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53

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T61807 5-HT6/7 antagonist 1

Dopamine Receptor; 5-HT Receptor GPCR/G Protein; Neuroscience
5-HT6/7 antagonist 1是一种 5-HT6/7/2A 和 D2 受体双重拮抗剂,可用于研究痴呆和阿尔兹海默症。
T3183 SAX-187

WAY 181187,WAY181187

5-HT Receptor GPCR/G Protein; Neuroscience
SAX-187 (SAX-187) 是一种有效的选择性5-HT6受体激动剂,Ki 为 2.2 nM,EC50为 6.6 nM。它介导 5-HT6 受体依赖性信号通路,可作为特异性激动剂。
T8720 PRX-07034 hydrochloride

PRX-07034

5-HT Receptor GPCR/G Protein; Neuroscience
PRX-07034 hydrochloride 是一种有效的高度选择性5-HT6受体拮抗剂,Ki 为 4-8 nM,IC50为 19 nM,可用于增强工作记忆和认知灵活性的研究。
T30798 Cerlapirdine

PF05212365,P -05212365,SAM-531,SAM531,PF-05212365,SAM 531,WAY-262,531

5-HT Receptor GPCR/G Protein; Neuroscience
Cerlapirdine (PF-05212365) 是一种选择性 5-羟色胺 6 (5-HT6) 受体的完全拮抗剂,用于治疗与阿尔茨海默病和精神分裂症相关的认知障碍。
T79325 5-HT6 agonist 1

5-HT Receptor GPCR/G Protein; Neuroscience
5-HT6 agonist 1 (Compound 19)为一种5-HT6激动剂 (Ki: 5 nM),展现出抗抑郁样特性并能改善认知缺陷,同时能抑制血小板聚集,具备高代谢稳定性。
T61837 5-HT6/5-HT2AR antagonist-1

5-HT6/5-HT2AR antagonist-1 is a powerful and effective compound that acts as a dual antagonist for both the 5-HT6 and 5-HT2A receptors. It exhibits high potency with K i values of 11 nM and 39 nM for the respective receptors [1].
T61207 5-HT6/5-HT2A receptor ligand-1

5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual antagonist for the 5-HT6 and 5-HT2A receptors. It exhibits a K i value of 2 nM and 11 nM for the respective receptors. This compound holds promise for research in neurological and psychiatric disorders [1].
T61220 5-HT6/5-HT2A receptor ligand-2

5-HT6/5-HT2A receptor ligand-2 (化合物 42) 是一种可透过血脑屏障的5-HT6/5-HT2A 的双拮抗剂 ,Ki 值分别为 25 nM 和 32 nM。5-HT6/5-HT2A receptor ligand-2 具有促认知特性。
T13007 ST1936 oxalate

5-HT Receptor GPCR/G Protein; Neuroscience
ST1936 oxalate 是一种 5-HT6 受体的选择性纳摩尔亲和激动剂,对人5-HT65-HT7和 5-HT2B 受体的 Ki 值分别为 13、168 和 245 nM。
T4118 SB 271046 hydrochloride

SB 271046A

5-HT Receptor GPCR/G Protein; Neuroscience
SB 271046 hydrochloride (SB 271046A) 是高效、选择性和具有口服活性的5-HT6受体拮抗剂,对大鼠、猪和人的pKi 分别为 9.02、8.55 和 8.81。它增加额叶皮层中的细胞外天冬氨酸和谷氨酸并表现出抗惊厥活性,EC50为 0.16 μM。它对 5-HT6 受体、结合位点和离子通道的选择性超过 200 倍。
T11948 Masupirdine free base

Masupirdine,SUVN-502 free base

5-HT Receptor GPCR/G Protein; Neuroscience
Masupirdine free base(SUVN-502 free base)是一种可口服且可穿过血脑屏障的 5-HT6 受体拮抗剂,对人类 5-HT6 受体的 Ki 值为 2.04 nM。Masupirdine free base 具有高效性和选择性且对多种靶点都具有抑制作用。Masupirdine free base 可用于研究像阿尔茨海默病类的神经系统疾病。
T10053 5HT6-ligand-1

