95
3
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7477 |
Antazoline
|
Others | Others |
Antazoline 具有抗组胺和抗胆碱能作用。它用于治疗各种心律失常。 | |||
T9353 |
OXOMEMAZINE
|
AChR; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Oxomemazine 是毒菌碱 M1 受体的选择性拮抗剂,具有明显的抗毒蕈碱活性。它是基于吩噻嗪的组胺 H1 受体阻滞剂,是抗组胺和抗胆碱能试剂,可用于咳嗽相关研究。 | |||
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。 | |||
T1278 |
Astemizole
Laridal,Histaminos,Paralergin,阿司咪唑 |
Potassium Channel; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience |
Astemizole (Laridal) 是一种长效、非镇静抗组胺药,用于治疗季节性过敏性鼻炎、哮喘、过敏性结膜炎和慢性特发性荨麻疹。它是组胺 H1 受体的拮抗剂,IC50值为 4 nM,还阻断 hERG K+通道,IC50值为 0.9 nM,具有抗胆碱能和止痒作用。 | |||
T0147 |
Clemastine fumarate
HS-592 (fumarate),富马酸氯马斯汀,Meclastine fumarate,Meclastine (fumarate) |
Autophagy; Histamine Receptor | Autophagy; GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Clemastine fumarate (Meclastine (fumarate)) 是一种合成乙醇胺,具有抗胆碱能、镇静和组胺 H1 拮抗作用。 | |||
T22501 |
2-Pyridylethylamine dihydrochloride
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
2-Pyridylethylamine dihydrochloride 是一种组胺 H1 受体激动剂。 | |||
T23297 |
(S)-(+)-Dimethindene maleate
|
AChR; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
(S)-(+)-Dimethindene maleate 是一种可口服且具有选择性毒蕈碱 M2 受体和组胺 H1 受体拮抗剂,抑制毒蕈碱 M1,M3 和 M4 受体。 | |||
T22842 |
HTMT dimaleate
HTMT马来酸氢盐,Histamine Trifluoromethyl Toluidide Dimaleate |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
HTMT dimaleate (Histamine Trifluoromethyl Toluidide Dimaleate) 是一种 H1 和 H2 受体激动剂。在自然抑制细胞中,它在 H2 受体介导的效应中的活性是组胺的 4 x 104倍。 | |||
T0263 |
Chloropyramine hydrochloride
Nilfan,盐酸氯吡胺,Alergosan,Halopyramine hydrochloride |
FAK; VEGFR; Histamine Receptor | Angiogenesis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Neuroscience; Tyrosine Kinase/Adaptors |
Chloropyramine hydrochloride (Alergosan) 是一种组胺受体 H1 拮抗剂,可抑制VEGFR-3和FAK 的生化功能。 | |||
T1469 |
Levocetirizine
Levocetirizine HCl,左西替利嗪 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Levocetirizine 是一种组胺 H1 受体拮抗剂,可用于研究变应性鼻炎和慢性特发性荨麻疹。它是一种抗组胺剂,是 Cetirizine 的 R 对映体,对组胺 H1 受体的亲和力高于 (S)-Cetirizine。 | |||
T0092 |
Antazoline hydrochloride
盐酸安他唑啉,Phenazocine HCl,Phenazoline hydrochloride,Antazoline HCl |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Antazoline hydrochloride (Phenazoline hydrochloride) 是一种抗组胺药,可与组胺H1受体结合,阻断内源性组胺的作用。它也具有抗胆碱能特性,可缓解鼻塞,也可用作眼药水。 | |||
T6426 |
Buclizine dihydrochloride
盐酸安其敏,Longifene,Buclina,Buclizine HCl,UCB-4445 |
5-HT Receptor; AChR; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Buclizine dihydrochloride (Buclina) 是可口服的一种哌嗪组胺 H1 受体拮抗剂,主要具有止吐和抗眩晕活性。 | |||
T1097 |
Loratadine
氯雷他定,SCH 29851,Loratidine |
Influenza Virus; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience |
Loratadine (SCH 29851) 是一种组胺 H1受体反向激动剂,IC50>32 μM。它抑制炎症介质的免疫释放,具有抗登革热病毒的活性。 | |||
T1470L |
Fexofenadine hydrochloride
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Fexofenadine hydrochloride 是 terfenadine 的羧化代谢衍生物和长效选择性组胺 H1 受体拮抗剂,具有抗组胺活性。 | |||
