Histamine Receptor

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研究领域

抑制剂选择性比较

特异性亚型抑制剂

Histamine Receptor产品

所有产品(77) Histamine Receptor抑制剂(17) Histamine Receptor拮抗剂(51) Histamine Receptor激动剂(9)

目录号	产品描述	文献引用	实验数据
S3913^New	Pimethixene maleate Pimethixene (Pimetixene) maleate 是一种抗组胺药、抗焦虑药和抗血清素的化合物，是多种monoamine receptors，包括多种 serotonin receptors 的高效拮抗剂。Pimethixene maleate 可抑制5-HT2A、5-HT2B、5-HT2C、5-HT1A、5-HT1B、5-HT6、5-HT7、Adrenergic α-1A、Dopamine D1 Receptor、Dopamine D2 Receptor、Dopamine D4.4 Receptor、Histamine H1 Receptor、Muscarinic M1 和 Muscarinic M2，对应的pKi值分别为10.22、10.44、8.42、7.63、<5、7.30、7.28、7.61、6.37、8.19、7.54、10.14、8.61和9.38。
S1291	Cetirizine DiHCl Cetirizine DiHCl (UCB P071) 是一种抗组胺剂。	Environ Toxicol Chem, 2021, 10.1002/etc.5018 J Allergy Clin Immunol, 2017, 139(4):1253-1265 J Allergy Clin Immunol, 2016, 10.1016/j.jaci.2016.03.028	Body temperatures of pretreated mice during IgG1-induced PSA in FcγRIIB-/- (n=6 per group) or WT (n=4 per group) mice.
S3208	Fexofenadine HCl Fexofenadine (MDL 16455A) 抑制组胺H1受体，IC50为246 nM。	Anticancer Res, 2019, 39(7):3767-3775 Sci Rep, 2016, 10.1038/srep25694
S4253	Epinastine HCl Epinastine (WAL-801CL) 是一种抗组胺剂和肥大细胞稳定剂，用于眼药水治疗过敏性结膜炎。
S2494	Olopatadine HCl Olopatadine HCl 是一种组胺抑制剂，也是肥大细胞稳定剂，抑制组胺释放，IC50为559 μM。
S4140	Buclizine HCl Buclizine HCl (UCB-4445)是哌嗪衍生物家族的antihistamine（抗组胺药）和anticholinergic（抗胆碱药）。
S3052	Rupatadine Fumarate Rupatadine Fumarate是一种PAFR和组胺(H1)受体抑制剂，K_i分别为550 nM和102 nM。
S2024	Ketotifen Fumarate Ketotifen Fumarate 是Ketotifen的富马酸盐，是H1抗组胺剂，也是肥大细胞稳定剂。	Environ Toxicol Chem, 2021, 10.1002/etc.5018
S3183	Amitriptyline HCl Amitriptyline HCl 是一种 serotonin transporter (SERT) 和 norepinephrine transporter (NET) 的抑制剂，其Ki值分别为3.45 nM和13.3 nM。Amitriptyline HCl 还可抑制histamine receptor H1、histamine receptor H4、5-HT2 和 sigma 1 receptor，对应的Ki值分别是0.5 nM、7.31 nM、235 nM和287 nM。Amitriptyline 是一种三环抗抑郁药物。	Environ Toxicol Chem, 2021, 10.1002/etc.5018 PLoS Pathog, 2020, 16;16(3):e1008341 Sci Rep, 2018, 8(1):15753
S3186	Azatadine dimaleate Azatadine (SCH10649) 是一种抗组胺和抗胆碱能药物，IC50分别为6.5nM和10nM。	Pharmaceuticals (Basel), 2019, 12(4)
S4131	Levodropropizine Levodropropizine可以抗过敏并抑制组胺受体，通过干扰外围感觉神经末端的刺激活化作用以及调节参与咳嗽反射的神经肽来减轻咳嗽。
S5947	Amitriptyline Amitriptyline (MK-230, N-750, Ro41575) 是一种三环抗抑郁药，具有止痛效果，被广泛用于治疗抑郁和神经性疼痛。Amitriptyline 是一种 serotonin transporter (SERT) 和 norepinephrine transporter (NET) 的抑制剂，其Ki值分别为3.45 nM和13.3 nM。Amitriptyline 还可抑制histamine receptor H1、histamine receptor H4、5-HT2 和 sigma 1 receptor，对应的Ki值分别是0.5 nM、7.31 nM、235 nM和287 nM。该产品呈胶状。	Cancers (Basel), 2019, 11(12)
S4672	Dimenhydrinate Dimenhydrinate是一种用于治疗由晕动症引起的恶心、呕吐、头晕的药物。
S2308	Hesperetin Hesperetin是一种生物类黄酮，更具体而言，是一种二氢黄酮。	Carcinogenesis, 2020, 41(7):993-1004
S4696	CarbinoxaMine Maleate Carbinoxamine maleate是一种组胺-H1受体阻滞剂，具有抗组胺和反副交感神经生理作用。	Am J Physiol Lung Cell Mol Physiol, 2019, 316(1):L20-L34 Anticancer Res, 2019, 39(7):3767-3775
S4240	Doxylamine Succinate Doxylamine succinate竞争性抑制组胺H1受体，具有镇静和抗胆碱作用。	Environ Toxicol Chem, 2021, 10.1002/etc.5018
S3176	Betahistine 2HCl Betahistine (PT-9) 是一种组胺H3受体抑制剂，IC50为1.9 μM。