5-HT Receptor GPCR/G Protein; Neuroscience
5HT6-ligand-1 是一种具有口服活性的 5-HT6 受体配体 (Ki = 1.43 nM)。
T1774 Intepirdine

RVT-101,SB 742457,GSK-742457

5-HT Receptor GPCR/G Protein; Neuroscience
Intepirdine (GSK-742457) 是5-HT6受体拮抗剂,pKi 为9.63,用于研究阿尔茨海默病治疗的试验。
T7103 idalopirdine

Lu AE58054

5-HT Receptor GPCR/G Protein; Neuroscience
Idalopirdine (Lu AE58054) 是一种选择性的5-HT6 受体拮抗剂,Ki 为 0.83 nM。
T11949 Masupirdine mesylate

SUVN-502 mesylate,SVN-502 mesylate

5-HT Receptor GPCR/G Protein; Neuroscience
Masupirdine mesylate (SUVN-502 mesylate) 是一种具有选择性且可穿越血脑屏障的 5-HT6 受体拮抗剂。Masupirdine mesylate 可用于研究阿尔茨海默病和痴呆等神经系统疾病。
T11183 EMDT

5-HT Receptor GPCR/G Protein; Neuroscience
EMDT是一种选择性 5-HT6 激动剂,具有抗抑郁作用。
T23396 ST1936

ST 1936 oxalate

5-HT Receptor GPCR/G Protein; Neuroscience
ST1936 (ST 1936 oxalate) 是一种具有选择性和高效性的 5-HT6 受体激动剂,抑制人 5-HT65-HT7 和 5-HT2B 受体,通过完全激活克隆的人 5-HT6 受体来刺激 cAMP、Ca2+、ERK1/2 和 Fyn 激酶。
T26085 rilapine

Rilapinum

Rilapine is an atypical antipsychotic with high affinity for the 5-HT6 receptor.
T23318L SB 258585

5-HT Receptor GPCR/G Protein; Neuroscience
SB 258585 是一种选择性 5-HT6受体拮抗剂。SB 258585 对人重组5-HT6受体的细胞系中的单个受体群体亲和力很高。SB 258585 可用于标记重组和天然5-HT6受体,可用于检测认知增强和抗精神病活性。
T12262L1 NPS ALX Compound 4a hydrochloride(1:1)

5-HT Receptor GPCR/G Protein; Neuroscience
NPS ALX Compound 4a hydrochloride(1:1)是一种有效、选择性的 5-羟色胺受体 6 (5-HT6) 受体拮抗剂,IC50 值为 7.2 nM,且具有高亲和力,Ki 值为 0.2 nM。
T22936 Idalopirdine Hydrochloride

Lu AE58054盐酸盐,Lu AE58054 Hydrochloride,Idalopirdine HCl

5-HT Receptor GPCR/G Protein; Neuroscience
Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) 是一种选择性的5-HT6 受体拮抗剂,Ki 为 0.83 nM。
T31592 E6801

E 6801,E-6801

5-HT Receptor GPCR/G Protein; Neuroscience
E6801是一种新型选择性5-HT6受体激动剂,具有广泛的生物活性。E6801可用于研究痴呆、帕金森病、抑郁症、肥胖症癫痫,焦虑等多种疾病。
T50090 3-(2-phenylethynyl)pyridine

Others Others
3-(2-phenylethynyl)pyridine 是一种吡啶衍生物,是人体中各种受体的配体,包括多巴胺 D2受体、sigma-1受体和5-HT6受体,已被研究用于治疗各种神经疾病,包括精神分裂症、抑郁症和阿尔茨海默病。
T12262 NPS ALX Compound 4a

5-HT Receptor GPCR/G Protein; Neuroscience
NPS ALX Compound 4a is a potent and selective antagonist of 5-HT6 receptor (IC50 of 7.2 nM)
T12262L NPS ALX Compound 4a dihydrochloride

