42
11
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11723L |
JNJ-39758979
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
JNJ-39758979是一种选择性的、高亲和力的、可口服的组胺 H4 受体拮抗剂,具有抗炎和止痒作用,对人、小鼠和猴子的组胺 H4 受体的 Ki 值分别为 12.5、5.3 和 25 nM。它对组胺诱导的 cAMP 抑制作用具有拮抗作用,pA2 为 7.9。 | |||
T22746 |
Tesmilifene fumarate
DPPE fumarate |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Tesmilifene fumarate (DPPE fumarate) 是一种 H1C 受体拮抗剂,可增强化疗的细胞毒性且保护正常细胞。 | |||
T0797 |
Cimetidine
西米替汀,SKF-92334,西咪替丁 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Cimetidine (SKF-92334) 是一种可口服的可逆组胺H2受体拮抗剂,Ki 为 0.6 μM。它抑制胃酸分泌,以及胃蛋白酶和胃泌素的输出,具有抗癌和抗炎活性。 | |||
T1336 |
Benztropine mesylate
Benzotropine mesylate,苯扎托品,Benzatropine mesylate,Benztropine methanesulfonate,甲磺酸苯扎托品 |
Dopamine Receptor; AChR; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Benztropine mesylate (Benztropine methanesulfonate) 是一种可口服的中枢性抗胆碱能剂,用于帕金森氏病的研究。它是抗组胺剂,抑制多巴胺的吸收。它也是人 D2多巴胺受体的变构拮抗剂,具有抗癌症干细胞的作用。 | |||
T26253 |
Tecastemizole
Norastemizole,R-43512,R43512,R 43512,T 1348 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Tecastemizole (R 43512) 是 H1 受体的选择性拮抗剂,是阿司咪唑的主要代谢产物,具有抗炎作用。 | |||
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。 | |||
T1110 |
Meclizine dihydrochloride
Meclozine dihydrochloride,NSC28728,Meclizine 2HCl,盐酸美克洛嗪 |
Apoptosis; Histamine Receptor | Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Meclizine dihydrochloride (NSC28728) 是一种组胺 H1 拮抗剂,用于治疗妊娠期间的晕动病、眩晕和恶心以及放射病。它是小鼠组成型雄甾烷受体激动剂,是人 CAR 的反向激动剂。它可透过血脑屏障,可用于多聚谷氨酰胺毒性障碍方面的研究。 | |||
T1090 |
Perphenazine
Perphenazin,Etaperazine,Trilafon,奋乃静 |
CaMK; Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Perphenazine (Trilafon) 是吩噻嗪衍生物和多巴胺拮抗剂,具有止吐和抗精神病特性。它能够抑制5-HT2A 受体,α1A 肾上腺素能受体,多巴胺D2、D3、D2L 受体,以及组胺H1受体,对应的Ki 值分别为5.6、10、0.765、0.13、3.4 和 8 nM。 | |||
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。 | |||
T27159 |
DF-1111301
DF1111301,DF 1111301 |
Platelet aggregation; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience; Others |
DF-1111301 是一种具有抗组胺 H1和抗PAF活性的新型抗过敏化合物。 | |||
T10945 |
D18024
|
Others | Others |
D18024 是一种酞嗪酮的衍生物,显示出抗过敏和抗组胺活性。 | |||
T0298 |
Dimenhydrinate
茶苯海明,Dramamine,Chloranautine,乘晕宁,Vomex A |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Dimenhydrinate (Vomex A) 是一种乙醇胺和组胺拮抗剂,具有抗过敏活性,可作为抗催吐剂。 | |||
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。 | |||
T34709 |
ST-1006
ST 1006 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
ST-1006是一种强效组胺 H4受体激动剂(pKi:7.94)。ST-1006具有抗炎作用。ST-1006是一种有效的嗜碱性粒细胞迁移诱导剂,可诱导嗜碱性粒细胞迁移。 ST-1006 具有抗炎作用和止痒作用。 | |||
T0217L |
(+)-Dropropizine
(+)-Dropropizine,左羟丙哌嗪 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
(+)-Dropropizine 可以抑制组胺受体,抗过敏,并通过调节参与咳嗽反射的神经肽和干扰感觉神经末梢的刺激激活来减少咳嗽。 | |||
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。 | |||
T1639 |
Amlexanox
氨来呫诺,CHX3673,Amoxanox,氨来诺,AA673 |
IL Receptor; FGFR; Others; IκB/IKK | Angiogenesis; Immunology/Inflammation; NF-κB; Others; Tyrosine Kinase/Adaptors |
