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Anti-infection

Antibiotic Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HCV Protease HIV HIV Integrase HIV Protease HSV Influenza Virus Orthopoxvirus Parasite TMV Reverse Transcriptase RSV SARS-CoV Virus Protease
Apoptosis

Apoptosis Bcl-2 Family Caspase c-Myc Ferroptosis FKBP IAP Family MDM-2/p53 PKD Necroptosis Pyroptosis RIP kinase Thymidylate Synthase TNF Receptor TRADD
Autophagy

Autophagy FKBP LRRK2 Mitophagy OGA ULK
Cell Cycle/DNA Damage

Antifolate APC ATM/ATR Aurora Kinase BMI-1 Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA/RNA Synthesis DNA-PK Early 2 Factor (E2F) Eukaryotic Initiation Factor (eIF) GAK G-quadruplex HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 DNA Stain Nucleoside Antimetabolite/Analog Nur77 p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 Cyclin G-associated Kinase (GAK) Nucleoside Antimetabolite/AnalogOrthopoxvirus ROCK ATF6 Haspin Kinase Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
Cytoskeletal Signaling

Arp2/3 Complex Dynamin Gap Junction Protein Integrin Kinesin Microtubule/Tubulin Mps1 Myosin PAK ROCK
Endocrinology/Hormones

Adrenergic Receptor Androgen Receptor Angiotensin-converting Enzyme (ACE) Aromatase Cholecystokinin Receptor TSH Receptor Estrogen Receptor/ERR GHSR Glucocorticoid Receptor GNRH Receptor Mineralocorticoid Receptor Opioid Receptor PGD synthase PGE synthase Progesterone Receptor Thyroid Hormone Receptor
Epigenetics

AMPK Aurora Kinase DNA Methyltransferase Epigenetic Reader Domain FTO HDAC Histone Acetyltransferase Histone Demethylase Histone Methyltransferase MicroRNA PARP PKC Protein Arginine Deiminase Methionine Adenosyltransferase (MAT) Sirtuin
GPCR/G Protein

5-HT Receptor Adenosine Receptor Adenylate Cyclase (AC) Adiponectin Receptor Adrenergic Receptor Angiotensin Receptor Bombesin Receptor Bradykinin Receptor Cannabinoid Receptor CaSR CCR CGRP Receptor Cholecystokinin Receptor CRFR CXCR TSH Receptor Neuropeptide Y Receptor Dopamine Receptor EBI2/GPR183 Endothelin Receptor Formyl peptide receptor (FPR) GHSR Glucagon Receptor Glucocorticoid Receptor GNRH Receptor GPCR19 GPR109A GPR119 GPR120 GPR139 GPR27 GPR40 GPR55 GPR84 Guanylate Cyclase Histamine Receptor Imidazoline Receptor Leukotriene Receptor LPL Receptor mAChR Melanocortin Receptor Melatonin Receptor mGluR Neurokinin Receptor Neurotensin Receptor Opioid Receptor Orexin Receptor (OX Receptor) Oxytocin Receptor P2Y Receptor PKG Prostaglandin Receptor Protease-Activated Receptor (PAR) Apelin Receptor (APJ) Ras GPR88 Free Fatty Acid Receptor E3 Ligase Ligand-Linker Conjugates RGS GPR4 Secretin Receptor Mas-related G-protein-coupled Receptor (MRGPR) GPR35 GPR52 MCHR1 (GPR24) Leukotriene Receptor GLP Receptor Somatostatin Receptor Vasopressin Receptor

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Histamine Receptor

Histamine Receptor相关产品（101）

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.