T83975 |
Fenclozine Maleate
S 1429 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Fenclozine Maleate (S 1429) 是一种潜在的组胺H1受体拮抗剂 ,可用于研究发热、炎症和疼痛。 | |||
T0246 |
Betahistine dihydrochloride
PT-9,Betahistine 2HCl,盐酸倍他司汀 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Betahistine dihydrochloride (Betahistine 2HCl) 是可口服的组胺 H1 受体激动剂和 H3 受体的拮抗剂,可用作血管扩张剂,用于类风湿性关节炎的研究。 | |||
T22354 |
Levocetirizine Dihydrochloride
Xyzal Dihydrochloride,(-)-Cetirizine Dihydrochloride |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Levocetirizine Dihydrochloride (Xyzal Dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Acting as an antihistaminic agent, it specifically targets the histamine H1-receptor. Levocetirizine Dihydrochloride is the R-enantiomer of Cetirizine, which gives it a higher affinity for the H1-receptor than the S-enantiomer. Due to this enhanced affinity, Levocetirizine Dihydrochloride is effective in treating allergic rhinitis and chronic idiopathic urticaria. | |||
T13566 |
Bamirastine
TAK-427 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Bamirastine 抑制配体结合到重组人组胺 H1 受体 (rhH1R),IC50 值为 17.3 nM。Bamirastine 对过敏性皮肤炎症有抑制作用。 | |||
T1115 |
Doxylamine succinate
琥珀酸多西拉敏,Decapryn |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Doxylamine succinate (Decapryn) 是一种吡啶衍生物组胺 H1 拮抗剂,具有明显的镇静特性。它竞争性阻断组胺 H1 受体并限制典型的过敏和过敏反应,可防止组胺引起的皮肤和粘膜疼痛和瘙痒。 | |||
T0118 |
Mizolastine
SL 850324,咪唑司汀,咪唑斯汀 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Mizolastine (SL 850324) 是组胺 H1 受体拮抗剂,IC50为 47 nM。它用于治疗过敏反应,如花粉热和荨麻疹等。 | |||
T1822 |
Clemizole
克立咪唑,吡咯咪唑 |
HCV Protease; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience; Proteases/Proteasome |
Clemizole 是一种 H1 组胺受体拮抗剂,可抑制 NS4B 的 RNA 结合和丙型肝炎病毒复制。它也是TRP5通道抑制剂。 | |||
T7893 |
Bepotastine
Bepotastine free base,贝托斯汀 |
Others; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience; Others |
Bepotastine (Bepotastine free base) 是一种选择性可口服的组胺 H1 受体拮抗剂,可用于过敏性鼻炎、过敏性结膜炎、荨麻疹和瘙痒症的研究。 | |||
T10680 |
Carebastine
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Carebastine 是 Ebastine 的活性代谢产物,可抑制巨噬细胞移动抑制因子的表达。它是组胺 H1 受体拮抗剂,可抑制 VEGF 诱导的 HUVEC 和 HPAEC 增殖,迁移和血管生成。 | |||
T10100 |
QF0301B
|
5-HT Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
QF0301B是一种有效的 α1肾上腺素能受体拮抗剂,对α2肾上腺素受体,5-HT2A和组胺H1受体有抑制作用。 | |||
T1822L |
Clemizole hydrochloride
克立咪唑盐酸,盐酸克立咪唑 |
HCV Protease; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience; Proteases/Proteasome |
Clemizole hydrochloride 是一种 TRPC5通道的抑制剂。它还是一种 H1 组胺受体拮抗剂,抑制 HCV 复制。 | |||
T0053 |
Hydroxyzine Pamoate
Hydroxyzine embonate,双羟萘酸羟嗪,Bobsule,Equipose |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Hydroxyzine Pamoate (Bobsule) 是一种组胺 H1 受体拮抗剂,可有效治疗慢性荨麻疹、皮炎和组胺介导的瘙痒。它可作为止吐剂和镇静剂,缓解焦虑和紧张。 | |||
T10000 |
(±)-Tazifylline
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
