355	(R)-baclofen STX209,Arbaclofen,(R)-巴氯芬	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	(R)-baclofen (STX209) 是一种选择性GABAB 受体激动剂。
T2990	Phenibut Phenybut,Fenigam,非尼布特,Fenibut,PhGABA,Aminophenylbutyric acid,β-Phenyl-γ-aminobutyric acid	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Phenibut (Aminophenylbutyric acid) 是GABA-B 激动剂，可作为 GABA 类似物，主要作用于 GABAB 受体，具有抗焦虑和增强认知的作用。
T4176	rac-BHFF (R,S)-BHFF	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	rac-BHFF ((R,S)-BHFF) 是具有口服活性的 GABAB 受体的异构增强剂，有抗焦虑活性。
T15737	Lesogaberan AZD-3355	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Lesogaberan is an effective and selective GABAB receptor agonist (EC50: 8.6 nM for human recombinant GABAB receptors). For rat brain GABAB and GABAA receptors, the binding affinity (Kis) is 5.1 nM and 1.4 μM, respectively.
T14938	CGP 36742 SGS-742	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	CGP 36742 is a selective antagonist of the GABAB receptor that can penetrate the blood-brain barrier after peripheral administration (IC50: 32 μM). It is useful in the treatment of depression.
T26995	CGP 64213 CGP-64213,CGP64213
	CGP 64213 is a GABAb receptor agonist.
T22649	CGP 46381	Others	Others
	CGP 46381 is a GABAB receptor antagonist.
T23368	SKF 97541	Others	Others
	GABAB agonist
T23147	Phaclofen	Others	Others
	GABAB antagonist
T22652	CGP 7930	Others	Others
	Positive allosteric modulator of GABAB receptors
T26992	CGP 47656 CGP47656,CGP-47656
	CGP 47656 is an agonist of GABAB receptor.
T28729	SCH-50910 free base SCH50910,SCH 50910
	SCH-50910 is an antagonist of GABAB receptor.
T26996	CGP 71872 CGP71872,CGP-71872
	CGP 71872 is an agonist of GABAB receptor.
T26994	CGP 62349 CGP-62349,CGP62349
	CGP 62349 is an antagonist of GABAB receptor.
T22651	CGP 54626 hydrochloride	Others	Others
	CGP 54626 hydrochloride is a GABAB receptor antagonist.
T26991	CGP 44532 CGP44532,CGP-44532
	CGP 44532 a GABAB receptor agonist.
T22495	2-Hydroxysaclofen	Others	Others
	2-Hydroxysaclofen is a GABAB receptor antagonist.
T23276	RuBi GABA trimethylphosphine	Others	Others
	GABAB receptor agonist
T26791	BHF-177
	BHF-177 is a positive allosteric modulator of the GABAB receptor. BHF-177 reduces self-administration of nicotine in animal studies.
T26998	CGP-54626 free base CGP54626,CGP 54626
	CGP-54626 is a selective antagonist of the GABAB receptor (IC50 = 4 nM ).
T22647	CGP 36216 hydrochloride	Others	Others
	CGP 36216 hydrochloride is a potent and selective antagonist of GABAB receptors (IC50: 43 µM).
T71911	CGP-11130 HCl
	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 t...
T39962	Valiloxibic acid XWL-008,Acidum valiloxibicum
