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histamine release inhibitor

" in MedChemExpress (MCE) Product Catalog:

40

Inhibitors & Agonists

1

Peptides

6

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-U00027
    Quinotolast sodium

    FR71021

    		 Histamine Receptor Leukotriene Receptor Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Quinotolast sodium in the concentration range of 1-100 μg/mL inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner.
    Quinotolast sodium
  • HY-B1404
    Nylidrin hydrochloride

    Buphenine hydrochloride

    		 Histamine Receptor Inflammation/Immunology
    Nylidrin hydrochloride is an inhibitor of IgE-mediated histamine release in passive sensitized rat peritoneal mast cells, and it has anti-allergic effects.
    Nylidrin hydrochloride
  • HY-N10182
    Spinacetin

    		Histamine Receptor Inflammation/Immunology
    Spinacetin is a natural product that can be isolated from Inula japonica. Spinacetin inhibits the release of histamine. Spinacetin has anti-inflammatory activity .
    Spinacetin
  • HY-12206
    Thioperamide
    1 Publications Verification

    MR-12842

    		 Histamine Receptor Neurological Disease
    Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM .
    Thioperamide
  • HY-12206A
    Thioperamide maleate
    1 Publications Verification

    MR-12842 maleate

    		 Histamine Receptor Neurological Disease
    Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide maleate inhibits [ 3H]histamine synthesis with a Ki of 31 nM .
    Thioperamide maleate
  • HY-13405
    Tiaramide hydrochloride

    RHC 2592-A

    		 Histamine Receptor Inflammation/Immunology
    Tiaramide (RHC 2592-A) hydrochloride is an analgesic agent with antiallergic activity, and is also a non-steroidal, anti-inflammatory compound. Tiaramide hydrochloride inhibits histamine release .
    Tiaramide hydrochloride
  • HY-13218
    Acitazanolast

    WP-871

    		 Histamine Receptor Inflammation/Immunology
    Acitazanolast is an orally active antiallergic agent, can inhibit histamine release. Acitazanolast can be used in study of type I anaphylaxis (immediate) caused by IgE antibodies .
    Acitazanolast
  • HY-14271
    Acreozast

    TYB-2285

    		 Histamine Receptor Inflammation/Immunology
    Acreozast (TYB-2285) is a histamine release inhibitor. Acreozast inhibits the histamine release primed with IL-3. Acreozast might regulate allergic inflammation in vivo by the suppression of mediator release primed with IL-3 .
    Acreozast
  • HY-N12295
    Ciwujianoside D1

    		Others Inflammation/Immunology
    Ciwujianoside D1 is a natural product that can inhibit histamine release induced by anti-immunoglobulin E from rat peritoneal mast cells .
    Ciwujianoside D1
  • HY-106076
    REV 2871

    Eclazolast; CHBZ

    		 Histamine Receptor Inflammation/Immunology
    REV 2871 (Eclazolast; CHBZ) is a potent and oral activity antiallergic agent. REV 2871 also is an irreversibility histamine release (HR) inhibitor .
    REV 2871
  • HY-109544
    Repirinast

    MY-5116

    		 Histamine Receptor Inflammation/Immunology
    Repirinast (MY-5116) is an orally active anti-allergic agent. Repirinast inhibits histamine release. Repirinast can be used in the research of bronchial asthma .
    Repirinast
  • HY-137941
    Roxatidine

    		Histamine Receptor Caspase NF-κB p38 MAPK Inflammation/Immunology
    Roxatidine is an active metabolite of Roxatidine acetate hydrochloride, is an orally active histamine H2-receptor antagonist. Roxatidine, an anti-ulcer agent, suppresses histamine release (thus inhibiting proton secretion) and inhibits the production of VEGF-1, an important marker of inflammation and angiogenesis. Anti-allergic inflammatory effect. Roxatidine is promising for research of gastric and duodenal ulcers .
    Roxatidine
  • HY-137941R
    Roxatidine (Standard)

    		Histamine Receptor Inflammation/Immunology
    Roxatidine (Standard) is the analytical standard of Roxatidine. This product is intended for research and analytical applications. Roxatidine is an active metabolite of Roxatidine acetate hydrochloride, is a histamine H2-receptor antagonist. Roxatidine, an anti-ulcer agent, suppresses histamine release (thus inhibiting proton secretion) and inhibits the production of VEGF-1, an important marker of inflammation and angiogenesis. Anti-allergic inflammatory effect .
    Roxatidine (Standard)
  • HY-B1404R
    Nylidrin (hydrochloride) (Standard)

    		Others Inflammation/Immunology
    Nylidrin (hydrochloride) (Standard) is the analytical standard of Nylidrin (hydrochloride). This product is intended for research and analytical applications. Nylidrin hydrochloride is an inhibitor of IgE-mediated histamine release in passive sensitized rat peritoneal mast cells, and it has anti-allergic effects.
    Nylidrin (hydrochloride) (Standard)
  • HY-P3317
    Azaline