Amlexanox (AA673) 是一种特异性的 IKKε和 TBK1抑制剂,其 IC50=1-2 μM。 | |||
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。 | |||
T4978 |
Sarpogrelate hydrochloride
盐酸沙格雷酯,MCI-9042 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Sarpogrelate hydrochloride (MCI-9042) 是一种选择性5-HT2R 拮抗剂,可用于研究与血栓形成有关的血管疾病,对 5-HT2A、5-HT2B 和 5-HT2C 受体的pKi 值分别为 8.52、6.57 和 7.43。 | |||
T26491 |
AA 2379
AA2379,AA-2379 |
||
AA 2379, an anti inflammatory agent, inhibits the vascular permeability induced by histamine, serotonin, and bradykinin. It also has some analgesic activity. | |||
T24951 |
VUF-10497
|
||
VUF-10497 is a histamine H4 receptor inverse agonist (pKi = 7.57). VUF-10497 was found to possess anti-inflammatory properties in vivo in the rat. VUF-10497 also possesses a considerable affinity for the human histamine H1 receptor. | |||
T27388 |
FR-A 19
FR-A-19,FRA19 |
||
FR-A 19, a Histamine H2 agonist, inhibits the release of IgE-mediated human basophil histamine in a nanomolar range. It has additional potent anti-allergic properties. | |||
T21388 |
Emedastine Difumarate
Rapimine,DSSTox_CID_26911,AL-3432A,富马酸依美斯汀,KB-2413,Emedastine fumarate,KB 2413 |
||
Emedastine Difumarate is a selective histamine H1 receptor antagonist with anti-allergic activity, prescribed for allergic conjunctivitis. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeabil | |||
T23597 |
A-940894
A940894,A 940894 |
||
A-940894 is a histamine H4 receptor antagonist with anti-inflammatory properties. A-940894 potently binds to both human and rat histamine H4 receptors and exhibits considerably lower affinity for the human histamine H1, H2, or H3 receptors. A-940894 has g | |||
T60498 | Chlorpheniramine | ||
Chlorpheniramine 是一种 H1 抗组胺药,用于治疗 IgE 介导的炎症,通常用于治疗过敏性疾病。 | |||
T0157L |
Roxatidine acetate
|
||
Roxatidine acetate is an anti-ulcer agent and histamine antagonist that inhibits gastric acid secretion. Compared to other similar drugs, Roxatidine acetate has an improved safety profile, in part because lower doses of roxatidine acetate are therapeutica | |||
T68206 | Arbortristoside A | ||
Arbortristoside A is an anti-inflammatory and antinociceptive. This activity may be due to the inhibiting effect of prostaglandin, histamine and serotonin. Arbortristoside A has also been shown to act on ulcerations and may facilitate healing of peptic ulcers. | |||
TP1408 |
Peptide 401
|
||
Peptide 401 is an antimicrobial peptide (AMP) derived from the venom of bees and wasps. Peptide 401 induces mast cell degranulation, activating histamine release from peritoneal mast cells. Additionally, peptide 401 exhibits some anti-inflammatory activit | |||
T74118 |
Roxatidine
|
||
Roxatidine 是 Roxatidine acetate 的活性代谢产物,是组胺 H2受体拮抗剂。Roxatidine 是抗溃疡药,抑制组胺释放(从而抑制质子分泌)并抑制炎症和血管生成的重要标志物 VEGF-1 的产生。具有抗过敏性炎症作用。 | |||
T68200 |
Roxatidine hydrochloride
|
||