5-HT Receptor GPCR/G Protein; Neuroscience
NPS ALX Compound 4a dihydrochloride is a potent and selective antagonist of 5-HT6 receptor (IC50 of 7.2 nM)
T12843 SB-399885 hydrochloride

5-HT Receptor GPCR/G Protein; Neuroscience
SB-399885 hydrochloride is an antagonist of 5-HT6 receptor.
T23029 MS 245 oxalate

Others Others
MS 245 oxalate is a 5-HT6 antagonist.
T23318 SB 258585 hydrochloride

Others Others
SB 258585 hydrochloride is a 5-HT6 receptor antagonist.
T23527 WAY208466 dihydrochloride

WAY 208466 dihydrochloride

Others Others
5-HT6 agonist
T62082 FPPQ

FPPQ 是一种 5-HT3 和 5-HT6 受体的双重拮抗剂,他们的 Ki 值分别为 0.9 nM 和 3 nM,表现出抗精神病和促认知活性。
T23350 SGS518 oxalate

SGS 518 oxalate

Others Others
SGS518 oxalate is a 5-HT6 antagonist.
T24716 Ro 04-6790 dihydrochloride

Ro 04-6790 dihydrochloride is an effective and selective antagonist of the serotonin 5-HT6 receptor.
T23240 Ro 04-6790

Others Others
Ro 04-6790 is a 5-HT6 receptor antagonist.
T22763 EMD 386088 hydrochloride

Others Others
EMD 386088 hydrochloride is a 5-HT6 receptor agonist.
T28768 SGS-518

SGS518,LY-483518,LY 483518,LY483518

SGS-518 is a selective antagonist of the 5-HT6 receptor.
T83289 5-HT6R antagonist 2

5-HT6R antagonist 2 (compound 29)为高选择性5-HT6受体拮抗剂,具备潜在的中枢神经系统(CNS)治疗应用。
T28594 Ro 63-0563

Ro-63-0563,Ro63-0563

Ro 63-0563 is a potent, 5-HT6 receptors selective antagonist.
T30230 AVN-211

CD-008-0173,AVN 211

AVN-211 (CD-008-0173) is a novel and highly selective 5-HT6 receptor small molecule antagonist for the treatment of Alzheimer's disease.
T23214 R 1485 dihydrochloride

Others Others
5-HT6 antagonist,selective and high affinity
T26691 AVN-322

AVN 322

AVN-322 is a 5-HT6 receptor antagonist. 5-HT6R antagonists improves cognition in animal models of cognitive impairment.
T4375 Methiothepin maleate

Metitepine,甲替平

5-HT Receptor GPCR/G Protein; Neuroscience
Methiothepin maleate (Metitepine) 是一种 5-HT1、5-HT65-HT7 血清素受体拮抗剂,可阻断血清素自身受体。
T27455 GSK-215083

GSK215083

GSK-215083 is a PET radioligand for the 5-HT6 receptor. GSK 215083 is a quinoline based compounds and acts by antagonising the 5-HT6 receptor. GSK-215083 binds to receptors 5-hydroxytrypamine-6 (5HT6) in the striatum and 5-hydroxytryptamine-2A (5HT2A) in
T28689 SB357134

SB-357134,SB 357134

SB357134 is a potent, selective and orally active antagonist of 5-HT6 receptor and shows nootropic effects in animal studies.
T68353 BVT-74316

BVT-74316 is an orally administered antagonist of the serotonin 6 receptor (5-HT6) being developed by Proximagen
T71593 AVN-101 free base

AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a multi-target drug candidate for the treatment of CNS disorders.
T63038 WAY-181187 oxalate

WAY-181187 (SAX-187) oxalate 是一种选择性的、有效的 5-HT6 受体的激动剂 (Ki: 2.2 nM; EC50: 6.6 nM)。WAY-181187 oxalate 是一种特异性激动剂,介导 5-HT6 受体依赖性信号通路(如 cAMP,Fyn 和 ERK1/2 激酶)。
T22044 BGC 20-761

