anti-histamine

D18024 is a phthalazinonderivat with anti-allergic and anti-histamine effect.

Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.

The physiologic effect of Methyl Paraben (Nipagin) is by means of Increased Histamine Release, and Cell-mediated Immunity. Methyl Paraben (Nipagin) is an antimicrobial agent, preservative, flavouring agent. Methyl Paraben (Nipagin) is a constituent of cloudberry, yellow passion fruit, white wine, botrytised wine and Bourbon vanilla.The physiologic effect of Methyl Paraben (Nipagin) has been shown to exhibit anti-microbial function.

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

KP136 (AL136) is an orally active anti-allergic compound that inhibits histamine release and is used in studies of asthma and allergic edema.

Meclizine, also known as Meclozine, is a piperazine class H1 antagonist with antihistamine properties that inhibits the interaction of histamine at H1 receptors reversibly. It serves as an effective anti-motion sickness agent, able to cross the blood-brain barrier. Additionally, Meclizine acts as an agonist ligand for the mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR, making it useful in research on polyQ toxicity disorders, including Huntington's disease.

Parogrelil Free Base (NM-702 Free Base) is a selective phosphodiesterase 3 inhibitor with bronchodilatory and anti-inflammatory effects, inhibits leukotriene (LT)D(4) and histamine-induced constriction of isolated guinea pig tracheal strips, and can be used in the study of bronchial asthma.

DF-1111301 is a novel anti-allergic compound with anti-histamine H1 and anti-PAF activity.

ST-1006 is a potent histamine H4 receptor agonist (pKi: 7.94).ST-1006 has anti-inflammatory effects.ST-1006 is a potent inducer of basophil migration and induces basophil migration.ST-1006 is a potent inducer of basophil migration. ST-1006 has anti-inflammatory and anti-pruritic effects.

Tecastemizole (R 43512) is a selective antagonist of H1 receptor and a major metabolite of astemizole with anti-inflammatory effects.

Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.

Rhodiocyanoside A has antiallergic activity, it exhibits inhibitory activity on the histamine release from rat peritoneal exudate cells sensitized with anti-DNP IgE and inhibits the PCA reaction in rats.

Koaburaside exhibits antioxidant activity with an IC50 value of 9.0μM, it shows weak inhibitory activity against influenza A neuraminidase. Koaburaside may have anti-allergic inflammatory activity, it can suppress histamine release from mast cells.

Bufrolin, an analog of Cromoglycate (histamine release inhibitor) and a potent agonist of GPR35, enhances the interaction between β-arrestin-2 and both human GPR35a and rat GPR35. It stabilizes mast cells, exhibiting antiallergic properties, and inhibits anti-inflammatory responses triggered by internalization peptides. Furthermore, Bufrolin is researched for its anti-inflammatory properties in pharmaceutic applications associated with internalization peptides [1] [2] [3].

Betahistine (Vasomotal) is a histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers. Betahistine dihydrochloride is an anti-vertigo drug. It is commonly prescribed for balance disorders or to alleviate vertigo symptoms associated with Ménière's disease.

(+)-Columbianetin ((S)-Columbianetin) is a new phytoalexin associated with celery (Apium graveolens) resistance to pathogens during storage, it also has antifungal activity. (+)-Columbianetin has anti-inflammatory effects, it promotes histamine release, and inhibits the histamine release by substance P, suggests that it may be helpful in regulating mast cell-mediated allergic inflammatory responses. (+)-Columbianetin can be effectively used to protect keratinocytes from UVB induced damage.

Alginic acid (Snow acid algin G) is a natural polysaccharide extracted from brown seaweeds with anti-anaphylactic and anti-inflammatory activities. Alginic acid inhibits histamine release and can be used in the food industry.

Bakkenolide D has anti-allergic effect, it and bakkenolide D demonstrates inhibitory effect on the trachea contraction induced by histamine in vitro, they have obvious anti-histamine activities.

Marmin have anti-ulcer effects, which are ascribed primarily to the maintenance of the mucosal barrier integrity and inhibition of gastric motor activity and secondarily due to the prevention of the effects of endogenous acetylcholine and histamine.

Ranitidine bismuth citrate, an orally administered Histamine H2-receptor antagonist, demonstrates a potent inhibitory concentration (IC 50) of 3.3 μM and exhibits high selectivity towards SARS-CoV-2-infected cells. It is widely utilized as an anti-Helicobacter pylori agent, exhibiting a minimum inhibitory concentration (MIC 90) value of 16 ng/L.

Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from patients with lung cancer). It is selective for these phosphodiesterases over PDE1 and PDE2, where it provides less than 25% inhibition. Fenspiride potentiates the airway relaxant effects of isoproterenol and sodium nitroprusside indicating an effect on cAMP and cGMP phosphodiesterases, respectively. Aerosolized fenspiride (1 mg/ml) reverses bronchoconstriction induced by capsaicin and, when used at aerosolized concentrations ranging from 1-10 mg/ml, reduces cough induced by citric aci......

AA 2379, an anti inflammatory agent, inhibits the vascular permeability induced by histamine, serotonin, and bradykinin. It also has some analgesic activity.

Cimetidine (SKF-92334) hydrochloride is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine hydrochloride shows anti-cancer and anti-inflammatory activity. Cimetidine hydrochloride is a gastric acid reducer that can be used in the research of duodenal and gastric ulcers[1] [2] [5].

Chlorpheniramine is an H1 anti-histamine agent for IgE-mediated inflammation that is commonly used for allergic diseases.

Peptide 401 is an antimicrobial peptide (AMP) derived from the venom of bees and wasps. Peptide 401 induces mast cell degranulation, activating histamine release from peritoneal mast cells. Additionally, peptide 401 exhibits some anti-inflammatory activit

1. Yunaconitine (Guayewuanine B) has anti-inflammatory and analgesic actions. 2. Yunaconitine was shown to have anti-thermic effect in pyrexial rats when administered orally at a dose of 5 μg/kg. 3. Yunaconitine shows positive effect in the granuloma inhibition test when it was subcutaneously injected, 1 μg/kg for 6 d, or added directly to the cotton-pellet. 4. Yunaconitine inhibited the increased vascular permeability caused byacetic acid and histamine, the leucocyte migratory response induced by injection of 1 % carrageenin .1 ml in rat's thoracic cavity.

Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 microM), while not affecting ADP- or arachidonic acid-induced platelet aggregation [1]. The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7+/-0.4 microM, 3.2+/-0.7 microM and 1.5+/-0.4 microM, respectively whereas for loratadine the IC50 was 2.1+/-0.9 microM, 4.0+/-1.3 M and 1.7+/-0.5 microM. SR-27417A exhibited no inhibitory effect [2].in vivo: Rupatadine blocked histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 micrograms/kg i.v.). Moreover, it potently inhibited PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg/kg i.v.) [1]. rupatadine treatment improved the declined lung function and significantly decreased animal death. Moreover, rupatadine was able not only to attenuate silica-induced silicosis but also to produce a superior therapeutic efficacy compared to pirfenidone, histamine H1 antagonist loratadine, or PAF antagonist CV-3988 [3]. [1]. Merlos M, et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21. [2]. Queralt M, et al. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60. [3]. Lv XX, et al. Rupatadine protects against pulmonary fibrosis by attenuating PAF-mediated senescence in rodents. PLoS One. 2013 Jul 15;8(7):e68631.

JNJ-39758979 is a selective and high-affinity histamine H4 receptor antagonist (Kis: 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively). JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2

A-987306 is a potent and oral bioavailable histamine H 4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 exhibits anti-inflammatory activity in mice peritonitis model [1].

Meclizine dihydrochloride (NSC28728) is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.

Izuforant (JW1601) (Compound 24) has potent anti-inflammatory and anti-pruritic activities. Izuforant has a binding affinity for human serotonin 3 receptor (h5-HT3R) with an IC50 value of 9.1 μM. Izuforant is also an orally active antagonist of histamine H4 receptor (H4R) with an IC50 value of 36 nM against human H4R [1] [2].

Ganoderic acid C2 has anti-inflammatory,and anti-tumor-promoting activities. Ganoderic acid C2 can inhibit histamine release, it also has inhibitory effects on the induction of Epstein-Barr Virus early antigen.

FR-A 19, a Histamine H2 agonist, inhibits the release of IgE-mediated human basophil histamine in a nanomolar range. It has additional potent anti-allergic properties.