Roxatidine hydrochloride is an anti-ulcer agent and histamine antagonist that suppresses gastric acid secretion. It effectively heals duodenal and gastric ulcers and reduces ulcer pain. Roxatidine acetate has an improved safety profile compared to other similar drugs, in part because lower doses of roxatidine acetate are therapeutically effective. | |||
T60584 |
Cimetidine hydrochloride
|
||
Cimetidine (SKF-92334) hydrochloride 是一种具有口服活性的,可逆的组胺H2受体拮抗剂 (Ki = 0.6 μM)。Cimetidine hydrochloride 显示出抗癌和抗炎活性。Cimetidine hydrochloride 是一种胃酸减少剂,它可用于十二指肠和胃溃疡的相关研究。 | |||
T71059 |
Ranitidine bismuth citrate
IST 622,雷尼替丁枸橼酸盐 |
||
Ranitidine bismuth citrate 为一种口服活性的组胺H2受体(Histamine H2-receptor)拮抗剂,其IC50值为3.3 μM,对SARS-CoV-2感染细胞显示高选择性。该化合物还是治疗幽门螺杆菌(Helicobacter Pylori)感染的常用试剂,其MIC90为16 ng/L。 | |||
T71141 |
Fenspiride-d5
|
||
Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from ... | |||
T22018 |
A 987306
|
||
A-987306 是一种高效、口服生物可利用的组胺H4拮抗剂,对大鼠和人 H4作用的Ki 值分别为 3.4 nM 和 5.8 nM。 A-987306 在小鼠腹膜炎模型中显示出抗炎活性。 | |||
T61011 | Izuforant | ||
Izuforant (JW1601) (Compound 24) 具有有效的抗炎和止痒活性。 Izuforant 对人血清素3受体 (h5-HT3R) 具有结合亲和力,IC50值为 9.1 μM。它也是组胺 H4 受体 (H4R) 的口服活性拮抗剂,对人 H4R 的IC50值为 36 nM。 | |||
T73352 |
A-943931
|
||
A-943931 是一种有效的选择性组胺 H4 受体拮抗剂,对人和大鼠 H4R 的 Ki 值分别为 4.6、3.8 nM。A-943931 具有抗炎和抗伤害作用。 | |||
T61603 | H3R antagonist 2 | ||
H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor antagonist. It exhibits inhibitory effects on acetylcholinesterase, butyrylcholinesterase, and human monoamine oxidase B (hMAO B) with IC50 values of 180 nM, 880 nM, and 775 nM, respectively. With a Ki of 170 nM for hH3R, H3R antagonist 2 demonstrates favorable anti-neuropathic pain and memory-enhancing effects. Additionally, it can cross the blood-brain barrier (BBB) [1]. | |||
T22242 |
Amodiaquine hydrochloride
|
||
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride) 是一种4-氨基喹啉类抗疟剂,是一种有效的口服活性的组胺 N-甲基转移酶 (histamine N-methyltransferase) 抑制剂,Ki 值为 18.6 nM。Amodiaquine dihydrochloride 也是一种Nurr1激动剂,可特异性结合Nurr1的配体结合域,EC50约为20 μM,具有抗炎作用。 | |||
T73665 |
Bufrolin
|
||
Bufrolin,作为Cromoglycate(组胺释放抑制剂)的类似物,是一种高效的GPR35激动剂,能够促进β-arrestin-2与人GPR35a或大鼠GPR35之间的相互作用。此外,Bufrolin亦可作为抗过敏性肥大细胞稳定剂,有效抑制内化肽诱导的抗炎反应,并且在内化肽连接药剂的药物递送研究中,被作为抗炎剂使用。 | |||
T62460 |
INCB38579
|
||
INCB38579 是一种选择性的、口服具有活力的、能够透过血脑屏障的组胺 H4受体 (HH4R) 拮抗剂,能够作用于 hH4R (IC50: 4.8 nM)、mH4R (IC50: 42 nM)、rH4R (IC50: 32 nM)。INCB38579 具有抗炎和抗瘙痒作用。 | |||
T36618 |
Rupatadine
|
||
Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in hu... | |||
T60417 |
Fenspiride
|
||
Fenspiride 是 H1-组胺受体的拮抗剂。 Fenspiride 是一种具有口服活性的非甾体类抗炎药,可用于治疗呼吸道感染和中耳炎。 Fenspiride 抑制磷酸二酯酶 4 和磷酸二酯酶 3 的活性,-logIC50 值分别为 4.16+/-0.09 和 3.44+/-0.12。 磷酸二酯酶 5 活性也受到抑制,-logIC50 值约为 3.8。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T20712 |
Conessine
Conessinum,Wrightine,地麻素,Roquessine,Neriine,Konessin |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Conessine (Conessinum) 是一种具有抗疟活性的甾体生物碱,是高效选择性H3 受体拮抗剂,对于人、狗、豚鼠和大鼠 H3受体的Ki 分别为 5.4、6.0、5.7 和 25 nM。 | |||
T20597 |
