Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TQ0311 |
GSK163090
|
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
GSK163090 是选择性和具有口服活性的5-HT1A/1B/1D 受体拮抗剂,pKi 值分别为 9.4、8.5 和 9.7。它抑制血清素再摄取转运蛋白的功能活性,pKi 值为 6.1,具有抗抑郁和抗焦虑活性。 | |||
T8593 |
RU 24969
5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole |
5-HT Receptor | GPCR/G Protein; Neuroscience |
RU 24969 (5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole) 是 5-HT1A 和 5-HT1B 受体的选择性激动剂,Ki 值分别为 0.38 和 2.5 nM。它可减少液体消耗并增加向前运动。 | |||
T22236 |
Alprenolol hydrochloride
阿普洛尔盐酸盐,盐酸阿普洛尔 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Alprenolol hydrochloride 是一种非选择性β受体阻滞剂,也是5-HT1A 受体拮抗剂。 | |||
T8737 |
GR 125743
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
GR 125743 是选择性的5-HT1B/1D 受体拮抗剂,与野生型的人 h5-HT1B 和 5-HT1D 结合的pKi 分别为 8.85 和 8.31,可用于帕金森病和心血管疾病的研究。 | |||
T0203 |
Sumatriptan succinate
舒马普坦琥珀酸盐,GR 43175,琥珀酸舒马曲坦 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Sumatriptan succinate (GR 43175) 是一种5-HT1受体激动剂,可作用于偏头疼的急性治疗。 | |||
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。 | |||
T7498 |
Eltoprazine hydrochloride
1-(2,3-二氢苯并[B][1,4]二氧杂芑-5-基)哌嗪,DU 28853 hydrochloride |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Eltoprazine hydrochloride (DU 28853 hydrochloride) 是5-HT1A 和5-HT1B 受体激动剂,也是5-HT2C 受体拮抗剂,pEC50分别为9.96、7.19和6.81。 | |||
T11075 |
Donitriptan
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
Donitriptan 是一种 5-HT 受体激动剂,对 5-HT1B 和 5-HT1D 的 pKi 分别为 9.4 和 9.3。 | |||
T12861 |
SB-277011
SB-277011A |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
SB-277011 (SB-277011A) 是多巴胺 D3 受体的特异性拮抗剂,对 D3 受体、D2 受体、5-HT1D 和 5-HT1B 的 pKi 值分别为 8.0、6.0、5.0 和 <5.2。 | |||
T22576 |
Anpirtoline hydrochloride
|
Others | Others |
5-HT1B receptor agonist | |||
T15414 |
GR 113808
GR-113808 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
GR 113808 是一种具有选择性的 5-HT4 receptor 拮抗剂,抑制 5-HT1B,5-HT2A,5-HT2C 和 5-HT3 受体,可减弱多巴胺释放。 | |||
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。 | |||
T12841 |
SB-224289 hydrochloride
SB-224289A |
5-HT Receptor | GPCR/G Protein; Neuroscience |
SB-224289 hydrochloride (SB-224289A) 是一种选择性的 5-HT1B receptor 拮抗剂,具有抗焦虑作用。 | |||
T22808 |
GR 46611
3-[3-[2-二甲基氨基乙基]-1H-吲哚-5-基]-N-[4-甲氧基苄基]丙烯酰胺 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
GR 46611 是一种选择性 5-HT1B 和 5-HT1D 受体激动剂,可用于治疗癫痫的研究。 | |||
T12847 |
SB-616234-A
SB-616234A |
5-HT Receptor | GPCR/G Protein; Neuroscience |
SB-616234-A 是选择性的,口服有效的5-HT1B receptor 拮抗剂。SB-616234-A 具有抗焦虑和抗抑郁活性。 | |||
T21666 |
Donitriptan hydrochloride
盐酸多尼普曲坦,Donitriptan HCl,Donitriptan monohydrochloride |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Donitriptan hydrochloride (Donitriptan monohydrochloride) 是一种有效的高亲和力 5-HT1B/1D 受体激动剂,pKi 分别为 9.4 和 9.3。 | |||
T50039 |
3-(2-aminopropyl)phenol hydrochloride
|
Others | Others |
3-(2-aminopropyl)phenol hydrochloride 是一种用作分子结构单元的苯乙胺类化合物。它是一种精神活性药物,是5-HT1A、5-HT1B 和5-HT2C 等几种血清素受体的部分激动剂,也是5-HT2A 受体的拮抗剂。 | |||
T22689 |
CP94253 hydrochloride
CP 94253 hydrochloride |
Others; 5-HT Receptor | GPCR/G Protein; Neuroscience; Others |
CP94253 hydrochloride (CP 94253 hydrochloride) 是一种有效的、特异性的和中枢活性的 5-HT1B 受体激动剂,Ki 为 2 nM。5-HT1A、5-HT1D、5-HT1C 和 5-HT2 的 Ki 分别为 89、49、860 和 1600 nM 。 | |||
T0216 |
Eletriptan hydrobromide
Eletriptan HBr,UK-116044,依来曲普坦氢溴酸盐 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Eletriptan hydrobromide (Eletriptan HBr) 是一种口服活性激动剂,对 5-HT1B/1D 受体具有特异性亲和力,Ki 值分别为 0.92 和 3.14 nM。 | |||
T2317 |
Almotriptan Malate
LAS 31416,PNU180638,马来酸阿莫曲坦 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Almotriptan Malate (PNU180638) 是一种选择性 5-HT1B/1D 受体激动剂,用于治疗成人偏头痛发作。 | |||
T21231 |
Almotriptan
阿莫曲坦,LAS 31416,阿莫曲普坦 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Almotriptan (LAS 31416) 是一种用于研究偏头痛的5-HT1B/1D 受体激动剂。 | |||
T1092 |
Zolmitriptan