S1847	Clemastine (HS-592) fumarate Clemastine Fumarate (HS-592, Meclastine)是一种选择性组胺H1受体拮抗剂，IC50为3 nM。Clemastine 可通过 mTOR 信号通路来刺激自噬。	Neuron, 2021, S0896-6273(21)00352-4 Neurosci Bull, 2021, 10.1007/s12264-021-00745-1 Nat Neurosci, 2020, 10.1038/s41593-020-0588-8	Detection of P2X7 receptor and histamine receptor H1 (HRH1) in hippocampus and mPFC. (A–F) CUMS treatment upregulated the protein expression of the purinergic receptor P2X, ligand-gated ion channel 7 (P2X7R) in both hippocampus and mPFC subregions. In the meantime, continuous intraperitoneal administration of clemastine protected mice from stress-induced upregulation of P2X7R in the hippocampus rather than mPFC. There is no statistical alteration of HRH1 expression in both subfields of hippocampus and mPFC, even when the mice were subjected to stress stimulation or clemastine injection (n = 4 for (A–F), p < 0.05, *p < 0.01).
S1245	Latrepirdine 2HCl Latrepirdine具有口服活性及神经活性，可以作为包括histamine receptors, GluR, 和5-HT receptors在内的多个药物靶点的拮抗剂，用作抗组织胺的药物。
S1358	Loratadine (SCH29851) Loratadine (SCH29851) 是一种选择性的histamine H1 receptor拮抗剂，用于治疗过敏。同时还是一种选择性的B(0)AT2抑制剂，其IC50为 4 μM。	EMBO Mol Med, 2021, e13929 Adv Ther (Weinh), 2020, 2000034 Cell Syst, 2019, 8(2):97-108
S3037	Bepotastine Besilate Bepotastine Besilate (TAU 284)是一种非镇静作用的，选择性的组胺1 (H1)受体拮抗剂，pIC50为5.7。	Hum Cell, 2021, 10.1007/s13577-021-00579-z Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S1382	Mianserin HCl Mianserin (ORG GB-94) l是一种四环类抗抑郁药。	Immunity, 2019, 50(5):1163-1171
S5196^New	Promethazine Promethazine 是一种有效的 histamine H1 receptor 的拮抗剂。Promethazine 是可用于过敏性疾病、恶心和呕吐、晕车和镇静的管理和治疗的药物。异丙嗪具有抗寄生虫的特性。
S5864^New	Levocetirizine Levocetirizine (LCZ, (R)-Cetirizine) 是Cetirizine的R-对映体，是一种 histamine H(1) receptor 的拮抗剂。
S2552	Azelastine HCl Azelastine HCl是有效的，第二代选择性组胺拮抗剂。	Theranostics, 2021, 11(4):1828-1844 Anticancer Res, 2019, 39(7):3767-3775
S1801	Ranitidine Hydrochloride Ranitidine (AH19065) 是组胺H2-受体拮抗剂，IC50为3.3±1.4 μM。	bioRxiv, 2021, 10.1101/2021.04.29.441931
S1866	Diphenhydramine HCl Diphenhydramine HCl 是组胺H1拮抗剂，可用于止吐止咳，治疗皮肤病和皮肤瘙痒，过敏反应，用作安眠药，治疗帕金森，作为感冒制剂一种组分。	Int J Pharm, 2019, 560:294-305 Anticancer Res, 2019, 39(7):3767-3775 Sci Rep, 2017, 7(1):8491
S4012	Desloratadine Desloratadine (SCH-34117, NSC 675447)是一种有效的人组胺H1受体拮抗剂，IC50为51nM.	Anticancer Res, 2019, 39(7):3767-3775
S1816	Chlorpheniramine Maleate Chlorpheniramine Maleate (Chlorpheniramine maleate, Chlorphenamine, NCI-C55265)是一种组胺H1受体拮抗剂，IC50为12 nM。	Anticancer Res, 2019, 39(7):3767-3775
S2813	Ciproxifan Maleate Ciproxifan (FUB 359) 是一种高效的，选择性的histamin H3-receptor拮抗剂，IC50为9.2 nM，作用于其他受体亚型具有低亲和力。	Acta Pharmacol Sin, 2020, 10.1038/s41401-020-00548-6 Oncol Lett, 2018, 16(4):4921-4928
S1986	Meclizine 2HCl Meclizine (NSC 28728) 是histamine H1 receptor拮抗剂,用于治疗恶心，晕动病，也是mCAR（组成型雄烷受体激动剂配体）激动剂配体，也是hCAR的反向激动剂。	Anticancer Res, 2019, 39(7):3767-3775 Front Pharmacol, 2017, 8:693
S2107	Mizolastine Mizolastine (SL 850324) 是一种组胺H1受体拮抗剂，IC50为47 nM，用于治疗花粉症（季节性过敏性鼻炎）、荨麻疹和其他过敏性反应。
