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1
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10170 |
5-HT7 agonist 1
4-[4-[(2-chlorophenyl)methyl]-1-piperazinyl]-1H-indole,4-[4-[(2-chlorophenyl)methyl]piperazin-1-yl]-1H-indole,4-[4-(2-chlorobenzyl)piperazino]-1H-indole |
5-HT Receptor | GPCR/G Protein; Neuroscience |
5-HT7 agonist 1 (4-[4-[(2-chlorophenyl)methyl]piperazin-1-yl]-1H-indole)是一种5-HT7的选择性激动剂(IC50=222.93 nM)。5-HT7 agonist 1可用于有关中枢神经系统疾病的研究。 | |||
T61375 | 5-HT7 agonist 2 | ||
5-HT7 agonist 2 is a highly potent 5-HT7 receptor agonist, exhibiting an IC50 value of 28.7 nM. This compound holds promise for studying and understanding various Central Nervous System (CNS) disorders [1]. | |||
T61515 | 5-HT7 receptor ligand 1 | ||
5-HT7 receptor ligand 1 (Compound 5c) is a potent ligand for the 5-HT7 receptor, with a K i value of 8 nM. The compound demonstrates non-hepatotoxic properties and displays moderate potential for drug-drug interactions with substrates of CYP3A4 or CYP2D6 enzymes [1]. | |||
T11720 |
JNJ-18038683
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
JNJ-18038683 是 5-羟色胺受体 7 拮抗剂,HEK293 细胞中检测出其对大鼠和人类 5-羟色胺受体 7 的pKi 值分别为 8.19和8.20。 | |||
T12855 |
SB 258719
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
SB 258719 是高亲和力的、选择性的5-HT7受体拮抗剂,pKi 为7.5。SB 258719在癌症和神经系统疾病领域有研究价值。 | |||
T5387 |
LP-211
|
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
LP-211 是一种可透过血脑屏障的选择性5-HT7受体激动剂,Ki 值为 0.58 nM,选择性高于 5-HT1A 受体和 D2受体,Ki 分别为188 和 142 nM。 | |||
T6655 |
SB-269970 hydrochloride
SB-269970A,SB269970 HCl |
5-HT Receptor | GPCR/G Protein; Neuroscience |
SB-269970 hydrochloride (SB-269970A) 是 SB-269970 的盐酸盐形式,是一种 5-HT7 受体拮抗剂,pKi 值为 8.3,对其选择性比其他 5-HT 受体大于50倍多。 | |||
T21337 |
Lurasidone
SM-13496,鲁拉西酮 |
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
Lurasidone (SM-13496) 是多巴胺 D2和5-HT7的拮抗剂,IC50值分别为 1.68 和 0.495 nM。它也是5-HT1A 受体的部分激动剂,IC50值为 6.75 nM。 | |||
T26375 |
(S)-Amisulpride
Esamisulpride,(S) Amisulpride,SEP-4199,(S)-氨磺必利 |
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
(S)-Amisulpride ((S) Amisulpride) 是一种有效的多巴胺D2/D3受体拮抗剂,具有抗精神和抗抑郁作用。它是5-HT7受体的拮抗剂,KI 值为 900 nM。 | |||
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-HT6、5-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。 | |||
T26690 |
AVN-101
|
5-HT Receptor; Adrenergic Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
AVN-101 是一种非常有效的 5-HT7 受体拮抗剂 (Ki = 153 pM)。 AVN-101 还对组胺 H1 (Ki = 0.58 nM) 和肾上腺素能 α2A、α2B 和 α2C (Ki = 0.41-3.6 nM) 受体表现出相当高的亲和力。 AVN-101在中枢神经系统疾病动物模型中显示出良好的口服生物利用度和促进脑血屏障通透性、低毒性和合理的疗效。 | |||
T1735 |
Lurasidone hydrochloride