BGC20-761 是一种选择性的5-HT6和多巴胺受体 (dopamine receptor) 拮抗剂,对人 5-HT65-HT2A,D2 受体的Ki 值分别为 20,69,和 140 nM。BGC20-761 可增强长期记忆。BGC20-761 具有作为抗精神病药物的潜在效用。
T78648 MAO-B-IN-3

Monoamine Oxidase Neuroscience
MAO-B-IN-3是一种选择性MAO-B抑制剂,具有可逆性,IC50为96 nM。该化合物还可与5-HT6R结合,Ki值为696 nM,适用于阿尔茨海默病研究。
T1951 Asenapine Maleate

Org 5222 maleate,Org 5222,马来酸阿塞那平,阿塞那平马来酸盐

5-HT Receptor GPCR/G Protein; Neuroscience
Asenapine Maleate (Org 5222 maleate) 是5-HT 和D2的拮抗剂,Ki 值分别为 0.03-4.0 nM, 1.3 nM。它也是抗精神病药物,用于治疗与双相 1 型障碍相关的精神分裂症和躁狂或混合发作。
T69104 SAX-187 hydrochloride

SAX-187 hydrochloride is a potent and selective 5-HT6 receptor agonist. SAX-187 hydrochloride possesses high affinity binding (2.2 and 4.8 nM, respectively) at the human 5-HT6 receptor and profile as full receptor agonists (SAX-187 hydrochloride: EC50=6.6 nM, Emax=93%). In the rat frontal cortex, acute administration of SAX-187 hydrochloride (3-30 mg/kg, subcutaneous (s.c.)) significantly increased extracellular GABA concentrations without altering the levels of glutamate or norepinephrine.