S1845	Cimetidine Cimetidine (SKF-92334) 是一种组胺类似物，竞争性地抑制组胺结合到组胺H2受体。	Cell Rep, 2021, 34(10):108832 bioRxiv, 2021, 10.1101/2021.04.29.441931 Anticancer Res, 2019, 39(7):3767-3775
S2065	Lafutidine Lafutidine (FRG-8813)是一种新开发的组胺H(2)受体拮抗剂，抑制胃酸分泌。
S1890	Nizatidine Nizatidine是一种组胺H2受体拮抗剂，作用于AChE，IC50为6.7 nM。	bioRxiv, 2021, 10.1101/2021.04.29.441931 Anticancer Res, 2019, 39(7):3767-3775
S3146	Tripelennamine HCl Tripelennamine (Pyribenzamine) 是一种广泛使用的组胺1拮抗剂(H1拮抗剂)，抑制PhIP糖脂化，IC50为30 μM。
S2044	Cyproheptadine HCl Cyproheptadine HCl 是Cyproheptadine的盐酸盐形式，是组胺受体拮抗剂，作用于5-HT₂受体，IC50为0.6 nM。	Cell Rep, 2020, 21;31(3):107548 Vet Med Sci, 2020, 10.1002/vms3.336 Anticancer Res, 2019, 39(7):3767-3775
S4026	Hydroxyzine 2HCl Hydroxyzine 2HCl抑制[³H]pyrilamine或[³H]desloratadine与人源组胺H1受体的结合， IC50分别为10 nM和19 nM。	Anticancer Res, 2019, 39(7):3767-3775 Nature, 2018, 560(7718):372-376	a, Quantification of sterol levels in OPCs (oligodendrocyte progenitor cells) treated with the indicated molecules at 2 μM. b, Quantification of sterol levels in OPCs treated with the indicated previously reported enhancers of oligodendrocyte formation (n = 2 wells per condition except DMSO, n = 6). Representative of two independent experiments; for concentrations, see Extended Data Fig. 6g. c, Quantification of EBP enzymatic activity in a biochemical assay. All treatments 10 μM. n = 3 independent enzymatic assays, except DMSO, n = 5. Bars indicate mean; error bars indicate s.d. Sigma H127, p-fluorohexahydro-sila-difenidol.
S4262	Ebastine Ebastine是强效的H1型组氨酸受体（H1-histamine receptor）拮抗剂，被用来治疗过敏性疾病。
S2585	Brompheniramine hydrogen maleate Brompheniramine hydrogen maleate是一种组胺H1受体拮抗剂。	Anticancer Res, 2019, 39(7):3767-3775
S2905	JNJ-7777120 JNJ-7777120是第一个，有效的，选择性非咪唑histamine H4 receptor拮抗剂，K_i为4.5 nM，比作用于其他组胺受体选择性高1000倍以上。	J Assoc Res Otolaryngol, 2021, 10.1007/s10162-021-00803-5 Neuropharmacology, 2020, 168:108028 Mol Ther Methods Clin Dev, 2018, 11:83-91
S4008	Pemirolast potassium Pemirolast potassium (BMY26517) 是一种组胺H1拮抗剂和肥大细胞稳定剂，用作抗过敏药。	Front Microbiol, 2020, 10:2936 Anticancer Res, 2019, 39(7):3767-3775
S4849	Levocetirizine Dihydrochloride Levocetirizine (Xyzal, (-)-Cetirizine) 是cetirizine的活性(R)-对映异构体，是新型二代histamine H1拮抗剂。	Anticancer Res, 2019, 39(7):3767-3775
S5670	Chloropyramine hydrochloride Chloropyramine hydrochloride (Halopyramine) is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects.
S5659	Emedastine Emedastine is a potent, high affinity histamine H1-receptor-selective antagonist with Ki of 1.3 ±0.1 nM for H1-receptors while considerably weaker at H2- (K1 = 49,067 ± 11,113 nM) and H3-receptors (Ki = 12,430 ± 1,282 nM).
S4139	Cyclizine 2HCl Cyclizine 2HCl是一种哌嗪衍生物，具有Histamine H1(组胺H1)受体拮抗剂活性。
S5940	Bepotastine Bepotastine是一种非镇静的、选择性histamine 1 (H1) receptor拮抗剂。
S4625	Alcaftadine Alcaftadine (Lastacaft, R89674) 是H1受体的高亲和力配体，pKi为8.5。Alcaftadine还是H2和H4受体的拮抗剂，对H3受体没有亲和力。
S4045	Pheniramine Maleate Pheniramine Maleate 是一种抗组胺剂，具有抗胆碱能特性，用于治疗花粉症或荨麻疹等过敏性疾病。
S5479	Cloperastine hydrochloride Cloperastine (HT-11) is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity.
