您当前的位置:

信号通路

-收起全部分类

Histamine Receptor

Histamine Receptor相关产品(77)
货号 产品名 中文名称 产品描述
SJ-MX3470 Pitolisant 替洛利生 Pitolisant (formerly BF2.649; Tiprolisant; BF2649; Ciproxidine; Wakix) is a novel, potent and selective nonimidazole inverse agonist of the recombinant human histamine H3 receptor with Ki of 0.16 nM. It has been approved in 2019 for the treatment of excessive daytime sleepiness in adults with narcolepsy. Histamine H3 receptor inverse agonists are known to enhance the activity of histaminergic neurons in brain and thereby promote vigilance and cognition. On the stimulation of guanosine 5'-O-(3-[35S]thio)triphosphate binding to this receptor, BF2.649 behaved as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity approximately 50% higher than that of ciproxifan. Its in vitro potency was approximately 6 times lower at the rodent receptor. In mice, the oral bioavailability coefficient, i.e., the ratio of plasma areas under the curve after oral and i.v. administrations, respectively, was 84%. BF2.649 dose dependently enhanced tele-methylhistamine levels in mouse brain, an index of histaminergic neuron activity, with an ED50 value of 1.6 mg/kg p.o., a response that persisted after repeated administrations for 17 days. In rats, the drug enhanced dopamine and acetylcholine levels in microdialysates of the prefrontal cortex. In cats, it markedly enhanced wakefulness at the expense of sleep states and also enhanced fast cortical rhythms of the electroencephalogram, known to be associated with improved vigilance. On the two-trial object recognition test in mice, a promnesiant effect was shown regarding either scopolamine-induced or natural forgetting. These preclinical data suggest that BF2.649 is a valuable drug candidate to be developed in wakefulness or memory deficits and other cognitive disorders.
SJ-MX3635 Pitolisant hydrochloride 替洛利生盐酸盐 Pitolisant hydrochloride (formerly also known as BF2.649; BF2649; Ciproxidine; Wakix) is a potent, cell-permeable and selective histamine H3 receptor inverse agonist (EC50 = 1.5 nM, Ki = 0.16 nM). BF2649 displays nootropic effects in cognitive disorders; reduces locomotor hyperactivity induced by methamphetamine.
SJ-MX3763 Cyclizine Cyclizine is a novel and potent histamine H1 receptor antagonist.
SJ-MX3769 Acrivastine 阿伐斯汀 Acrivastine (BW825C) is an antihistamine with reduced sedating potential.
SJ-MX2522 Bilastine 比拉斯汀 Bilastine is a novel and potent antihistamine drug.
SJ-MX2641 Lodoxamide tromethamine 洛度沙胺氨丁三醇 Lodoxamide tromethamide (U-42585E), the Tromethamide salt of Lodoxamide, is an antiallergic drug acting as a potent GPR35 agonist with an EC50 of 1.61 nM in a β-arrestin-2 interaction assay using CHO-K1 cells expressing the human receptor. It inhibits histamine release induced by compound 48/80, anti-IgE, or A23187 in isolated rat peritoneal mast cells (IC50s = 0.1-50 µM) and inhibits A23187-induced calcium influx in mast cells. It reduces antigen-induced histamine release from rat conjunctival tissue by 46% in vitro when used at a concentration of 10 µg/ml. Lodoxamine (0.1 and 10%, w/v) reduces the immediate hypersensitivity response in rat conjunctiva in vivo in a dose-dependent manner and reduces mast cell degranulation in a topical ovalbumin challenge. Formulations containing lodoxamide have been used in the treatment of vernal conjunctivitis and keratitis.
SJ-MX1537 Thonzylamine Thonzylamine 是一种具有口服活性的 H1 组胺受体拮抗剂,具有良好的抗组胺和抗过敏特性。Thonzylamine 可用于过敏性疾病,鼻充血,过敏性结膜炎和其他过敏性疾病的研究。
SJ-MX2129 Desloratadine (Sch34117) 地氯雷他定 Desloratadine (Sch34117) 是非镇静 H1 抗组胺药 Loratadine 的主要口服代谢物。Desloratadine 是一种选择性 H1 受体拮抗剂,具有抗过敏和抗炎活性。
SJ-MX2480 Chlorpheniramine maleate 马来酸氯苯那敏 Chlorpheniramine maleate (Piriton; Chlortrimeton; Deconamine; Neorestamin; NCIC-55265; NCIC55265; Chlo-Amine; Chlor-100; Chlor-Trimeton), the Maleate salt of Chlorpheniramine, is a potent and 1st-generation alkylamine-based histamine H1 receptor antagonist with anti-allergic effects. It inhibits histamine H1 receptor with an IC50 of 12 nM. Chlorpheniramine has been widely used for the prevention and treatment of the symptoms of allergic conditions such as rhinitis and urticaria.
SJ-MX2497 Alcaftadine 阿卡他定 Alcaftadine is an H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.
