Histamine Receptors are a class of G protein-coupled receptors with histamine as their endogenous ligand. There are four known histamine receptors: H1 receptor, H2 receptor, H3 receptor, H4 receptor. The H1 receptor is a histamine receptor belonging to the family of Rhodopsin-like G-protein-coupled receptors. This receptor, which is activated by the biogenic amine histamine, is expressed throughout the body, to be specific, in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of Protein Kinase A. Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act asautoreceptors in presynaptic histaminergic neurons, and also control histamine turnover by feedback inhibition of histamine synthesis and release. The Histamine H4 receptor has been shown to be involved in mediating eosinophil shape change and mast cell chemotaxis.


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Chlorpheniramine-d4 maleate

Chlorpheniramine-d4 (maleate) is deuterium labeled Chlorpheniramine (maleate).

  • CAS Number: 2747915-71-3
  • MF: C20H19D4ClN2O4
  • MW: 394.89
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mebhydrolin

Mebhydrolin is a specific histamine H1 receptor antagonist.

  • CAS Number: 524-81-2
  • MF: C19H20N2
  • MW: 276.37600
  • Catalog: Histamine Receptor
  • Density: 1.12 g/cm3
  • Boiling Point: 856.1ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 471.6ºC

Betahistine EP Impurity C

Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine[1]. Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA)[2][3].

  • CAS Number: 5452-87-9
  • MF: C15H19N3
  • MW: 241.33100
  • Catalog: Histamine Receptor
  • Density: 1.067g/cm3
  • Boiling Point: 371.9ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 178.7ºC

Seliforant

Seliforant (SENS-111, SENS111) is a novel potent, selective histamine H4 receptor antagonist.

  • CAS Number: 1164115-89-2
  • MF: C12H21N5
  • MW: 235.329
  • Catalog: Histamine Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 412.9±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 203.5±28.7 °C

(6-CHLORO-1H-BENZOIMIDAZOL-2-YL)-(4-METHYL-PIPERAZIN-1-YL)-METHANONE

JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively[1][2].

  • CAS Number: 73903-17-0
  • MF: C13H15ClN4O
  • MW: 278.73700
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fenspiride-d5 hydrochloride

Fenspiride-d5 hydrochloride is the deuterium labeled Fenspiride hydrochloride. Fenspiride hydrochloride is an α adrenergic and H1 histamine receptor antagonist[1][2].

  • CAS Number: 1246815-28-0
  • MF: C15H16D5ClN2O2
  • MW: 301.82
  • Catalog: Adrenergic Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

norastemizole

Tecastemizole (Norastemizole), a major metabolite of Astemizole, is a potent and selective H1 receptor antagonist. Tecastemizole shows anti-inflammatory activities[1].

  • CAS Number: 75970-99-9
  • MF: C19H21FN4
  • MW: 324.40
  • Catalog: Histamine Receptor
  • Density: 1.28g/cm3
  • Boiling Point: 519.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 268.2ºC

Histamine

Histamine is an organic nitrogenous compound involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter.

  • CAS Number: 51-45-6
  • MF: C5H9N3
  • MW: 111.145
  • Catalog: Histamine Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 331.0±17.0 °C at 760 mmHg
  • Melting Point: 83-84ºC
  • Flash Point: 180.3±8.1 °C

Cipralisant (enantiomer)

Cipralisant (GT-2331) enantiomer is the enantiomer of Cipralisant (HY-106993), Cipralisant is an orally active, potent, selective, and high affinity histamine H3 receptor antagonist (rat Ki=0.47 nM)[1][2][3][4][5].