S5656	Diphenylpyraline hydrochloride Diphenylpyraline hydrochloride is the hydrochloride salt form of diphenylpyraline, which is an antihistamine used in the treatment of allergic rhinitis, hay fever, and allergic skin disorders.
S1880	Roxatidine Acetate HCl Roxatidine Acetate HCl是特异性的，竞争性的组胺H2受体拮抗剂，IC50为3.2 μM，抑制胃酸分泌和溃疡形成。
S5718	Acrivastine Acrivastine is an antihistamine medicine that relieves the symptoms of allergies.
S5447	Triprolidine Hydrochloride Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.
S5647	Emedastine Difumarate Emedastine Difumarate (Rapimine, Emedastine fumarate) is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity.
S5018	Mebhydrolin napadisylate Mebhydrolin Napadisylate (Diazoline, Diazolin, Incidal, Omeril)是一种抗组胺类药物，用于治疗过敏。
S8598	S 38093 S 38093是histamine H3拮抗剂/反向激动剂，对大鼠、小鼠和人源H3受体具有中等亲和力（Ki值分别为8.8、1.44、1.2 μM），对其他组胺能受体没有亲和力。
S5926	Pitolisant hydrochloride Pitolisant (Tiprolisant, BF-2649)是一种高亲和力的、竞争性H3受体拮抗剂，Ki为0.16 nM。同时也是组胺H3受体的反向激动剂（EC50=1.5 nM）。
S0398	Astemizole Astemizole (R 43512)是一种 histamine H1-receptor 拮抗剂，其IC50值为4.7 nM。Astemizole 还是一种有效的 ether à-go-go 1 (Eag1) 和 Eag-related gene (Erg) potassium channels 的抑制剂。Astemizole 具有抗肿瘤和止痒的作用。
S5649	Hydroxyzine pamoate Hydroxyzine Pamoate is the pamoate salt form of hydroxyzine, a synthetic piperazine histamine H1-receptor antagonist with anti-allergic, antispasmodic, sedative, anti-emetic and anti-anxiety properties.	Anticancer Res, 2019, 39(7):3767-3775
S3721	Bilastine Bilastine是一种新型耐受的、无镇静作用的抗组胺剂，针对H1 receptor。其效果迅速并持久。
S5662	Ranitidine Ranitidine is an H2 histamine receptor antagonist that works by blocking histamine and thus decreasing the amount of acid released by cells of the stomach.	bioRxiv, 2021, 10.1101/2021.04.29.441931 Anticancer Res, 2019, 39(7):3767-3775
S3120	Doxepin HCl Doxepin是一种精神药物，是一种三环类抗抑郁药，具有抗焦虑活性。
S4353	Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
S6435	Mequitazine Mequitazine (LM-209)是histamine H1拮抗剂，可与组胺竞争性结合胃肠道、血管和呼吸道效应细胞上正常H1受体。
S2078	Famotidine Famotidine (MK208)是组胺H2受体拮抗剂，IC50为0.6 mM，常用来治疗胃灼热，GERD，溃疡和其他消化系统不良情况。	bioRxiv, 2021, 10.1101/2021.04.29.441931 Anticancer Res, 2019, 39(7):3767-3775
S6469	Thonzylamine Thonzylamine (Neohetramine) 是抗组胺剂和抗胆碱能药。
S4293	Promethazine HCl Promethazine HCl 是一种强效的histamine H₁受体拮抗剂,被用作镇静和抗过敏的药物。	bioRxiv, 2020, 2020/9/20.4.7.30734 Anticancer Res, 2019, 39(7):3767-3775 Chem Biol Interact, 2019, 315:108888
S1357	Lidocaine Lidocaine (Alphacaine)是一种选择性的，逆向外周组胺H1受体激动剂，IC50大于32 μM。	Exp Ther Med, 2021, 21(5):424 Nat Biomed Eng, 2020, 4(3):286-297 J Cell Biochem, 2019, 120(10):16533-16542
S3968	Histamine Histamine, an organic nitrogenous compound, is involved in local immune responses regulating physiological function in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. It is a potent H1 and H2 receptor agonist.	Life Sci, 2019, 227:74-81
S4117	Histamine Phosphate Histamine Phosphate直接作用于血管，扩张H1和H2受体介导的动脉和毛细血管。
S4118	Histamine 2HCl Histamine 2HCl是一种有机氮化合物，通过对组胺1/2的刺激来对哺乳类大脑中靶细胞起作用。	Front Pharmacol, 2017, 8:667
S6612	Betazole Dihydrochloride Betazole Dihydrochloride (Ametazole, 2-(3-Pyrazolyl)ethanamine)是histamine H2激动剂，在临床上用于检测胃分泌功能。
S5498	Betahistine mesylate Betahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator.
S6569	VUF10460 VUF10460是histamine H4 receptor激动剂。
S5619	Betahistine Betahistine is an antivertigo drug that primarily acts as a histamine H1 agonist.