Lurasidone HCl,SM-13496 (Hydrochloride),盐酸鲁拉西酮,SM-13496 |
Dopamine Receptor; 5-HT Receptor; Norepinephrine | GPCR/G Protein; Neuroscience |
Lurasidone hydrochloride (Lurasidone HCl) 是多巴胺 D2和5-HT7的拮抗剂,IC50值分别为 1.68 和 0.495 nM,用于治疗精神分裂症和双相情感障碍。它也是5-HT1A 受体的部分激动剂,IC50值为 6.75 nM。 | |||
T14782 |
Brilaroxazine
RP5063 |
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
Brilaroxazine (RP5063) 是一种有效的多模式多巴胺/5-HT 调节剂。 Brilaroxazine 是多巴胺 D2、D3 和 D4 受体、5-HT1A (Ki = 1.5 nM) 和 5-HT2A (Ki = 2.5 nM) 的部分激动剂,具有拮抗活性 5-HT2B 和 5-HT7 受体,Ki 分别为 0.19 nM 和 2.7 nM。 Brilaroxazine 可用于研究神经精神和神经系统疾病的认知障碍。 | |||
T11326 |
Frovatriptan succinate hydrate
Frovelan,夫罗曲坦琥珀酸盐水合物 ,Frova |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Frovatriptan succinate hydrate (Frova) 是一种有效、高亲和力、选择性和口服活性的 5-HT1B、HT1D 受体激动剂和中等有效的 5-HT7 受体激动剂,pKi 值分别为 8.6、8.4 和 6.7。它可有效治疗各种偏头痛,包括恶心、呕吐、畏光和畏声等相关症状。 | |||
T24885 |
Tiospirone
BMY 13859-1 |
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
Tiospirone (BMY 13859-1) 是一种 5-HT2 受体拮抗剂,也是一种多巴胺阻滞剂, 抑制 D2,5-HT1a,5-HT7 和 sigma 受体。Tiospirone 可用于研究神经分裂等神经系统相关疾病。 | |||
T2395L |
Vortioxetine hydrobromide
氢溴酸沃替西汀,Vortioxetine (Lu AA21004) HBr,Vortioxetine HBr,盐酸沃替西汀,Lu AA21004 hydrobromide |
5-HT Receptor; Serotonin Transporter | GPCR/G Protein; Neuroscience |
Vortioxetine hydrobromide (Lu AA21004 hydrobromide) 是5-HT1A、5-HT1B、5-HT3A、5-HT7受体和5-羟色胺转运体(SERT)的抑制剂,Ki 值分别为 15、33、3.7、19 和 1.6 nM。 | |||
T2395 |
Vortioxetine
沃替西汀,Lu AA 21004 |
5-HT Receptor; Serotonin Transporter | GPCR/G Protein; Neuroscience |
Vortioxetine (Lu AA 21004) 是5-HT1A、5-HT1B、5-HT3A、5-HT7受体和 5-羟色胺转运体抑制剂,Ki 值分别为 15、33、3.7、19 和 1.6 nM。它作为抗抑郁药,用于治疗重度抑郁症。 | |||
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。 | |||
T37816 |
SB 243213
|
||
SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders[1]. SB 243213 shows little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows... | |||
T37073 |
LP 12 hydrochloride
|
||
LP 12 hydrochloride 是一种选择性的 5-HT7 受体激动剂(Ki=0.13 nM)。LP 12 hydrochloride 对 5-HT7 的选择性优于 D2、5-HT1A 和 5-HT2A 受体 (Ki 值分别为 224 nM、60.9 nM 和 >1000 nM)。 | |||
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-HT6、5-HT7和 5-HT2B 受体的 Ki 值分别为 13、168 和 245 nM。 | |||
T12842 |
SB-269970
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
SB-269970 is a antagonist of 5-HT7 receptor(pKi of 8.3). | |||
T22931 |
LP 44
|
Others | Others |
5-HT7 receptor agonist | |||
T10380 |
AS19
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
AS19 is a potent, selective 5-HT7 receptor agonist (IC50: 0.83 nM; Ki: 0.6 nM). AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis: 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). | |||