	Valiloxibic acid is a prodrug of γ-Hydroxybutyric acid (GHB).GHB is a naturally occurring neurotransmitter and a psychoactive drug, it acts on the GHB receptor and is a weak agonist at the GABAB receptor.
T21759	CGP 55845 hydrochloride
	CGP55845 hydrochloride 是一种有效的选择性 GABAB 受体拮抗剂，IC50为 6 nM, 具有神经学研究的潜力。
T80164	α-Conotoxin PeIA
	α-Conotoxin PeIA 是一种具有镇痛作用的 α-芋螺毒素，能够抑制 α6β4、α9α10 和 α3β2 nAChR。同时，α-Conotoxin PeIA 亦作为 N 型 calcium channel 的效力抑制剂，通过激活 GABAB 受体发挥作用。
T26569	ADX71441 ADX 71441,ADX-71441
	ADX71441 is a GABAB positive allosteric modulator (PAM). ADX71441 increases urinary latencies and reduces the number of urinary events and the total and average urinary volumes. ADX71441 may also mitigate alcoholism and have analgesic effects in the bladd
T70531	CGP 55845
	CGP 55845 is a potent, selective GABAB receptor antagonist (IC50 = 5 nM) that prevents agonist binding (pKi = 8.35) and inhibits GABA and glutamate release (pEC50 values are 8.08 and 7.85 respectively).
T8639	Phenibut (hydrochloride) 3-Amino-4-phenylbutyric acid hydrochloride,3-氨基-4-苯基丁酸盐酸盐	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Phenibut hydrochloride (3-Amino-4-phenylbutyric acid hydrochloride) 是 GABA-B 激动剂，口服有活性，可作用于 GABAB 受体，充当 GABA 类似物。它具有促智 (增强认知) 及抗焦虑的能力。
T72215	Lesogaberan hydrochloride AZD-3355 hydrochloride
	Lesogaberan (AZD-3355) hydrochloride 是一种有效的选择性 GABAB 受体激动剂，对人重组 GABAB 受体的 EC50为 8.6 nM。通过脑膜中 [3H]GABA 结合位移测量，Lesogaberan hydrochloride 对大鼠 GABAB 和 GABAA 受体的亲和力 (Kis)：分别为 5.1 nM 和 1.4 μM。Lesogaberan hydrochloride 通过外周作用模式抑制短暂的食管下括约肌松弛。
T12867L	SCH 50911	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	SCH 50911 is (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid and is a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor (IC50: 1.1 μM). SCH 50911 antagonizes GABA(B) autoreceptors, increasi
T73608	Muscimol hydrochloride
	Muscimol (Agarin; Agarine) hydrochloride 是一种具有精神活性的异恶唑。Muscimol hydrochloride 也是抑制性神经递质 GABA 离子型受体的选择性激动剂。Muscimol hydrochloride 可以从毒蝇伞和相关蘑菇中分离出来。总之，Muscimol 是一种有效的 GABAA 受体激动剂 (EC50=0.2 μM)，部分 GABAC 受体激动剂和无活性的 GABAB 受体激动剂。Muscimol hydrochloride 具有镇静、抗焦虑和致幻作用。
T40572	Lesogaberan napadisylate AZD-3355 napadisylate
	Lesogaberan (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC 50 of 8.6 nM for human recombinant GABA B receptors. It demonstrates an affinity (Ki) of 5.1 nM for rat GABA B receptors and 1.4 μM for GABA A receptors, as determined by its displacement of [3H]GABA binding in brain membranes. Notably, Lesogaberan napadisylate exerts a peripheral mode of action, inhibiting transient lower esophageal sphincter relaxation.