S4382	Pyrilamine Maleate Pyrilamine Maleate (Mepyramine) is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling.

目录号	产品描述	文献引用	实验数据
S3913^New	Pimethixene maleate Pimethixene (Pimetixene) maleate 是一种抗组胺药、抗焦虑药和抗血清素的化合物，是多种monoamine receptors，包括多种 serotonin receptors 的高效拮抗剂。Pimethixene maleate 可抑制5-HT2A、5-HT2B、5-HT2C、5-HT1A、5-HT1B、5-HT6、5-HT7、Adrenergic α-1A、Dopamine D1 Receptor、Dopamine D2 Receptor、Dopamine D4.4 Receptor、Histamine H1 Receptor、Muscarinic M1 和 Muscarinic M2，对应的pKi值分别为10.22、10.44、8.42、7.63、<5、7.30、7.28、7.61、6.37、8.19、7.54、10.14、8.61和9.38。
S1291	Cetirizine DiHCl Cetirizine DiHCl (UCB P071) 是一种抗组胺剂。	Environ Toxicol Chem,2021, 10.1002/etc.5018 J Allergy Clin Immunol,2017, 139(4):1253-1265 J Allergy Clin Immunol,2016, 10.1016/j.jaci.2016.03.028	Body temperatures of pretreated mice during IgG1-induced PSA in FcγRIIB-/- (n=6 per group) or WT (n=4 per group) mice.
S3208	Fexofenadine HCl Fexofenadine (MDL 16455A) 抑制组胺H1受体，IC50为246 nM。	Anticancer Res,2019, 39(7):3767-3775 Sci Rep,2016, 10.1038/srep25694
S4253	Epinastine HCl Epinastine (WAL-801CL) 是一种抗组胺剂和肥大细胞稳定剂，用于眼药水治疗过敏性结膜炎。
S2494	Olopatadine HCl Olopatadine HCl 是一种组胺抑制剂，也是肥大细胞稳定剂，抑制组胺释放，IC50为559 μM。
S4140	Buclizine HCl Buclizine HCl (UCB-4445)是哌嗪衍生物家族的antihistamine（抗组胺药）和anticholinergic（抗胆碱药）。
S3052	Rupatadine Fumarate Rupatadine Fumarate是一种PAFR和组胺(H1)受体抑制剂，K_i分别为550 nM和102 nM。
S2024	Ketotifen Fumarate Ketotifen Fumarate 是Ketotifen的富马酸盐，是H1抗组胺剂，也是肥大细胞稳定剂。	Environ Toxicol Chem,2021, 10.1002/etc.5018
S3183	Amitriptyline HCl Amitriptyline HCl 是一种 serotonin transporter (SERT) 和 norepinephrine transporter (NET) 的抑制剂，其Ki值分别为3.45 nM和13.3 nM。Amitriptyline HCl 还可抑制histamine receptor H1、histamine receptor H4、5-HT2 和 sigma 1 receptor，对应的Ki值分别是0.5 nM、7.31 nM、235 nM和287 nM。Amitriptyline 是一种三环抗抑郁药物。	Environ Toxicol Chem,2021, 10.1002/etc.5018 PLoS Pathog,2020, 16;16(3):e1008341 Sci Rep,2018, 8(1):15753
S3186	Azatadine dimaleate Azatadine (SCH10649) 是一种抗组胺和抗胆碱能药物，IC50分别为6.5nM和10nM。	Pharmaceuticals (Basel),2019, 12(4)
S4131	Levodropropizine Levodropropizine可以抗过敏并抑制组胺受体，通过干扰外围感觉神经末端的刺激活化作用以及调节参与咳嗽反射的神经肽来减轻咳嗽。
S5947	Amitriptyline Amitriptyline (MK-230, N-750, Ro41575) 是一种三环抗抑郁药，具有止痛效果，被广泛用于治疗抑郁和神经性疼痛。Amitriptyline 是一种 serotonin transporter (SERT) 和 norepinephrine transporter (NET) 的抑制剂，其Ki值分别为3.45 nM和13.3 nM。Amitriptyline 还可抑制histamine receptor H1、histamine receptor H4、5-HT2 和 sigma 1 receptor，对应的Ki值分别是0.5 nM、7.31 nM、235 nM和287 nM。该产品呈胶状。	Cancers (Basel),2019, 11(12)
S4672	Dimenhydrinate Dimenhydrinate是一种用于治疗由晕动症引起的恶心、呕吐、头晕的药物。
S2308	Hesperetin Hesperetin是一种生物类黄酮，更具体而言，是一种二氢黄酮。	Carcinogenesis,2020, 41(7):993-1004
S4696	CarbinoxaMine Maleate Carbinoxamine maleate是一种组胺-H1受体阻滞剂，具有抗组胺和反副交感神经生理作用。	Am J Physiol Lung Cell Mol Physiol,2019, 316(1):L20-L34 Anticancer Res,2019, 39(7):3767-3775
S4240	Doxylamine Succinate Doxylamine succinate竞争性抑制组胺H1受体，具有镇静和抗胆碱作用。	Environ Toxicol Chem,2021, 10.1002/etc.5018
S3176	Betahistine 2HCl Betahistine (PT-9) 是一种组胺H3受体抑制剂，IC50为1.9 μM。

目录号	产品描述	文献引用	实验数据
S1847	Clemastine (HS-592) fumarate Clemastine Fumarate (HS-592, Meclastine)是一种选择性组胺H1受体拮抗剂，IC50为3 nM。Clemastine 可通过 mTOR 信号通路来刺激自噬。	Neuron, 2021, S0896-6273(21)00352-4 Neurosci Bull, 2021, 10.1007/s12264-021-00745-1 Nat Neurosci, 2020, 10.1038/s41593-020-0588-8	Detection of P2X7 receptor and histamine receptor H1 (HRH1) in hippocampus and mPFC. (A–F) CUMS treatment upregulated the protein expression of the purinergic receptor P2X, ligand-gated ion channel 7 (P2X7R) in both hippocampus and mPFC subregions. In the meantime, continuous intraperitoneal administration of clemastine protected mice from stress-induced upregulation of P2X7R in the hippocampus rather than mPFC. There is no statistical alteration of HRH1 expression in both subfields of hippocampus and mPFC, even when the mice were subjected to stress stimulation or clemastine injection (n = 4 for (A–F), p < 0.05, *p < 0.01).
