Histamine Receptor

信号通路图

研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S4199	Antazoline HCl	14 mg/mL	40 mg/mL	4 mg/mL
S1291	Cetirizine DiHCl	92 mg/mL	92 mg/mL	<1 mg/mL
S3208	Fexofenadine HCl	2 mg/mL	107 mg/mL	107 mg/mL
S4253	Epinastine HCl	57 mg/mL	57 mg/mL	57 mg/mL
S2494	Olopatadine HCl	13 mg/mL	75 mg/mL	8 mg/mL
S4140	Buclizine HCl	<1 mg/mL	0.2 mg/mL	<1 mg/mL
S3052	Rupatadine Fumarate	<1 mg/mL	9 mg/mL	13 mg/mL
S2024	Ketotifen Fumarate	<1 mg/mL	8 mg/mL	<1 mg/mL
S3186	Azatadine dimaleate	105 mg/mL	105 mg/mL	<1 mg/mL
S4131	Levodropropizine	15 mg/mL	47 mg/mL	47 mg/mL
S2308	Hesperetin	<1 mg/mL	60 mg/mL	<1 mg/mL
S4696	CarbinoxaMine Maleate	81 mg/mL	81 mg/mL	81 mg/mL
S4240	Doxylamine Succinate	78 mg/mL	78 mg/mL	78 mg/mL
S3176	Betahistine 2HCl	38 mg/mL	38 mg/mL	1 mg/mL
S1847	Clemastine Fumarate	<1 mg/mL	35 mg/mL	<1 mg/mL
S1245	Latrepirdine 2HCl	<1 mg/mL	24 mg/mL	13 mg/mL
S1358	Loratadine	<1 mg/mL	17 mg/mL	76 mg/mL
S3037	Bepotastine Besilate	<1 mg/mL	109 mg/mL	<1 mg/mL
S1382	Mianserin HCl	30 mg/mL	60 mg/mL	21 mg/mL
S5926	Pitolisant hydrochloride	66 mg/mL	66 mg/mL	66 mg/mL
S5649	Hydroxyzine pamoate	-1 mg/mL	100 mg/mL	-1 mg/mL
S5662	Ranitidine	-1 mg/mL	63 mg/mL	-1 mg/mL
S5670	Chloropyramine hydrochloride	-1 mg/mL	65 mg/mL	-1 mg/mL
S5656	Diphenylpyraline hydrochloride	-1 mg/mL	63 mg/mL	-1 mg/mL
S5718	Acrivastine	-1 mg/mL	10 mg/mL	-1 mg/mL
S5447	Triprolidine Hydrochloride	-1 mg/mL	62 mg/mL	-1 mg/mL
S5479	Cloperastine hydrochloride	-1 mg/mL	73 mg/mL	-1 mg/mL
S5018	Mebhydrolin napadisylate	-1 mg/mL	8 mg/mL	-1 mg/mL
S4849	Levocetirizine Dihydrochloride	92 mg/mL	92 mg/mL	7 mg/mL
S2552	Azelastine HCl	35 mg/mL	28 mg/mL	42 mg/mL
S1801	Ranitidine Hydrochloride	70 mg/mL	70 mg/mL	<1 mg/mL
S1866	Diphenhydramine HCl	58 mg/mL	58 mg/mL	58 mg/mL
S4012	Desloratadine	<1 mg/mL	26 mg/mL	62 mg/mL
S1816	Chlorpheniramine Maleate	78 mg/mL	78 mg/mL	78 mg/mL
S2813	Ciproxifan Maleate	1 mg/mL	54 mg/mL	54 mg/mL
S1986	Meclizine 2HCl	<1 mg/mL	4 mg/mL	<1 mg/mL
S2107	Mizolastine	<1 mg/mL	<1 mg/mL	<1 mg/mL
S1845	Cimetidine	<1 mg/mL	51 mg/mL	3 mg/mL
S2065	Lafutidine	<1 mg/mL	86 mg/mL	13 mg/mL
S1890	Nizatidine	28 mg/mL	66 mg/mL	18 mg/mL
S3146	Tripelennamine HCl	58 mg/mL	2 mg/mL	1 mg/mL
S2044	Cyproheptadine HCl	<1 mg/mL	65 mg/mL	20 mg/mL
S4026	Hydroxyzine 2HCl	90 mg/mL	90 mg/mL	15 mg/mL
S4262	Ebastine	<1 mg/mL	4 mg/mL	11 mg/mL
S2585	Brompheniramine hydrogen maleate	46 mg/mL	87 mg/mL	18 mg/mL
S2905	JNJ-7777120	<1 mg/mL	56 mg/mL	8 mg/mL
S4008	Pemirolast potassium	53 mg/mL	<1 mg/mL	<1 mg/mL
S4139	Cyclizine 2HCl	68 mg/mL	7 mg/mL	<1 mg/mL
S4625	Alcaftadine	<1 mg/mL	28 mg/mL	61 mg/mL
S4045	Pheniramine Maleate	71 mg/mL	71 mg/mL	71 mg/mL
S1880	Roxatidine Acetate HCl	77 mg/mL	77 mg/mL	12 mg/mL
S8598	S 38093	<1 mg/mL	57 mg/mL	57 mg/mL
S3721	Bilastine	<1 mg/mL	1 mg/mL	<1 mg/mL
S3120	Doxepin HCl	63 mg/mL	63 mg/mL	63 mg/mL
S2078	Famotidine	<1 mg/mL	67 mg/mL	<1 mg/mL
S4293	Promethazine HCl	64 mg/mL	64 mg/mL	34 mg/mL
S5498	Betahistine mesylate	-1 mg/mL	65 mg/mL	-1 mg/mL
S1357	Lidocaine	9 mg/mL	47 mg/mL	47 mg/mL
S3968	Histamine	-1 mg/mL	22 mg/mL	-1 mg/mL
S4117	Histamine Phosphate	42 mg/mL	<1 mg/mL	<1 mg/mL
S4118	Histamine 2HCl	37 mg/mL	3 mg/mL	<1 mg/mL