化合物

(E)-GABAB receptor antagonist 1

Cat.No: T11137

Target: GABA Receptor

GABAB receptor antagonist 1

Cat.No: T11350

Target: GABA Receptor

Cat.No: T21793

Target: GABA Receptor

Cat.No: T4363

Synonym: 4-苄氧基苯基异硫氰酸酯,CGP 52432

Target: GABA Receptor

Cat.No: T4440

Target: GABA Receptor

Cat.No: T4522

Target: GABA Receptor

3-Aminopropylphosphonic Acid

Cat.No: T38205

Target: GABA Receptor

Cat.No: T68087

Target: Others

Cat.No: T36520

Target: Cannabinoid Receptor, GABA Receptor

Cat.No: T6355

Synonym: STX209,Arbaclofen,(R)-巴氯芬

Target: GABA Receptor

Cat.No: T2990

Synonym: Phenybut,Fenigam,非尼布特,Fenibut,PhGABA,Aminophenylbutyric acid,β-Phenyl-γ-aminobutyric acid

Target: GABA Receptor

Cat.No: T4176

Synonym: (R,S)-BHFF

Target: GABA Receptor

Cat.No: T15737

Synonym: AZD-3355

Target: GABA Receptor

Cat.No: T14938

Synonym: SGS-742

Target: GABA Receptor

Cat.No: T26995

Synonym: CGP-64213,CGP64213

Cat.No: T22649

Target: Others

Cat.No: T23368

Target: Others

Cat.No: T23147

Target: Others

Cat.No: T22652

Target: Others

Cat.No: T26992

Synonym: CGP47656,CGP-47656

SCH-50910 free base

Cat.No: T28729

Synonym: SCH50910,SCH 50910

Cat.No: T26996

Synonym: CGP71872,CGP-71872

Cat.No: T26994

Synonym: CGP-62349,CGP62349

CGP 54626 hydrochloride

Cat.No: T22651

Target: Others

Cat.No: T26991

Synonym: CGP44532,CGP-44532

2-Hydroxysaclofen

Cat.No: T22495

Target: Others

RuBi GABA trimethylphosphine

Cat.No: T23276

Target: Others

Cat.No: T26791

CGP-54626 free base

Cat.No: T26998

Synonym: CGP54626,CGP 54626

CGP 36216 hydrochloride

Cat.No: T22647

Target: Others

Cat.No: T71911

Valiloxibic acid

Cat.No: T39962

Synonym: XWL-008,Acidum valiloxibicum

CGP 55845 hydrochloride

Cat.No: T21759

α-Conotoxin PeIA

Cat.No: T80164

Cat.No: T26569

Synonym: ADX 71441,ADX-71441

Cat.No: T70531

Phenibut (hydrochloride)

Cat.No: T8639

Synonym: 3-Amino-4-phenylbutyric acid hydrochloride,3-氨基-4-苯基丁酸盐酸盐

Target: GABA Receptor

Lesogaberan hydrochloride

Cat.No: T72215

Synonym: AZD-3355 hydrochloride

Cat.No: T12867L

Target: GABA Receptor

Muscimol hydrochloride

Cat.No: T73608

Lesogaberan napadisylate

Cat.No: T40572

Synonym: AZD-3355 napadisylate

Cat. No.	Product Name	Target	Signaling Pathways
T4881	Phosphorylethanolamine O-Phosphorylethanolamine,乙醇胺磷酸酯	Others; Endogenous Metabolite	Metabolism; Others
	Phosphorylethanolamine (O-Phosphorylethanolamine) 是磷脂代谢的一种磷酸单酯代谢物。Phosphorylethanolamine 是磷脂合成的前体，也是磷脂分解的产物。与其他器官相比，大脑中磷酸单酯的含量要高得多。在大脑发育过程中，磷单酯通常在神经增生期间升高。这也与大脑发育过程中正常的程序性细胞死亡和突触修剪的发生相吻合。这些发现与磷酸单酯在膜生物合成中的作用是一致的。Phosphorylethanolamine 与抑制性神经递质GABA和GABAB受体部分激动剂 3-氨基丙基膦酸具有很强的结构相似性。Phosphorylethanolamine 是一种磷单酯，在阿尔茨海默病患者的大脑中减少。
T0508	γ-Aminobutyric acid Gamma-aminobutyric acid,4-Aminobutyric acid,4-氨基丁酸,γ-氨基丁酸,GABA,4-Aminobutanoic acid,Piperidic acid	GABA Receptor; Endogenous Metabolite	Membrane transporter/Ion channel; Metabolism; Neuroscience
	γ-Aminobutyric acid (4-Aminobutyric acid) 是成年哺乳动物大脑中主要的抑制性神经递质，能够与离子移变 GABA 受体(GABAA) 受体和促代谢受体 (GABAB) 受体结合发挥作用。

天然产物

Phosphorylethanolamine

Cat.No: T4881

Synonym: O-Phosphorylethanolamine,乙醇胺磷酸酯

Target: Others, Endogenous Metabolite

γ-Aminobutyric acid

Cat.No: T0508

Synonym: Gamma-aminobutyric acid,4-Aminobutyric acid,4-氨基丁酸,γ-氨基丁酸,GABA,4-Aminobutanoic acid,Piperidic acid

Target: GABA Receptor, Endogenous Metabolite

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