S1245	Latrepirdine 2HCl Latrepirdine具有口服活性及神经活性，可以作为包括histamine receptors, GluR, 和5-HT receptors在内的多个药物靶点的拮抗剂，用作抗组织胺的药物。
S1358	Loratadine (SCH29851) Loratadine (SCH29851) 是一种选择性的histamine H1 receptor拮抗剂，用于治疗过敏。同时还是一种选择性的B(0)AT2抑制剂，其IC50为 4 μM。	EMBO Mol Med, 2021, e13929 Adv Ther (Weinh), 2020, 2000034 Cell Syst, 2019, 8(2):97-108
S3037	Bepotastine Besilate Bepotastine Besilate (TAU 284)是一种非镇静作用的，选择性的组胺1 (H1)受体拮抗剂，pIC50为5.7。	Hum Cell, 2021, 10.1007/s13577-021-00579-z Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S1382	Mianserin HCl Mianserin (ORG GB-94) l是一种四环类抗抑郁药。	Immunity, 2019, 50(5):1163-1171
S5196^New	Promethazine Promethazine 是一种有效的 histamine H1 receptor 的拮抗剂。Promethazine 是可用于过敏性疾病、恶心和呕吐、晕车和镇静的管理和治疗的药物。异丙嗪具有抗寄生虫的特性。
S5864^New	Levocetirizine Levocetirizine (LCZ, (R)-Cetirizine) 是Cetirizine的R-对映体，是一种 histamine H(1) receptor 的拮抗剂。
S2552	Azelastine HCl Azelastine HCl是有效的，第二代选择性组胺拮抗剂。	Theranostics, 2021, 11(4):1828-1844 Anticancer Res, 2019, 39(7):3767-3775
S1801	Ranitidine Hydrochloride Ranitidine (AH19065) 是组胺H2-受体拮抗剂，IC50为3.3±1.4 μM。	bioRxiv, 2021, 10.1101/2021.04.29.441931
S1866	Diphenhydramine HCl Diphenhydramine HCl 是组胺H1拮抗剂，可用于止吐止咳，治疗皮肤病和皮肤瘙痒，过敏反应，用作安眠药，治疗帕金森，作为感冒制剂一种组分。	Int J Pharm, 2019, 560:294-305 Anticancer Res, 2019, 39(7):3767-3775 Sci Rep, 2017, 7(1):8491
S4012	Desloratadine Desloratadine (SCH-34117, NSC 675447)是一种有效的人组胺H1受体拮抗剂，IC50为51nM.	Anticancer Res, 2019, 39(7):3767-3775
S1816	Chlorpheniramine Maleate Chlorpheniramine Maleate (Chlorpheniramine maleate, Chlorphenamine, NCI-C55265)是一种组胺H1受体拮抗剂，IC50为12 nM。	Anticancer Res, 2019, 39(7):3767-3775
S2813	Ciproxifan Maleate Ciproxifan (FUB 359) 是一种高效的，选择性的histamin H3-receptor拮抗剂，IC50为9.2 nM，作用于其他受体亚型具有低亲和力。	Acta Pharmacol Sin, 2020, 10.1038/s41401-020-00548-6 Oncol Lett, 2018, 16(4):4921-4928
S1986	Meclizine 2HCl Meclizine (NSC 28728) 是histamine H1 receptor拮抗剂,用于治疗恶心，晕动病，也是mCAR（组成型雄烷受体激动剂配体）激动剂配体，也是hCAR的反向激动剂。	Anticancer Res, 2019, 39(7):3767-3775 Front Pharmacol, 2017, 8:693
S2107	Mizolastine Mizolastine (SL 850324) 是一种组胺H1受体拮抗剂，IC50为47 nM，用于治疗花粉症（季节性过敏性鼻炎）、荨麻疹和其他过敏性反应。
S1845	Cimetidine Cimetidine (SKF-92334) 是一种组胺类似物，竞争性地抑制组胺结合到组胺H2受体。	Cell Rep, 2021, 34(10):108832 bioRxiv, 2021, 10.1101/2021.04.29.441931 Anticancer Res, 2019, 39(7):3767-3775
S2065	Lafutidine Lafutidine (FRG-8813)是一种新开发的组胺H(2)受体拮抗剂，抑制胃酸分泌。
S1890	Nizatidine Nizatidine是一种组胺H2受体拮抗剂，作用于AChE，IC50为6.7 nM。	bioRxiv, 2021, 10.1101/2021.04.29.441931 Anticancer Res, 2019, 39(7):3767-3775
S3146	Tripelennamine HCl Tripelennamine (Pyribenzamine) 是一种广泛使用的组胺1拮抗剂(H1拮抗剂)，抑制PhIP糖脂化，IC50为30 μM。