T23319 |
SB 258719 hydrochloride
|
Others | Others |
Selective 5-HT7 receptor antagonist | |||
T27207 |
DR-4004
DR4004,DR 4004 |
||
DR-4004 is a selective serotonin 5-HT7 receptor antagonist. | |||
T22750 |
DR4485 hydrochloride
DR 4485 hydrochloride |
Others | Others |
5-HT7 antagonist | |||
T22940 |
LY 215840
|
Others | Others |
5-HT2/5-HT7 receptor antagonist | |||
T62064 | PDE4B/7A-IN-2 | ||
5-HT1A/5-HT7受体拮抗剂(5-HT1A Ki=8 nM,Kb=0.04 nM;5-HT7 Ki=451 nM,Kb=460 nM)具有 PDE4B/PDE7A 抑制活性(PDE4BIC50=80.4μM;PDE7AIC50=151.3μM),其抗抑郁样作用强于作为参考活性分子的依西酞普兰。 | |||
T64269 |
LP 12 hydrochloride hydrate
|
||
LP 12 hydrochloride hydrate 是一种选择性的、有效的 5-HT7 受体激动剂 (Ki: 0.13 nM)。LP 12 hydrochloride hydrate 对 5-HT7 的选择性高于 D2 受体 (Ki: 224 nM)、5-HT1A 受体 (Ki: 60.9 nM) 和 5-HT2A 受体 (Ki>1000 nM)。 | |||
T22930 | LP 20 hydrochloride | Others | Others |
ligand of the 5-HT7 receptor | |||
T0811L |
Amisulpride hydrochloride
APD-421,Amisulpride HCl,APD 421,APD421,Sultopride,氨磺必利盐酸盐 |
||
Amisulpride is an antagonist of 5-HT7 receptor and dopamine D2 and D3 receptors. It modulates beta 2- arresting signaling and increases neurite outgrowth. | |||
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. | |||
T4375 |
Methiothepin maleate
Metitepine,甲替平 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Methiothepin maleate (Metitepine) 是一种 5-HT1、5-HT6、5-HT7 血清素受体拮抗剂,可阻断血清素自身受体。 | |||
T13308 |
Vortioxetine D8
Lu AA 21004 D8 |
Others | Others |
Vortioxetine D8 is a deuterium labeled Vortioxetine. Vortioxetine is an 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT inhibitor (Kis: 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively). | |||
T60620 | UCSF686 | ||
UCSF686 是一种 UCSF678 类似物,不具有 5-HT5A 效力,同时保留了脱靶亲和力(5-HT1A、5-HT2B 和 5-HT7)。 当使用 UCSF678 探测培养物和体内的 5-HT5A 依赖性活性时,建议将 UCSF686 作为对照化合物 [1]。 | |||
T11892 |
Lurasidone D8 Hydrochloride
SM-13496 D8 |
Others | Others |
Lurasidone D8 Hydrochloride is an inhibitor of Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C, and is the deuterium labeled Lurasidone. | |||
T37212 |
5-hydroxy-Nω-methyl Tryptamine (oxalate)
|
||
5-hydroxy-Nω-methyl Tryptamine is a metabolite of serotonin in humans that has also been found in plants. It is an agonist of the 5-HT receptor subtype 5-HT7 (IC50 = 23 pM in a radioligand binding assay). 5-hydroxy-Nω-methyl Tryptamine increases intracellular cyclic AMP production in HEK293 cells expressing 5-HT7 (EC50 = 22 nM). It inhibits serotonin uptake in HEK293 cells expressing human serotonin transporters (IC50 = 490 nM). Elevated levels of urinary 5-hydroxy-Nω-methyl tryptamine have been... | |||