Alginic acid
Protanal LF,褐藻酸,Snow acid algin G,Kelacid,Sazzio,Norgine |
Apoptosis; Autophagy; Histamine Receptor | Apoptosis; Autophagy; GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Alginic acid (Snow acid algin G) 是一种从褐海藻中提取的天然多糖,具有抗过敏和抗炎活性。 Alginic acid 抑制组胺释放,可用于食品工业。 | |||
T5S1286 |
(+)-Columbianetin
二氢山芹醇,(S)-Columbianetin,Columbianetin |
Antifungal | Microbiology/Virology |
(+)-Columbianetin ((S)-Columbianetin) 是 Columbianetin 的异构体。其中Columbianetin 是一种植物抗毒素,与芹菜贮藏过程中对病原体的抗性有关,具有良好的抗真菌和抗炎作用。 | |||
TN1661 |
Ganoderic acid C2
灵芝酸 C2 |
Reductase; Histamine Receptor; Immunology/Inflammation related | Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience |
Ganoderic acid C2 是分离自灵芝的一种三萜化合物, 具有潜在的抗肿瘤生物活性,以及抗组胺、抗衰老和细胞毒性作用。它对rat lens aldose reductase 具有很高的抑制活性,IC50为 3.8 µM。 | |||
T5S1889 |
Yunaconitine
Guayewuanine B,滇乌头碱 |
Others | Others |
Yunaconitine (Guayewuanine B) 是一种乌头类生物碱,具有剧毒。 | |||
T3728 |
Methyl Paraben
尼泊金甲酯,Methyl parahydroxybenzoate,Nipagin,对羟基苯甲酸甲酯,Methylparaben,Methyl 4-hydroxybenzoate,Methyl p-hydroxybenzoate |
Endogenous Metabolite; Antibacterial; Antibiotic | Metabolism; Microbiology/Virology |
Methyl Paraben (Nipagin) 是一种标准化的过敏原,是从云南铁杉中分离出来对羟基苯甲酸的甲酯。它是一种抗菌剂、防腐剂、调味剂。它的生理作用是通过增加组胺释放和细胞调控免疫实现的。 | |||
TN3483 |
Bakkenolide D
|
IL Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Bakkenolide D has anti-allergic effect, it and bakkenolide D demonstrates inhibitory effect on the trachea contraction induced by histamine in vitro, they have obvious anti-histamine activities. | |||
TN2155 |
Rhodiocyanoside A
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Rhodiocyanoside A has antiallergic activity, it exhibits inhibitory activity on the histamine release from rat peritoneal exudate cells sensitized with anti-DNP IgE and inhibits the PCA reaction in rats. | |||
TN4392 |
Koaburaside
|
IL Receptor; TNF; Influenza Virus | Apoptosis; Immunology/Inflammation; Microbiology/Virology |
Koaburaside exhibits antioxidant activity with an IC50 value of 9.0μM, it shows weak inhibitory activity against influenza A neuraminidase. Koaburaside may have anti-allergic inflammatory activity, it can suppress histamine release from mast cells. | |||
TN1913 |
Marmin
|
Calcium Channel; Antifection; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience |
Marmin have anti-ulcer effects, which are ascribed primarily to the maintenance of the mucosal barrier integrity and inhibition of gastric motor activity and secondarily due to the prevention of the effects of endogenous acetylcholine and histamine. | |||
TN3325 |
9-O-Feruloyl-5,5'-dimethoxylariciresinol
|
IL Receptor; TNF | Apoptosis; Immunology/Inflammation |
(+)-9'-O-trans-feruloyl-5,5'-dimethoxylariciresinol may have anti-allergic inflammatory effect, it can inhibit release of histamine from mast cells. It shows cytotoxicity against a small panel of human tumor cell lines, with ED50 values of 9.86 to approxi |