(±)-Tazifylline 是一种选择性的长效组胺 H1 受体拮抗剂。 Tazifylline 对 H2 受体、α- 和 β-肾上腺素能受体、5-羟色胺和毒蕈碱受体亚型的亲和力要低得多。 | |||
T4250 |
Bilastine
比拉斯汀,Bilaxten |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Bilastine (Bilaxten) 是新型抗组胺药,对H1组胺受体具有高度选择性,起效快,作用时间长的特性,可用于变应性鼻结膜炎和荨麻疹。 | |||
T0903 |
Cinnarizine
Stugeron,桂利嗪,Cinarizine,Dimitronal,Stutgin |
Calcium Channel; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Cinnarizine (Stugeron) 是一种哌嗪衍生物,具有组胺 H1 受体和钙通道阻断活性,具有扩张血管和止吐的特性,可促进脑血流,用于脑中风、创伤后脑症状和脑动脉硬化的研究。 | |||
T16759 |
Ritanserin
利坦丝林,R 55667 |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Ritanserin (R 55667) 是一种长效、高效、相对选择性、可口服的5-HT2受体拮抗剂,IC50值为 0.9 nM。 | |||
T2533 |
Alcaftadine
R89674,Lastacaft,阿卡他定 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Alcaftadine (Lastacaft) 是一种 H1 组胺受体拮抗剂,用于预防与过敏性结膜炎相关的瘙痒。它是一种广谱抗组胺剂,对组胺H1和H2受体具有高亲和力,对H4受体的亲和力较低,还具有调节免疫细胞募集和肥大细胞稳定的作用。 | |||
T2200 |
Hydroxyzine dihydrochloride
Hydroxyzine 2HCl,盐酸羟嗪 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Hydroxyzine dihydrochloride (Hydroxyzine 2HCl) 是一种苯二氮卓抗组胺剂,是可口服的组胺 H1 受体和血清素拮抗剂,可有效治疗慢性荨麻疹、皮炎和组胺介导的瘙痒。它还可以作为止吐剂和镇静剂,有缓解焦虑和紧张的作用。 | |||
T3979 |
Emedastine
LY188695,依美斯汀,Emadine |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Emedastine (LY188695) 是一种可口服的,选择性和高亲和力的组胺 H1受体拮抗剂,Ki 值为 1.3 nM。它是苯并咪唑衍生物,可用于过敏性鼻炎、过敏性皮肤疾病和过敏性结膜炎的研究。 | |||
T12489L |
Pimethixene maleate
Pimetixene maleate |
Dopamine Receptor; 5-HT Receptor; AChR; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Pimethixene maleate (Pimetixene maleate) 是一种高效的 5-HT2B 受体拮抗剂,具有镇静和镇咳活性。Pimethixene maleate 抑制 5-HT1A,5-HT2A,5-HT2B,5-HT2C,组胺 H1,多巴胺 D2 和 D4.4 以及毒蕈碱 M1 和 M2,可用于研究儿童干咳和刺激性咳嗽。 | |||
T4195 |
Betahistine
PT 9 base,倍他司汀,Vasomotal,Serc base |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Betahistine (Vasomotal) 是可口服的组胺 H1 受体激动剂和 H3 受体的拮抗剂,可用作血管扩张剂,用于类风湿性关节炎的研究。 | |||
T1266 |
Terfenadine
(±)-Terfenadine,特非那定,MDL-991 |
Apoptosis; Potassium Channel; 5-HT Receptor; Caspase; Na+/Ca2+ Exchanger; HER; AChR; Histamine Receptor | Angiogenesis; Apoptosis; GPCR/G Protein; Immunology/Inflammation; JAK/STAT signaling; Membrane transporter/Ion channel; Neuroscience; Proteases/Proteasome; Tyrosine Kinase/Adaptors |
Terfenadine ((±)-Terfenadine) 是一种hERG 开放通道抑制剂,IC50为 204 nM。它也是一种 H1 组胺受体拮抗剂,通过调节Ca2+稳态在黑素瘤细胞中起到有效的细胞凋亡诱导作用。 Terfenadine 诱导 ROS 依赖性细胞凋亡,同时激活Caspase-4,-2,-9。 | |||
T9084 |
Cetirizine Impurity B dihydrochloride
De(carboxymethoxy) Cetirizine Acetic Acid Dihydrochloride,西替利嗪杂质B二盐酸盐,西替利嗪杂质04 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Cetirizine Impurity B dihydrochloride (De(carboxymethoxy) Cetirizine Acetic Acid Dihydrochloride) 是 Cetirizine dihydrochloride 的杂质。Cetirizine 是一种抗组胺剂,是口服有活力的、特异性 H1受体拮抗剂。它能够抑制过敏反应期间嗜酸性粒细胞趋化,可以标记抗过敏特性。 | |||
T19839 |
Oxatomide
Oxatomida |
P2X Receptor; Calcium Channel; 5-HT Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Oxatomide (Oxatomida) 是一种有效且具有口服活性的双重 H1 组胺受体 和 P2X7 受体双重拮抗剂,具有抗组胺和抗过敏活性。Oxatomide 可用于阻断人 P2X7 受体中 ATP 诱导的电流 ,IC50 为 0.95 μM。Oxatomide 对 ATP 诱导的 Ca2+ 内流具有抑制作用,IC50 值为 0.43 μM。Oxatomide 对 5-羟色胺具有抑制作用。Oxatomide可用于治疗免疫系统疾病和研究超敏反应。 | |||