SJ-MX2514 Azatadine dimaleate 马来酸阿扎他定 Azatadine dimaleate (SCH10649; SCH-10649; Idulamine; Idulian; Lergocil; Optimine; Zadine), the dimaleate salt of azatadine, is a potent histamine and cholinergic inhibitor that has been approved for treating allergic rhinitis and chronic urticaria. It inhibits histamine and cholinergic receptors with IC50s of 6.5 nM and 10 nM, respectively.
SJ-MX2525 Bepotastine besilate 苯磺酸贝托司汀;苯磺酸贝他斯汀;苯磺酸贝托斯汀;苯磺酸贝他司汀 Bepotastine besilate (bepotastine besylate; TAU-284; TAU284; Bepreve; Talion), the besylate salt of Bepotastine, is a 2nd generation, non-sedating, and selective antagonist of histamine 1 (H1) receptor with a pIC50 of 5.7. Bepostatine besilate has been approved to treat allergic rhinitis and urticaria and pruritus. Bepotastine besilate inhibits the action of histamine by blocking histamine H1 receptors, antagonising the vasoconstrictor, and to a lesser extent, the vasodilator effects of histamine. Mast cell stabilisers inhibit degranulation and consequently the release of histamine by interrupting the normal chain of intracellular signals. The brand of Bepostatine besilate is Talion.
SJ-MX2539 Mianserin hydrochloride 盐酸米安色林 Mianserin hydrochloride (formerly ORG GB-94; ORG-GB 94; Depnon, Lantanon, Lerivon, Lumin, Norval, Tolvon), the hydrochloride salt of mianserin which is a psychoactive tetracyclic compound, is a novel and potent antagonist (inverse agonist) of H1 histamine receptor and 5-HT serotonin receptors used for the treatment of depression. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.
SJ-MX2542 Brompheniramine maleate 马来酸溴苯那敏 Brompheniramine (Bromfed, Dimetapp, Bromfenex, Dimetane, BPN, Lodrane), the maleate salt of Brompheniramine which is an OTC drug for cold and allergic rhinitis, is a first-generation antagonist of the histamine H1 receptors. It has been used for the treatment of common cold and allergic rhinitis, such as runny nose, itchy eyes, watery eyes, and sneezing.
SJ-MX2544 Buclizine dihydrochloride Buclizine hydrochloride (AH-2526, UCB 4445; AH2526;UCB-4445, Buclina, Longifene, Posdel, Vibazine), the hydrochloride salt of buclizine which is used for motion sickness, is a piperazine derivative and a sedating antihistamine with antimuscarinic and moderate sedative action. Buclizine has been used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in diseases affecting the vestibular apparatus.
SJ-MX2552 Carbinoxamine maleate salt Carbinoxamine maleate salt is a antihistamine and anticholinergic agent. It was first launched in the United States by the McNeil Corporation under the brand name Clistin. It is now available under the brand name Palgic as 4 mg tablets or 4 mg/5 mL liquid. Carbinoxamine is a histamine antagonist, specifically an H1-antagonist.
SJ-MX2590 Doxepin hydrochloride 盐酸多塞平 Doxepin hydrochloride is a highly potent Histamine H1 Receptor (histamine H1) antagonist. Doxepin hydrochloride also binds to histamine H4 receptor. Doxepin hydrochloride is an inhibitor of AR and mAChR. Doxepin hydrochloride is a dibenzoxepin analogue and tricyclic antidepressant with antipruritic and sedative activities. Doxepin also has antagonistic effects on histamine (H1 and H2), 5-HT2, alpha-1 adrenergic, and muscarinic receptors. The antipruritic effect of this agent is the result mediated through inhibition of histamine receptors.
SJ-MX2597 Ebastine 依巴斯汀 Ebastine (formerly LAS-W 090; RP-64305; LAS W090; RP64305; Ebast, Ebatin, Ebatrol, Atmos, Ebet, Kestine, KestineLIO) is a long-acting and selective H1-histamine receptor antagonist used for the treatment of allergic conditions. Ebastine has low potential for causing drowsiness. It does not cross the BBB-blood–brain barrier and thus has a low incidence of causing CNS side effects.
SJ-MX2635 Lafutidine 拉呋替丁 Lafutidine (formerly FRG-8813; FRG8813; trade name: Protecadin; Stogar) is a 2nd-generation histamine H2 receptor antagonist used to treat gastric ulcers, duodenal ulcers, and wounds in the stomach associated with chronic gastritis. Lafutidine acts by inhibiting the secretion of gastric acid. It has been marketed in Japan and India.
SJ-MX2676 Nizatidine 尼扎替丁 Nizatidine (Tazac, Axid, LY-139037, LY 139037, LY139037) is a potent histamine H2 receptor antagonist used in the treatment of peptic ulcer disease and gastroesophageal reflux disease. It inhibits histamine H2 receptor with an IC50 of 0.9 nM.