  • CAS Number: 223420-11-9
  • MF: C14H20N2
  • MW: 216.32
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Epinastine

Epinastine(WAL801) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.Target: Histamine ReceptorEpinastine shows a high affinity to H1-receptors in receptor binding studies in the guinea pig ileum. Epinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs [1]. Epinastine is able to displace specific [3H]NC-5Z binding at low concentrations in the locust nervous tissue. Epinastine binds to the honey bees neuronal octopamine receptor with Ki of 1.1 nM. Epinastine antagonises octopamine-induced cAMP formation in the insect brain [2]. Epinastine causes an inhibition of histamine release from rat peritoneal mast cells induced by both antigen-antibody reaction and compound 48/80. Epinastine is similarly effective in inhibiting compound 48/80-induced histamine release not only from isolated rat peritoneal mast cells but also from rat mesenterial pieces. Epinastine is effective in inhibiting not only Ca2+ uptake into lung mast cells in actively sensitized guinea pigs but also Ca2+ release from the intracellular Ca store of rat peritoneal mast cells exposed to both compound 48/80 and substance P [3]. Epinastine shows a dose- and time-dependent suppressive effect on IL-8, one of the chemokines for eosinophils, released from eosinophils isolated from atopic diseases [4].

  • CAS Number: 80012-43-7
  • MF: C16H15N3
  • MW: 249.31000
  • Catalog: Histamine Receptor
  • Density: 1.32 g/cm3
  • Boiling Point: 428ºC at 760 mmHg
  • Melting Point: 270ºC
  • Flash Point: 212.7ºC

Tiotidine

Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors[1][2].

  • CAS Number: 69014-14-8
  • MF: C10H16N8S2
  • MW: 312.41800
  • Catalog: Histamine Receptor
  • Density: 1.5g/cm3
  • Boiling Point: 543.6ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 282.5ºC

Meclizine dihydrochloride

Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sicknessTarget: Histamine H1 ReceptorMeclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness, possesses anticholinergic, central nervous system depressant, and local anesthetic effects [1]. Meclizine is an agonist ligand for mouse CAR (constitutive androstane receptor), and an inverse agonist for human CAR. Meclizine increases mCAR transactivation in a dose-dependent manner, stimulates binding of steroid receptor coactivator 1 to the murine receptor in vitro. In contrast, meclizine suppresses hCAR transactivation and inhibits the phenobarbital-induced expression of the CAR target genes, cytochrome p450 monooxygenase (CYP)2B10, CYP3A11, and CYP1A2, in primary hepatocytes derived from mice expressing hCAR, but not mCAR [2].

  • CAS Number: 1104-22-9
  • MF: C25H29Cl3N2
  • MW: 463.870
  • Catalog: Histamine Receptor
  • Density: 1.159g/cm3
  • Boiling Point: 495.3ºC at 760mmHg
  • Melting Point: 212 °C
  • Flash Point: 253.3ºC

Perphenazine

Perphenazine is a typical antipsychotic drug, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.

  • CAS Number: 58-39-9
  • MF: C21H26ClN3OS
  • MW: 403.969
  • Catalog: 5-HT Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 580.4±50.0 °C at 760 mmHg
  • Melting Point: 35339ºC
  • Flash Point: 304.8±30.1 °C

AChE-IN-14

AChE-IN-14 is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease[1].

  • CAS Number: 2390042-05-2
  • MF: C28H35NO3
  • MW: 433.58
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

jnj39758979

JNJ-39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM.

  • CAS Number: 1046447-90-8
  • MF: C11H19N5
  • MW: 221.302
  • Catalog: Histamine Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 439.6±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 219.6±31.5 °C

PF-03654746

PF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration.PF-03654746 reduces allergen-induced nasal symptoms, might be a novel therapeutic strategy to further explore allergic rhinitis[1].PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD)[2].

  • CAS Number: 935840-31-6
  • MF: C18H24F2N2O
  • MW: 322.39300
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Lodoxamide

Lodoxamide is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.

  • CAS Number: 53882-12-5
  • MF: C11H6ClN3O6
  • MW: 311.63500
  • Catalog: Histamine Receptor
  • Density: 1.78g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rupatadine

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].

  • CAS Number: 158876-82-5
  • MF: C26H26ClN3
  • MW: 415.958
  • Catalog: Autophagy
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 586.4±50.0 °C at 760 mmHg
  • Melting Point: 58-61ºC
  • Flash Point: 308.4±30.1 °C

Bepotastine tosylate

Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research[1][2][3].