T6423 |
BRL-15572 dihydrochloride
四氢罂粟碱盐酸盐,BRL 15573 dihydrochloride |
5-HT Receptor | GPCR/G Protein; Neuroscience |
BRL-15572 dihydrochloride (BRL 15573 dihydrochloride) 是一种 5-HT1D 受体拮抗剂,pKi 为 7.9,对 5-HT1A 和 5-HT2B 受体也显示出相当大的亲和力,其选择性是 5-HT1B 受体的 60 倍。 | |||
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。 | |||
T4305 |
8-OH-Dpat
8-Hydroxy-DPAT |
5-HT Receptor | GPCR/G Protein; Neuroscience |
8-OH-Dpat (8-Hydroxy-DPAT) 是选择性5-HT 激动剂,对 5-HT1A 的pIC50值为 8.19,对 5-HT7 的Ki 值为 466 nM,对 5-HT1B (pIC50, 5.42) 和 5-HT (pIC50<5) 的作用很弱。 | |||
T12899L |
SEP-363856 hydrochloride
SEP-856 hydrochloride |
Others; 5-HT Receptor | GPCR/G Protein; Neuroscience; Others |
SEP-363856 hydrochloride (SEP-856 hydrochloride) 是一种口服活性和 CNS 活性的精神药物,具有独特的非 D2/5-HT2A 作用机制,发挥其抗精神病样作用,具有治疗精神分裂症的潜力。 | |||
T0074 |
Chlorprothixene
Truxal,Clorprotixeno,Taractan,氯普噻吨 |
Dopamine Receptor; 5-HT Receptor; Antibacterial; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience |
Chlorprothixene (Truxal) 是一种多巴胺和组胺受体拮抗剂,具有抗精神病作用。它高亲和力地结合人 D1,D2,D3,D5,H1 受体,Ki 分别为 18 nM,2.96 nM,4.56 nM,9 nM 和 3.75 nM。 | |||
T6647 |
Rotigotine-
Neupro,N-0923,罗替戈汀,N-0437,SPM 962 |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Rotigotine (N-0923) 是多巴胺受体激动剂,是5-HT1A receptor 的部分激动剂,以及α2B-肾上腺素受体的拮抗剂,用于治疗帕金森病和不宁腿综合征。 | |||
T11894 |
Lusaperidone
R107474 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Lusaperidone (R107474) 是一种有效的α2肾上腺素受体 (adrenergic receptor) 拮抗剂,是 α (2)-肾上腺素受体的潜在放射性配体,对 α2A和α2C 具有抑制作用, Ki 值分别为0.13和0.15 nM。 | |||
T21446 |
Rotigotine Hydrochloride
Rotigotine (Hydrochloride),N 0923,N-0924,Rotigotine HCl,盐酸罗替戈汀,N-0923,罗替戈汀盐酸盐 |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Rotigotine Hydrochloride (N-0924) 是多巴胺受体激动剂,是5-HT1A 受体的部分激动剂,以及α2B-肾上腺素受体的拮抗剂,具有抗帕金森病活性。 | |||
T12899 |
SEP-363856
SEP-856 |
Others | Others |
SEP-363856 是一种口服活性和 CNS 活性的精神药物,具有独特的非 D2/5-HT2A 作用机制,发挥其抗精神病样作用,具有治疗精神分裂症的潜力。 | |||
T22589 | Asenapine hydrochloride | Others | Others |
Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder. | |||
T40439 |
Sarizotan
EMD 128130 |
||
Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors. It has shown potent activity with IC 50 values of 6.5 nM for rat 5-HT 1A , 0.1 nM for human 5-HT 1A , 15.1 nM for rat D 2 , 17 nM for human D 2 , 6.8 nM for human D 3 , and 2.4 nM for human D 4.2 . | |||
T22858 |
Iloperidone hydrochloride
|
Others | Others |
Iloperidone hydrochloride is a D(2)/5-HT(2) receptor antagonist. It is also an atypical antipsychotic for the treatment of schizophrenia symptoms. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 |