S2044	Cyproheptadine HCl Cyproheptadine HCl 是Cyproheptadine的盐酸盐形式，是组胺受体拮抗剂，作用于5-HT₂受体，IC50为0.6 nM。	Cell Rep, 2020, 21;31(3):107548 Vet Med Sci, 2020, 10.1002/vms3.336 Anticancer Res, 2019, 39(7):3767-3775
S4026	Hydroxyzine 2HCl Hydroxyzine 2HCl抑制[³H]pyrilamine或[³H]desloratadine与人源组胺H1受体的结合， IC50分别为10 nM和19 nM。	Anticancer Res, 2019, 39(7):3767-3775 Nature, 2018, 560(7718):372-376	a, Quantification of sterol levels in OPCs (oligodendrocyte progenitor cells) treated with the indicated molecules at 2 μM. b, Quantification of sterol levels in OPCs treated with the indicated previously reported enhancers of oligodendrocyte formation (n = 2 wells per condition except DMSO, n = 6). Representative of two independent experiments; for concentrations, see Extended Data Fig. 6g. c, Quantification of EBP enzymatic activity in a biochemical assay. All treatments 10 μM. n = 3 independent enzymatic assays, except DMSO, n = 5. Bars indicate mean; error bars indicate s.d. Sigma H127, p-fluorohexahydro-sila-difenidol.
S4262	Ebastine Ebastine是强效的H1型组氨酸受体（H1-histamine receptor）拮抗剂，被用来治疗过敏性疾病。
S2585	Brompheniramine hydrogen maleate Brompheniramine hydrogen maleate是一种组胺H1受体拮抗剂。	Anticancer Res, 2019, 39(7):3767-3775
S2905	JNJ-7777120 JNJ-7777120是第一个，有效的，选择性非咪唑histamine H4 receptor拮抗剂，K_i为4.5 nM，比作用于其他组胺受体选择性高1000倍以上。	J Assoc Res Otolaryngol, 2021, 10.1007/s10162-021-00803-5 Neuropharmacology, 2020, 168:108028 Mol Ther Methods Clin Dev, 2018, 11:83-91
S4008	Pemirolast potassium Pemirolast potassium (BMY26517) 是一种组胺H1拮抗剂和肥大细胞稳定剂，用作抗过敏药。	Front Microbiol, 2020, 10:2936 Anticancer Res, 2019, 39(7):3767-3775
S4849	Levocetirizine Dihydrochloride Levocetirizine (Xyzal, (-)-Cetirizine) 是cetirizine的活性(R)-对映异构体，是新型二代histamine H1拮抗剂。	Anticancer Res, 2019, 39(7):3767-3775
S5670	Chloropyramine hydrochloride Chloropyramine hydrochloride (Halopyramine) is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects.
S5659	Emedastine Emedastine is a potent, high affinity histamine H1-receptor-selective antagonist with Ki of 1.3 ±0.1 nM for H1-receptors while considerably weaker at H2- (K1 = 49,067 ± 11,113 nM) and H3-receptors (Ki = 12,430 ± 1,282 nM).
S4139	Cyclizine 2HCl Cyclizine 2HCl是一种哌嗪衍生物，具有Histamine H1(组胺H1)受体拮抗剂活性。
S5940	Bepotastine Bepotastine是一种非镇静的、选择性histamine 1 (H1) receptor拮抗剂。
S4625	Alcaftadine Alcaftadine (Lastacaft, R89674) 是H1受体的高亲和力配体，pKi为8.5。Alcaftadine还是H2和H4受体的拮抗剂，对H3受体没有亲和力。
S4045	Pheniramine Maleate Pheniramine Maleate 是一种抗组胺剂，具有抗胆碱能特性，用于治疗花粉症或荨麻疹等过敏性疾病。
S5479	Cloperastine hydrochloride Cloperastine (HT-11) is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity.