佐米曲普坦,311C90,BW-311C90 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Zolmitriptan (311C90) 是一种5-HT1B/1D 受体部分激动剂,可用于偏头痛的研究,对 5-HT1B、5-HT1D、5-HT1F 受体的Ki 分别为 5.01、0.63 和 63.09 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。 | |||
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。 | |||
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。 | |||
T6602 |
Naratriptan hydrochloride
Naratriptan HCl,Amerge,Naramig,盐酸那拉曲坦,GR-85548A hydrochloride |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Naratriptan hydrochloride (GR-85548A hydrochloride) 是一种5-HT1受体激动剂,有抗偏头疼特性。它还可以通过刺激三叉神经系统感觉神经末梢上的 5-HT1D/1B 受体来发挥其作用,从而减少促炎神经肽的释放。 | |||
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... | |||
T36949 |
Niaprazine
|
5-HT Receptor; Adrenergic Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Niaprazine 是有效的组胺 H1 受体拮抗剂,具有抗组胺和抗血清素活性。Niaprazine 在睡眠障碍方面有研究的价值。 | |||
T22872 |
Isamoltane hemifumarate
|
Others | Others |
5-HT1B antagonist | |||
T22653 |
CGS 12066B dimaleate
|
Others | Others |
5-HT1B full agonist | |||
T23055 |
NAS181
NAS-181 |
Others | Others |
rat 5-HT1B receptor antagonist | |||
T10360 |
AR-A 2
AR-A 000002 |
Others | Others |
AR-A 2 is a selective 5-HT1B receptor antagonist, with a high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki: 0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki: 5 nM). | |||
T23405 |
Sumatriptan
|
Others | Others |
Sumatriptan succinate is a selective 5-HT1 receptor agonist with specificity towards 5-HT1D, 5-HT1B, and 5-HT1A. | |||
T14190 |
Alniditan
Alnitidan |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Alniditan is a receptors agonist of 5-HT1B/1D in HEK 293 cells (IC50: 1.7 and 1.3 nM). For 5-HT1B/1D receptors, the pKi values are 8.96 and 9.40, respectively. | |||
T12861L |
SB-277011 dihydrochloride
SB-277011A dihydrochloride |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate antagonist of dopamine D3 receptor(pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively). | |||
T28678 |
SB 649915
SB-649915,SB649915 |
||
SB 649915 is a serotonin reuptake inhibitor and 5-HT1A and 5-HT1B receptor antagonist. | |||
T22524 |
5-Nonyloxytryptamine oxalate
|
Others | Others |
5-HT1B agonist | |||
T22809 |
GR 55562 dihydrochloride
|
Others | Others |
5-HT1B (5-HT1Dβ) silent antagonist | |||
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). | |||
T22953 |
LY 393558
|
Others | Others |
Dual 5-HT1B/1D receptor antagonist | |||
T22806 |
GR 127935 hydrochloride
|
Others | Others |
5-HT1B/1D receptor antagonist | |||
T21407 |
Frovatriptan Succinate
Frovatriptan succinate hydrate,NCGC00183880-01,Frovatriptan Succinate monohydrate,KB-295988 |
||
Frovatriptan Succinate is a synthetic triptan with 5-HT1B/1D receptors agonist activity. It is indicated for the acute treatment of migraine. | |||
T27432 |
GR-55562 dihydrobromide
GR 55562 dihydrobromide |
||
GR-55562 dihydrobromide is a antagonist of 5-HT1B/5-HT1D serotonin receptor. | |||
T27000 |
CGS-12066 maleate salt
CGS12066,CGS-12066,CGS -12066 |
||
CGS-12066 maleate salt is an agonist of 5-HT1B serotonin receptor. | |||
T24386 |
L-Alprenolol
(-)-Alprenolol,(S)-Alprenolol |
||
L-Alprenolol is a non-selective beta-blocker and a 5-HT1A and 5-HT1B receptor antagonist. | |||
T71103 |
AZD3676
|
||
AZD3676 is a novel dual antagonist of serotonin 5-HT1A and 5-HT1B receptor. | |||
T22688 |
CP 93129 dihydrochloride
|
Others | Others |
5-HT1B agonist, potent and highly selective | |||
T28677 |
SB 272183
SB-272183,SB272183 |
||
SB 272183 is a highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drug. | |||
T70559 |
GR-127935
|
||
GR-127935 is a potent and selective 5-HT1B/1D receptor antagonist. | |||
T71209 |
CGS 12066A
|
||
CGS 12066A is a drug which acts as a potent and selective agonist for the 5-HT1B receptor with lower affinity for the three 5-HT₂ receptor subtypes. It is used for studying the role of the 5-HT1B receptor in various processes including perception of pain and the sleep-wake cycle. |