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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T2688 |
LY310762
LY310762 HCl |
5-HT Receptor | GPCR/G Protein; Neuroscience |
LY310762 是 5-HT1D 受体拮抗剂,Ki 为 249 nM。 | |||
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。 | |||
T5858 |
Sertindole
Lu 23-174,舍吲哚 |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Autophagy | Autophagy; GPCR/G Protein; Neuroscience |
Sertindole (Lu 23-174) 是一种非典型抗精神病药,可与多巴胺 D2 受体和血清素受体亚型 5-HT1D、5-HT2A 和 5-HT2C 结合,Kd 值分别为 2.7、20、0.14 和 6 nM。 | |||
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。 | |||
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。 | |||
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 。 | |||
T34081 |
Piromelatine
NEU-P-11,NEU-P 11,NEU-P11 |
P2X Receptor; 5-HT Receptor; MT Receptor; Sodium Channel; TRP/TRPV Channel | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
Piromelatine 是褪黑激素 MT1/MT2 受体、5-HT1A 和 5-HT1D 的激动剂,也是 5-HT2B 的拮抗剂。Piromelatine 具有抗痛觉活性,对 P2X3、TRPV1 和 Nav1.7 通道有抑制作用,可用于促进睡眠、缓解疼痛、抗神经退行性疾病和抗抑郁疾病的研究。 | |||
T23265 |
RS 67333 hydrochloride
RS 67333 (hydrochloride),RS 67333 HCl,盐酸RS67333 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
RS 67333 hydrochloride (RO5203648) 是一种有效的、选择性的5-HT4 受体 (5-HT4R) 部分激动剂,在豚鼠纹状体中的 pKi 为 8.7。RS 67333 hydrochloride 对其他几种受体的亲和力较低,包括 5-HT1A、5-HT1D、5-HT2A、5-HT2C、多巴胺 D1、D2 和毒蕈碱 M1-M3 受体。RS 67333 hydrochloride 具有神经保护作用,可用于阿尔茨海默病研究。 | |||
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。 | |||
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。 | |||
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... | |||
T16556 |
PNU-142633
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
PNU-142633 has anti-migraine efficacy. PNU-142633 is a high affinity and selective 5-HT1D receptor agonist (Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively). | |||
T26598 | Alniditan dihydrochloride | ||
Alniditan dihydrochloride is a potent 5-HT1D agonist and migraine-abortive agent. | |||
T23405 |
Sumatriptan
|
Others | Others |
Sumatriptan succinate is a selective 5-HT1 receptor agonist with specificity towards 5-HT1D, 5-HT1B, and 5-HT1A. | |||
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). | |||
T27628 |
IS-159
IS 159,IS159 |
||
IS-159, a 5-HT1D agonist, is used potentially for the treatment of migraine. | |||
T28679 |
SB 714786
SB-714786,SB714786 |
||
SB 714786 is a selective antagonist of 5-HT1D. | |||
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). | |||
T22681 |
CP 135807
|
Others | Others |
CP 135807 is a 5-HT1D receptor agonist. | |||
T22901 |
L-703,664 succinate
|
Others | Others |
L-703,664 succinate is a 5-HT1D receptor agonist. | |||
T27432 |
GR-55562 dihydrobromide
GR 55562 dihydrobromide |
||
GR-55562 dihydrobromide is a antagonist of 5-HT1B/5-HT1D serotonin receptor. | |||
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). | |||
T27879 |
LY 165163
LY-165,163,LY165,163,LY 165,163 |
||
LY-165163 is a selective antagonists of 5-HT1A and 5-HT1D serotonin receptor. | |||
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。 | |||
T19701 |
L-694,247
|
||
L-694,247 is a selective and extremely potent agonist of the 5-HT1D receptor. | |||
T31617 |
Elzasonan citrate
|
||
Elzasonan Citrate is a selective 5-HT1B and 5-HT1D receptor antagonist for the treatment of depression. | |||
T28431 |
PNU109291
PNU-109291,PNU 109291 |
||
PNU109291, a potent and selective agonist of the 5-HT1D receptor, effectively mitigates dural plasma extravasation induced by trigeminal ganglion stimulation. | |||
T27059 |
CP-122288
|
||
CP-122288 is a potent and selective agonist for the 5-HT1B, 5-HT1D and 5-HT1F serotonin receptor subtypes. CP-122288 is potent as an inhibitor of plasma protein extravasation and neurogenic inflammation. | |||
T19690 |
SB 224289
SB224289,SB-224289 |
||
SB 224289 is a selective antagonist of 5-HT1B receptor with pKi of 8.2. It is a centrally active following oral administration in vivo. SB 224289 displays 60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand | |||
T35104 |
Way 100135
Way-100135,Way100135 |
||
Way 100135 is a serotonergic drug of the phenylpiperazine family which is used in scientific research. It acts as a potent 5-HT1A receptor antagonist and a partial agonist of the 5-HT1D receptor, and to a much lesser extent, of the 5-HT1B receptor. | |||
T36063 |
N-desmethyl Zolmitriptan
|
||
N-desmethyl Zolmitriptan (DZT) is an active metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist zolmitriptan . DZT is an agonist of 5-HT1B receptors that induces contraction of isolated human cerebral arteries (EC50 = 100 nM). | |||
T2459 |
BRL 54443
BRL54443 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
BRL 54443 是一种有效的 5-HT1E/1F 受体激动剂,pKi 值分别为 8.7 和 8.9。 | |||
T71211 |
Rizatriptan-d6 benzoate salt
|
||
Rizatriptan-d6 is intended for use as an internal standard for the quantification of rizatriptan by GC- or LC-MS. Rizatriptan is an agonist of the serotonin receptor subtypes 5-HT1B and 5-HT1D. It is selective for 5-HT1B and 5-HT1D receptors over 5-HT1A receptors. Rizatriptan induces vasoconstriction in isolated human middle meningeal arteries. In vivo, rizatriptan reduces head grooming, the number of oculotemporal strokes, eye blinking, and one-eye closures in a Cacna1a mutant transgenic mou... | |||
T60989 |
Sumatriptan hydrochloride
|
||
Sumatriptan (GR 43175) hydrochloride 可用于研究偏头痛,它是一种口服有效的5-HT1受体激动剂。Sumatriptan hydrochloride 对5-HT1D、5-HT1B 和5-HT1A 受体的 Ki 值分别为 17 nM、27 nM 和 100 nM。 | |||
T63096 | SB-277011 hydrochloride | ||
SB-277011 hydrochloride (SB-277011A hydrochloride) 是一种强效的、选择性的、口服具有活力的、能透过血脑屏障的多巴胺 D3受体(D3R) 拮抗剂,对啮齿动物和人 D3R 的 Ki 值分别为 10.7 nM 和 11.2 nM。SB-277011 hydrochloride 对 D3 受体的选择性是其他多巴胺受体的 80-100 倍,作用于 D3 受体 (pKi:8.0),D2 受体 (pKi:6.0)、5-HT1B 受体 (pKi<5.2) 和 5-HT1D 受体 (pKi:5.9)。 | |||
T11827 |
Pradigastat
ANJ908,LCQ908-NXA,LCQ908A,LCQ-908 |
Transferase | Metabolism |
Pradigastat (LCQ-908) 是一种具有口服活性、有效性和选择性的二酰基甘油酰基转移酶 1 (DGAT1) 抑制剂,可用于治疗便秘,可用于研究肥胖和糖尿病。 | |||
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。 | |||
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。 | |||
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. | |||
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。 | |||
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 . |