  • CAS Number: 1160415-45-1
  • MF: C28H33ClN2O6S
  • MW: 561.09
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pheniramine maleate

Pheniramine Maleate ia an antihistamine and vasoconstrictor.

  • CAS Number: 132-20-7
  • MF: C20H24N2O4
  • MW: 356.416
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: 348.3ºC at 760 mmHg
  • Melting Point: 104-108°C
  • Flash Point: 164.5ºC

JZP 361

JZP-361 is a potent and reversible inhibitor of human recombinant MAGL (hMAGL, IC50=46 nM), and has almost 150-fold higher selectivity over human recombinant fatty acid amide hydrolase (hFAAH, IC50=7.24 μM) and 35-fold higher selectivity over human α/β-hydrolase-6 (hABHD6, IC50=1.79 μM). JZP-361 represents a dual-acting pharmacological tool possessing both MAGL inhibitory and antihistaminergic activities[1].

  • CAS Number: 1680193-80-9
  • MF: C22H20ClN5O
  • MW: 405.880
  • Catalog: Histamine Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 611.7±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 323.8±34.3 °C

NEDOCROMIL SODIUM

Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).

  • CAS Number: 69049-74-7
  • MF: C19H15NNa2O7
  • MW: 415.30400
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: 645.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 344.2ºC

VUF8430 dihydrobromide

VUF 8430 (dihydrobromide) is a potent and selective histamine H4 receptor agonist with a Ki of 31.6 nM and an EC50 of 50 nM[1].

  • CAS Number: 100130-32-3
  • MF: C4H13Br2N5S
  • MW: 323.05300
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: 348.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 164.8ºC

Betazole

Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity[1][2][3].

  • CAS Number: 105-20-4
  • MF: C5H9N3
  • MW: 111.14500
  • Catalog: Histamine Receptor
  • Density: 1.14g/cm3
  • Boiling Point: 284.1ºC at 760mmHg
  • Melting Point: 25°C
  • Flash Point: 150.3ºC

Cimetidine hydrochloride

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

  • CAS Number: 70059-30-2
  • MF: C10H17ClN6S
  • MW: 288.80000
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: 488ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 248.9ºC

CP-66948

CP-66948 is a histamine H2-receptor antagonist with gastric antisecretory activity and mucosal protective properties.

  • CAS Number: 101189-47-3
  • MF: C13H20N6S
  • MW: 292.40300
  • Catalog: Histamine Receptor
  • Density: 1.34g/cm3
  • Boiling Point: 561.6ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 293.4ºC

4'-O-Methylnyasol

4'-O-Methylnyasol is an inhibitor of β-hexosaminidase. 4'-O-Methylnyasol inhibits β-hexosaminidase release from rat basophilic leukemia-2H3 cells with an IC50 of 52.67 μM[1].

  • CAS Number: 79004-25-4
  • MF: C18H18O2
  • MW: 266.33
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cetirizine

Cetirizine, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. IC50 value:Target: Histamine H1 receptorCetirizine crosses the blood-brain barrier only slightly, reducing the sedative side-effect common with older antihistamines. It has also been shown to inhibit eosinophil chemotaxis and LTB4 release. At a dosage of 20 mg, Boone et al. found that it inhibited the expression of VCAM-1 in patients with atopic dermatitis. The levorotary enantiomer of cetirizine, known as levocetirizine, is the more active form. From Wikipedia.

  • CAS Number: 83881-51-0
  • MF: C21H25ClN2O3
  • MW: 388.888
  • Catalog: Histamine Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 542.1±45.0 °C at 760 mmHg
  • Melting Point: 110-115°C
  • Flash Point: 281.6±28.7 °C

Antazoline

Antazoline is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect[1][2][3].

  • CAS Number: 91-75-8
  • MF: C17H19N3
  • MW: 265.353
  • Catalog: Histamine Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 475.5±38.0 °C at 760 mmHg
  • Melting Point: 159ºC
  • Flash Point: 241.4±26.8 °C

Benztropine-d3 mesylate

Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate[1]. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2][3].

  • CAS Number: 202529-16-6
  • MF: C22H26D3NO4S
  • MW: 406.55
  • Catalog: Dopamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A