    Azaline A

    		 GnRH Receptor Endocrinology
    Azaline (Azaline A) is a gonadotropin-releasing hormone (GnRH) receptor antagonist with a KD value of 0.48 nM. Azaline can effectively induce histamine release, with an effect comparable to that of GnRH, and it can completely inhibit ovulation at a dose of 2.0-3.0 μg per female rat. Azaline has potential applications in regulating reproductive functions .
    Azaline
  • HY-U00364
    CI-949

    		Histamine Receptor Prostaglandin Receptor Leukotriene Receptor Inflammation/Immunology Endocrinology
    CI-949 is an allergic mediator release inhibitor, which inhibits histamine, leukotriene C4/D4 (LTC4/LTD4), and thromboxane B2 (TXB2) release with IC50s of 11.4 μM, 0.5 μM and 0.1 μM, respectively.
    CI-949
  • HY-105999A
    APC 366 hydrochloride

    		Ser/Thr Protease Inflammation/Immunology
    APC 366 hydrochloride is a selective inhibitor of mast cell trypsin activity. APC 366 hydrochloride is able to inhibit trypsin-induced histamine release in human tonsil and lung cells. APC 366 hydrochloride may have important applications in regulating allergic reactions and inflammation .
    APC 366 hydrochloride
  • HY-W754020
    Elbanizine

    		Histamine Receptor Others
    Elbanizine inhibits histamine, bradykinin, histamin-release from rat mast cells (IC50 of 0.26 μM) and the IgE-mediated passive cutaneous anaphylaxis (PCA) reaction. Elbanizine exhibits antiallergic and antiasthmatic in guinea pig model .
    Elbanizine
  • HY-123103
    Linetastine

    		Lipoxygenase Histamine Receptor Inflammation/Immunology
    Linetastine is an orally active and potent 5-Lipoxygenase inhibitor. Linetastine shows antihistamine activity. Linetastine inhibits leukotriene production and antagonizes the effect of histamine. Linetastine inhibits the release of leukotrienes B4 and C4 from calcium ionophore-stimulated human leukocytes .
    Linetastine
  • HY-B0640A
    Epinastine hydrochloride

    WAL801 hydrochloride

    		 Histamine Receptor Inflammation/Immunology Endocrinology
    Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action .
    Epinastine hydrochloride
  • HY-17043
    Loratadine
    5+ Cited Publications

    Loratidine; SCH 29851

    		 Flavivirus Dengue virus Histamine Receptor Infection Inflammation/Immunology Endocrinology Cancer
    Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
    Loratadine
  • HY-B0640
    Epinastine

    WAL801

    		 Histamine Receptor Inflammation/Immunology Endocrinology
    Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action .
    Epinastine
  • HY-123432
    AHR-13268D

    		Histamine Receptor Inflammation/Immunology
    AHR-13268D is an oral active antiallergic and antihistaminic agent, with bioavailable approximately 88%. AHR-13268D is a potent inhibitor of histamine release from rat peritoneal mast cells, with the IC50 of 0.51 nM .
    AHR-13268D
  • HY-N3622
    Corchoionoside C

    (6S,9S)-Roseoside

    		 Others Inflammation/Immunology
    Corchoionoside C ((6S,9S)-Roseoside), an ionone glucoside, can be isolated from Capparis spinosa. Corchoionoside C inhibits the antigen-antibody reaction induced histamine release from rat peritoneal exudate cells .
    Corchoionoside C
  • HY-113802
    VUF 8328

    		Histamine Receptor Neurological Disease
    VUF 8328 is a potent histamine H(3) receptor agonist. VUF 8328 inhibits the electrically-evoked [ 3H]-no-radrenaline release from rat cortical slices. VUF 8328 is promising for research of central nervous system disorders .
    VUF 8328
  • HY-106064A
    Piriprost potassium

    U 60257B

    		 Leukotriene Receptor Inflammation/Immunology
    Piriprost (U-60,257B) potassium is an inhibitor of leukotriene synthesis. Piriprost potassium inhibits the release of both leukotriene and histamine with an IC50 of 0.11 μM from isolated porcine lung cells. Piriprost potassium increases alkaline phosphatase (ALP) activity in cultured endometrial stromal cells .
    Piriprost potassium
  • HY-N3421
    Koaburaside

    		Interleukin Related TNF Receptor Influenza Virus Infection Inflammation/Immunology Cancer
    Koaburaside is a cytoprotective and anti-inflammatory natural compound. Koaburaside shows antioxidant activity with an IC50 of 9.0 μM for DPPH-free radical scavenging assay. Koaburaside inhibits histamine release and expressions of IL-6 and TNF-α in human mast cells. Koaburaside also effectively inhibits influenza A neuraminidase .
    Koaburaside
  • HY-N3007A
    (E)-Naringenin chalcone

    		Others Inflammation/Immunology
    (E)-Naringenin chalcone is an orally active anti-allergic agent. (E)-Naringenin chalcone also has antioxidant, anti-inflammatory activities. (E)-Naringenin chalcone can improve adipocyte functions. (E)-Naringenin chalcone inhibits histamine release from rat peritoneal mast cell .
    (E)-Naringenin chalcone
  • HY-130592
    Compound 48/80 trihydrochloride