特异性亚型抑制剂

Histamine Receptor抑制剂（64）
新Histamine Receptor产品

产品目录	产品描述	文献引用	实验数据
S4199^New	Antazoline HCl Antazoline HCl是第一代抗组胺药，与组胺H1受体结合，抑制内源性组胺的作用。
S1291	Cetirizine DiHCl Cetirizine DiHCl是一种抗组胺剂。	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 HCl抑制组胺H1受体，IC50为246 nM。	Sci Rep, 2016, 10.1038/srep25694
S4253	Epinastine HCl Epinastine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。
S3186	Azatadine dimaleate Azatadine dimaleate是一种抗组胺和抗胆碱能药物，IC50分别为6.5nM和10nM。
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。
S2308	Hesperetin Hesperetin是一种生物类黄酮，更具体而言，是一种二氢黄酮。
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。
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。
S3176	Betahistine 2HCl Betahistine 2HCl是一种组胺H3受体抑制剂，IC50为1.9 μM。
S1847	Clemastine Fumarate Clemastine Fumarate是一种选择性组胺H1受体拮抗剂，IC50为3 nM。	Neurosci Bull, 2015, 31(5):617-25 Front Cell Neurosci, 2018, 12:412	(B,C) Analysis indicates the total distance was unchanged between cuprizone-exposed mice with or without clemastine treatment (B), but the distance in the central field decreased upon 6-week exposure to cuprizone, while clemastine gradually rescued the behavioral change (C). *P <0.05, n = 10 animals/group.
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 Loratadine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。
S3037	Bepotastine Besilate Bepotastine Besilate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。
S1382	Mianserin HCl Mianserin HCl是一种四环类抗抑郁药。
S5926^New	Pitolisant hydrochloride Pitolisant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）。
S5649^New	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.
S5662^New	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.
S5670^New	Chloropyramine hydrochloride Chloropyramine hydrochloride is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects.
S5656^New	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.
S5718^New	Acrivastine Acrivastine is an antihistamine medicine that relieves the symptoms of allergies.
S5659^New	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).
S5647^New	Emedastine Difumarate Emedastine Difumarate is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity.
S5447^New	Triprolidine Hydrochloride Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.
S5479^New	Cloperastine hydrochloride Cloperastine is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity.
S5018^New	Mebhydrolin napadisylate Mebhydrolin Napadisylate是一种抗组胺类药物，用于治疗过敏。
S4849^New	Levocetirizine Dihydrochloride Levocetirizine是cetirizine的活性(R)-对映异构体，是新型二代histamine H1拮抗剂。
S2552	Azelastine HCl Azelastine HCl是有效的，第二代选择性组胺拮抗剂。
S1801	Ranitidine Hydrochloride Ranitidine是组胺H2-受体拮抗剂，IC50为3.3±1.4 μM。
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。	Sci Rep, 2017, 7(1):8491
S4012	Desloratadine Desloratadine是一种有效的人组胺H1受体拮抗剂，IC50为51nM.
S1816	Chlorpheniramine Maleate Chlorpheniramine Maleate是一种组胺H1受体拮抗剂，IC50为12 nM。
S2813	Ciproxifan Maleate Ciproxifan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。
S1986	Meclizine 2HCl Meclizine 2HCl 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。
S2107	Mizolastine Mizolastine 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 是一种组胺类似物，竞争性地抑制组胺结合到组胺H2受体。
S2065	Lafutidine Lafutidine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。
S3146	Tripelennamine HCl Tripelennamine HCl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。
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。	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。
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。
S4008	Pemirolast potassium Pemirolast potassium是一种组胺H1拮抗剂和肥大细胞稳定剂，用作抗过敏药。
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。
S4625	Alcaftadine Alcaftadine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。
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。
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。
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。
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。
S2078	Famotidine Famotidine 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。
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。
S5619^New	Betahistine Betahistine is an antivertigo drug that primarily acts as a histamine H1 agonist.
S5498^New	Betahistine mesylate Betahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator.
S1357	Lidocaine Lidocaine是一种选择性的，逆向外周组胺H1受体激动剂，IC50大于32 μM。	Antiviral Res, 2016, 132:38-45
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.
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。

研究领域

产品类型

Histamine Receptor

信号通路图

研究领域

特异性亚型抑制剂