T40652 |
Meclizine
Meclozine |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Meclizine (Meclozine) (Meclozine)具有抗组胺作用,可可逆地抑制组胺与H1受体的相互作用。Meclizine 是哌嗪类H1拮抗剂的一个成员。Meclizine 是一种有效的抗运动病剂。Meclizine 可通过血脑屏障。Meclizine 是小鼠组成型雄烷受体(CAR)的激动剂配体,也是人CAR 的反向激动剂。Meclizine 可用于polyQ 毒性疾病的研究,如亨廷顿病。 | |||
T73447 |
NP10679
|
||
NP10679 是一种选择性、pH 依赖性的GluN2B 亚基特异的 N-methyl-D-aspartate (NMDA) 受体抑制剂,具有较高的口服生物利用度和良好的脑穿透性。NP10679 在 pH 6.9 和 7.6 下,抑制 GluN2B 的IC50分别为 23 和 142 nM。NP10679 是histamine H1的拮抗剂和hERG 通道抑制剂,IC50分别为 73 和 620 nM。NP10679 是一种可逆的人肝脏CYP 酶抑制剂。 | |||
T0162 |
Quetiapine
ICI204636,Quetiapin,喹硫平 |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; AChR; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Quetiapine (ICI204636) 是5-HT 受体激动剂和多巴胺受体拮抗剂,对人5-HT1A 的 pEC50值为 4.77,对人 D2的 pIC50值为 6.33。它用于治疗精神分裂症,以及治疗与 I 型双相情感障碍相关的急性躁狂发作。它对人 D2、HT1、5-HT2A、5-HT2C 受体具有中高等亲和力,pKi 值为 7.25、5.74、7.54和5.55。 | |||
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。 | |||
T16541 |
Pirolate
CP-32387 |
Others | Others |
Pirolate is a receptor of histamine H1. | |||
T70467 |
Alinastine
|
||
Alinastine is a noncompetitive histamine H1 receptor antagonist. | |||
T71791 | Setastine HCl | ||
Setastine HCl is a potent antagonist of histamine H1-receptor mediated responses. | |||
T68632 | Pibaxizine | ||
Pibaxizine is diphenylmethyl piperazine derivatives. It is a histamine H1 receptor antagonist. | |||
T20951 |
Quifenadine
Phencarol,Fencarol,Fenatin |
||
Quifenadine, an H1-histamine receptor blocker, has antiarrhythmic properties. | |||
T20815 |
4-Chloroloratadine
4-Chloro loratadine,Loratadine specified impurity C |
||
4-Chloroloratadine is an impurity of Loratadine, a nonsedating-type histamine H1-receptor. | |||
T70306 |
Loratadine N-oxide
|
||
Loratadine N-oxide is a metabolite of the histamine H1 receptor inverse agonist loratadine. | |||
T12703 |
ReN-1869 hydrochloride
NNC-05-1869 hydrochloride |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
ReN 1869 hydrochloride is a novel, selective antagonist of histamine H1 receptor. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1008 |
Psoralenoside
|
CaMK; Calcium Channel; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Psoralenoside 是源于补骨脂中的苯并呋喃苷,具有抗肿瘤、抗菌、促进成骨细胞增殖和雌激素样活性。它对组胺 H1、钙调素和电压门控 l 型钙通道具有较高的亲和力。 | |||
T20884 |
Hydroxyzine
Hydroxyzine free base,羟嗪 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Hydroxyzine (Hydroxyzine free base) 是一种组胺 H1 受体拮抗剂,可有效治疗慢性荨麻疹、皮炎和组胺介导的瘙痒。它可作为止吐剂和镇静剂,缓解焦虑和紧张。 | |||
T2848 |
Osthole
Osthol,NSC 31868,蛇床子素,Ostol |
Apoptosis; HBV; Parasite; Histamine Receptor | Apoptosis; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience |
Osthole (Osthol) 是一种天然抗组胺药替代试剂,可刺激成骨细胞增殖和分化。它可抑制组胺 H1受体活性,还可抑制细胞培养物中 HBV 的分泌。 |