化合物

5-HT6/7 antagonist 1
Cat.No: T61807
Synonym:
Target: Dopamine Receptor, 5-HT Receptor
SAX-187
Cat.No: T3183
Synonym: WAY 181187,WAY181187
Target: 5-HT Receptor
PRX-07034 hydrochloride
Cat.No: T8720
Synonym: PRX-07034
Target: 5-HT Receptor
Cerlapirdine
Cat.No: T30798
Synonym: PF05212365,P -05212365,SAM-531,SAM531,PF-05212365,SAM 531,WAY-262,531
Target: 5-HT Receptor
5-HT6 agonist 1
Cat.No: T79325
Synonym:
Target: 5-HT Receptor
5-HT6/5-HT2AR antagonist-1
Cat.No: T61837
Synonym:
Target:
5-HT6/5-HT2A receptor ligand-1
Cat.No: T61207
Synonym:
Target:
5-HT6/5-HT2A receptor ligand-2
Cat.No: T61220
Synonym:
Target:
ST1936 oxalate
Cat.No: T13007
Synonym:
Target: 5-HT Receptor
SB 271046 hydrochloride
Cat.No: T4118
Synonym: SB 271046A
Target: 5-HT Receptor
Masupirdine free base
Cat.No: T11948
Synonym: Masupirdine,SUVN-502 free base
Target: 5-HT Receptor
5HT6-ligand-1
Cat.No: T10053
Synonym:
Target: 5-HT Receptor
Intepirdine
Cat.No: T1774
Synonym: RVT-101,SB 742457,GSK-742457
Target: 5-HT Receptor
idalopirdine
Cat.No: T7103
Synonym: Lu AE58054
Target: 5-HT Receptor
Masupirdine mesylate
Cat.No: T11949
Synonym: SUVN-502 mesylate,SVN-502 mesylate
Target: 5-HT Receptor
EMDT
Cat.No: T11183
Synonym:
Target: 5-HT Receptor
ST1936
Cat.No: T23396
Synonym: ST 1936 oxalate
Target: 5-HT Receptor
rilapine
Cat.No: T26085
Synonym: Rilapinum
Target:
SB 258585
Cat.No: T23318L
Synonym:
Target: 5-HT Receptor
NPS ALX Compound 4a hydrochloride(1:1)
Cat.No: T12262L1
Synonym:
Target: 5-HT Receptor
Idalopirdine Hydrochloride
Cat.No: T22936
Synonym: Lu AE58054盐酸盐,Lu AE58054 Hydrochloride,Idalopirdine HCl
Target: 5-HT Receptor
E6801
Cat.No: T31592
Synonym: E 6801,E-6801
Target: 5-HT Receptor
3-(2-phenylethynyl)pyridine
Cat.No: T50090
Synonym:
Target: Others
NPS ALX Compound 4a
Cat.No: T12262
Synonym:
Target: 5-HT Receptor
NPS ALX Compound 4a dihydrochloride
Cat.No: T12262L
Synonym:
Target: 5-HT Receptor
SB-399885 hydrochloride
Cat.No: T12843
Synonym:
Target: 5-HT Receptor
MS 245 oxalate
Cat.No: T23029
Synonym:
Target: Others
SB 258585 hydrochloride
Cat.No: T23318
Synonym:
Target: Others
WAY208466 dihydrochloride
Cat.No: T23527
Synonym: WAY 208466 dihydrochloride
Target: Others
FPPQ
Cat.No: T62082
Synonym:
Target:
SGS518 oxalate
Cat.No: T23350
Synonym: SGS 518 oxalate
Target: Others
Ro 04-6790 dihydrochloride
Cat.No: T24716
Synonym:
Target:
Ro 04-6790
Cat.No: T23240
Synonym:
Target: Others
EMD 386088 hydrochloride
Cat.No: T22763
Synonym:
Target: Others
SGS-518
Cat.No: T28768
Synonym: SGS518,LY-483518,LY 483518,LY483518
Target:
5-HT6R antagonist 2
Cat.No: T83289
Synonym:
Target:
Ro 63-0563
Cat.No: T28594
Synonym: Ro-63-0563,Ro63-0563
Target:
AVN-211
Cat.No: T30230
Synonym: CD-008-0173,AVN 211
Target:
R 1485 dihydrochloride
Cat.No: T23214
Synonym:
Target: Others
AVN-322
Cat.No: T26691
Synonym: AVN 322
Target:
Methiothepin maleate
Cat.No: T4375
Synonym: Metitepine,甲替平
Target: 5-HT Receptor
GSK-215083
Cat.No: T27455
Synonym: GSK215083
Target:
SB357134
Cat.No: T28689
Synonym: SB-357134,SB 357134
Target:
BVT-74316
Cat.No: T68353
Synonym:
Target:
AVN-101 free base
Cat.No: T71593
Synonym:
Target:
WAY-181187 oxalate
Cat.No: T63038
Synonym:
Target:
BGC 20-761
Cat.No: T22044
Synonym:
Target:
MAO-B-IN-3
Cat.No: T78648
Synonym:
Target: Monoamine Oxidase
Asenapine Maleate
Cat.No: T1951
Synonym: Org 5222 maleate,Org 5222,马来酸阿塞那平,阿塞那平马来酸盐
Target: 5-HT Receptor
SAX-187 hydrochloride
Cat.No: T69104
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T21499 Dimebolin

Latrepirdine,Dimebon,Dimebone

5-HT Receptor GPCR/G Protein; Neuroscience
Dimebolin (Latrepirdine) 是一种 5-HT6 拮抗剂。
T3369 Nuciferine

(-)-Nuciferine,VLT 049,荷叶碱,Sanjoinine E

Dopamine Receptor; 5-HT Receptor GPCR/G Protein; Neuroscience
Nuciferine ((-)-Nuciferine) 是一种在埃及蓝睡莲和水芙蓉中发现的生物碱,是5-HT2A、5-HT2B 和5-HT2C 拮抗剂,IC50分别为 478 nM、1 μM 和 131 nM。它也是5-HT7的反向激动剂,IC50为 150 nM。

天然产物

Dimebolin
Cat.No: T21499
Synonym: Latrepirdine,Dimebon,Dimebone
Target: 5-HT Receptor
Nuciferine
Cat.No: T3369
Synonym: (-)-Nuciferine,VLT 049,荷叶碱,Sanjoinine E
Target: Dopamine Receptor, 5-HT Receptor
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