Tesmilifene fumarate (DPPE fumarate) (DPPE fumarate) is an H1C receptor antagonist。

H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor antagonist. It exhibits inhibitory effects on acetylcholinesterase, butyrylcholinesterase, and human monoamine oxidase B (hMAO B) with IC50 values of 180 nM, 880 nM, and 775 nM, respectively. With a Ki of 170 nM for hH3R, H3R antagonist 2 demonstrates favorable anti-neuropathic pain and memory-enhancing effects. Additionally, it can cross the blood-brain barrier (BBB) [1].

Arbortristoside A is an anti-inflammatory and antinociceptive. This activity may be due to the inhibiting effect of prostaglandin, histamine and serotonin. Arbortristoside A has also been shown to act on ulcerations and may facilitate healing of peptic ulcers.

Roxatidine hydrochloride is an anti-ulcer agent and histamine antagonist that suppresses gastric acid secretion. It effectively heals duodenal and gastric ulcers and reduces ulcer pain. Roxatidine acetate has an improved safety profile compared to other similar drugs, in part because lower doses of roxatidine acetate are therapeutically effective.

(+)-9'-O-trans-feruloyl-5,5'-dimethoxylariciresinol may have anti-allergic inflammatory effect, it can inhibit release of histamine from mast cells. It shows cytotoxicity against a small panel of human tumor cell lines, with ED50 values of 9.86 to approxi

Buclizine dihydrochloride (Buclina) is the hydrochloride salt form of buclizine, a piperazine histamine H1 receptor antagonist with primarily antiemetic and antivertigo activities. Buclizine dihydrochloride binds to and blocks the histamine H1 receptor, thereby preventing the symptoms that are caused by histamine activity. Buclizine dihydrochloride exerts its anti-emetic effect by binding to and blocking the muscarinic and histamine receptors in the vomiting center of the central nervous system (CNS). This may prevent activation of the chemoreceptor trigger zone (CTZ) and may reduce nausea and vomiting.

Emedastine Difumarate is a selective histamine H1 receptor antagonist with anti-allergic activity, prescribed for allergic conjunctivitis. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeabil

A-940894 is a histamine H4 receptor antagonist with anti-inflammatory properties. A-940894 potently binds to both human and rat histamine H4 receptors and exhibits considerably lower affinity for the human histamine H1, H2, or H3 receptors. A-940894 has g

Cimetidine (SKF-92334) is a histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.

Dimenhydrinate (Vomex A) is an ethanolamine and histamine antagonist with anti-allergic activity.

(+)-Dropropizine can inhibit histamine receptor, anti-allergic, and reduce a cough by modulation of neuropeptides involved in the cough reflex and by interfering with stimulus activation of peripheral endings of sensory nerves.

Fenspiride is an antagonist of H1-histamine receptors. Fenspiride is an orally active non-steroidal anti-inflammatory agent that can be used for the treatment of respiratory tract infections and otitis media. Fenspiride inhibited phosphodiesterase 4 and phosphodiesterase 3 activities with -logIC50 values of 4.16+/-0.09 and 3.44+/-0.12, respectively. Phosphodiesterase 5 activity was also inhibited with a -logIC50 value of approximately 3.8.

Sarpogrelate hydrochloride (MCI-9042) , a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate hydrochloride was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate hydrochloride lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate hydrochloride -induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD.

Roxatidine acetate is an anti-ulcer agent and histamine antagonist that inhibits gastric acid secretion. Compared to other similar drugs, Roxatidine acetate has an improved safety profile, in part because lower doses of roxatidine acetate are therapeutica

A-943931, a selective and potent antagonist of the histamine H4 receptor (H4R), demonstrates affinity with pKi values of 4.6 and 3.8 nM for human and rat H4Rs, respectively. This compound exhibits anti-inflammatory and antinociceptive properties.

Roxatidine, the active metabolite of Roxatidine acetate hydrochloride, serves as a histamine H2-receptor antagonist and exhibits anti-ulcer properties. It functions by suppressing the release of histamine, thereby inhibiting proton secretion, and also reduces the production of VEGF-1, a key indicator of inflammation and angiogenesis. This compound demonstrates an anti-allergic inflammatory effect [1].

INCB38579 is a selective, orally active, histamine H4 receptor (HH4R) antagonist that crosses the blood-brain barrier and acts on hH4R (IC50: 4.8 nM), mH4R (IC50: 42 nM), and rH4R (IC50: 32 nM). INCB38579 has anti-inflammatory and antipruritic effects.