S5656	Diphenylpyraline hydrochloride Diphenylpyraline hydrochloride is the hydrochloride salt form of diphenylpyraline, which is an antihistamine used in the treatment of allergic rhinitis, hay fever, and allergic skin disorders.
S1880	Roxatidine Acetate HCl Roxatidine Acetate HCl是特异性的，竞争性的组胺H2受体拮抗剂，IC50为3.2 μM，抑制胃酸分泌和溃疡形成。
S5718	Acrivastine Acrivastine is an antihistamine medicine that relieves the symptoms of allergies.
S5447	Triprolidine Hydrochloride Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.
S5647	Emedastine Difumarate Emedastine Difumarate (Rapimine, Emedastine fumarate) is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity.
S5018	Mebhydrolin napadisylate Mebhydrolin Napadisylate (Diazoline, Diazolin, Incidal, Omeril)是一种抗组胺类药物，用于治疗过敏。
S8598	S 38093 S 38093是histamine H3拮抗剂/反向激动剂，对大鼠、小鼠和人源H3受体具有中等亲和力（Ki值分别为8.8、1.44、1.2 μM），对其他组胺能受体没有亲和力。
S5926	Pitolisant hydrochloride Pitolisant (Tiprolisant, BF-2649)是一种高亲和力的、竞争性H3受体拮抗剂，Ki为0.16 nM。同时也是组胺H3受体的反向激动剂（EC50=1.5 nM）。
S0398	Astemizole Astemizole (R 43512)是一种 histamine H1-receptor 拮抗剂，其IC50值为4.7 nM。Astemizole 还是一种有效的 ether à-go-go 1 (Eag1) 和 Eag-related gene (Erg) potassium channels 的抑制剂。Astemizole 具有抗肿瘤和止痒的作用。
S5649	Hydroxyzine pamoate Hydroxyzine Pamoate is the pamoate salt form of hydroxyzine, a synthetic piperazine histamine H1-receptor antagonist with anti-allergic, antispasmodic, sedative, anti-emetic and anti-anxiety properties.	Anticancer Res, 2019, 39(7):3767-3775
S3721	Bilastine Bilastine是一种新型耐受的、无镇静作用的抗组胺剂，针对H1 receptor。其效果迅速并持久。
S5662	Ranitidine Ranitidine is an H2 histamine receptor antagonist that works by blocking histamine and thus decreasing the amount of acid released by cells of the stomach.	bioRxiv, 2021, 10.1101/2021.04.29.441931 Anticancer Res, 2019, 39(7):3767-3775
S3120	Doxepin HCl Doxepin是一种精神药物，是一种三环类抗抑郁药，具有抗焦虑活性。
S4353	Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
S6435	Mequitazine Mequitazine (LM-209)是histamine H1拮抗剂，可与组胺竞争性结合胃肠道、血管和呼吸道效应细胞上正常H1受体。
S2078	Famotidine Famotidine (MK208)是组胺H2受体拮抗剂，IC50为0.6 mM，常用来治疗胃灼热，GERD，溃疡和其他消化系统不良情况。	bioRxiv, 2021, 10.1101/2021.04.29.441931 Anticancer Res, 2019, 39(7):3767-3775
S6469	Thonzylamine Thonzylamine (Neohetramine) 是抗组胺剂和抗胆碱能药。
S4293	Promethazine HCl Promethazine HCl 是一种强效的histamine H₁受体拮抗剂,被用作镇静和抗过敏的药物。	bioRxiv, 2020, 2020/9/20.4.7.30734 Anticancer Res, 2019, 39(7):3767-3775 Chem Biol Interact, 2019, 315:108888

目录号	产品描述	文献引用
S1357	Lidocaine Lidocaine (Alphacaine)是一种选择性的，逆向外周组胺H1受体激动剂，IC50大于32 μM。	Exp Ther Med, 2021, 21(5):424 Nat Biomed Eng, 2020, 4(3):286-297 J Cell Biochem, 2019, 120(10):16533-16542
S3968	Histamine Histamine, an organic nitrogenous compound, is involved in local immune responses regulating physiological function in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. It is a potent H1 and H2 receptor agonist.	Life Sci, 2019, 227:74-81
S4117	Histamine Phosphate Histamine Phosphate直接作用于血管，扩张H1和H2受体介导的动脉和毛细血管。
S4118	Histamine 2HCl Histamine 2HCl是一种有机氮化合物，通过对组胺1/2的刺激来对哺乳类大脑中靶细胞起作用。	Front Pharmacol, 2017, 8:667
S6612	Betazole Dihydrochloride Betazole Dihydrochloride (Ametazole, 2-(3-Pyrazolyl)ethanamine)是histamine H2激动剂，在临床上用于检测胃分泌功能。
S5498	Betahistine mesylate Betahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator.
S6569	VUF10460 VUF10460是histamine H4 receptor激动剂。
S5619	Betahistine Betahistine is an antivertigo drug that primarily acts as a histamine H1 agonist.
S4382	Pyrilamine Maleate Pyrilamine Maleate (Mepyramine) is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling.

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