    C48/80 trihydrochloride

    		 Phospholipase Neurological Disease
    Compound 48/80 trihydrochloride (C48/80 trihydrochloride) is a mixture of condensation products of N-methyl-p-methoxyphenethylamine with formaldehyde. Compound 48/80 trihydrochloride is also a histamine releaser and a mast cell degranulator. Compound 48/80 inhibits phosphatidylinositol-specific phospholipase C activity from human platelets .
    Compound 48/80 trihydrochloride
  • HY-B0640AR
    Epinastine hydrochloride (Standard)

    WAL801 hydrochloride (Standard)

    		 Histamine Receptor Inflammation/Immunology Endocrinology
    Epinastine (hydrochloride) (Standard) is the analytical standard of Epinastine (hydrochloride). This product is intended for research and analytical applications. Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action .
    Epinastine hydrochloride (Standard)
  • HY-17043R
    Loratadine (Standard)

    		Dengue virus Flavivirus Histamine Receptor Infection Inflammation/Immunology Endocrinology Cancer
    Loratadine (Standard) is the analytical standard of Loratadine. This product is intended for research and analytical applications. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
    Loratadine (Standard)
  • HY-167715
    Traxanox

    		Histamine Receptor Phosphodiesterase (PDE) Inflammation/Immunology
    Traxanox is an orally available diuretic that enhances phagocytosis of yeast granules by mouse peritoneal macrophages and rat peritoneal polymorphonuclear leukocytes in vitro. Traxanox inhibits IgE-mediated histamine release and cyclic AMP phosphodiesterase activity.Traxanox exhibits anti-inflammatory activity, as it inhibits the anaphylactoid reaction and reduces pleural fluid accumulation in experimental models of inflammation. Traxanox also demonstrates a synergistic effect when combined with hydrocortisone or indomethacin in suppressing adjuvant arthritis in rats.
    Traxanox
  • HY-126127
    BRL 22321 free base

    		Histamine Receptor Inflammation/Immunology
    BRL 22321 free base is a stabilizer with similar mast cell stabilizing activity to Cromolyn sodium (HY-B0320A) and also has some smooth muscle relaxant activity. BRL 22321 free base is more potent than Cromolyn sodium (HY-B0320A) in inhibiting rat passive cutaneous and peritoneal anaphylaxis and antigen-induced histamine release from passively sensitized rat peritoneal cells .
    BRL 22321 free base
  • HY-106481
    Bufrolin

    		GPR35 Histamine Receptor Inflammation/Immunology
    Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide .
    Bufrolin
  • HY-B0539
    Desloratadine
    Maximum Cited Publications
    10 Publications Verification

    Sch34117

    		 Histamine Receptor TNF Receptor Leukotriene Receptor Inflammation/Immunology
    Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (Ki=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria .
    Desloratadine
  • HY-B1693
    Levomepromazine
    1 Publications Verification

    Methotrimeprazine

    		 5-HT Receptor Dopamine Receptor Histamine Receptor Autophagy Enterovirus Calcium Channel Infection Neurological Disease Inflammation/Immunology
    Levomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca 2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca 2+ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting .
    Levomepromazine
  • HY-W344044
    Levomepromazine maleate

    Methotrimeprazine maleate

    		 5-HT Receptor Dopamine Receptor Histamine Receptor Autophagy Enterovirus Calcium Channel Infection Neurological Disease Inflammation/Immunology
    Levomepromazine maleate (Methotrimeprazine maleate) is an orally active antipsychotic compound and Ca 2+ release inducer. Levomepromazine maleate inhibits SERCA pump and induces an increase in cytoplasmic Ca 2+ levels. Levomepromazine maleate has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine maleate can induce adaptive ER stress and autophagy. In addition, Levomepromazine maleate has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine maleate can be used in the study psychiatric disorders and relieving nausea and vomiting .
    Levomepromazine maleate
  • HY-B1693R
    Levomepromazine (Standard)

    Methotrimeprazine (Standard)

    		 5-HT Receptor Dopamine Receptor Autophagy Histamine Receptor Enterovirus Calcium Channel Infection Neurological Disease Inflammation/Immunology
    Levomepromazine (Standard) is the analytical standard of Levomepromazine. This product is intended for research and analytical applications. Levomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca 2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca 2+ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting .
    Levomepromazine (Standard)
  • HY-12191
    A-331440

    		Histamine Receptor Metabolic Disease
    A-331440 is a potent and selective histamine H3 receptor antagonist that regulates neurotransmitter release by inhibiting presynaptic H3 receptors. In preclinical studies involving mice on a high-fat diet, A-331440 demonstrated dose-dependent effects on weight reduction and fat loss. At 5 mg/kg, it effectively decreased body weight comparable to dexfenfluramine, while at 15 mg/kg, it significantly reduced body fat and improved insulin tolerance, similar to mice on a low-fat diet. These findings suggest that A-331440 holds promise as an antiobesity agent by modulating histaminergic pathways involved in food intake and metabolic regulation .
    A-331440
  • HY-111136
    BL-1020 mesylate

    		GABA Receptor 5-HT Receptor Dopamine Receptor Histamine Receptor Neurological Disease
    BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAA receptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate .
    BL-1020 mesylate

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