Promethazine sulfoxide is a metabolite of the histamine H1 receptor antagonist Promethazine. It is formed from promethazine by the cytochrome P450 (CYP) isoform CYP2D6.

Gizzerosine is an H2 receptor agonist. It can stimulate the gastric acid secretion of broiler chickens, thus causing gizzard erosion in them. Gizzerosine has significant research value in the fields of agricultural farming and feed science.

BL 6341A is an antagonist for histamine H2 receptor with Ki of 3.5-4.4 nM, that inhibits histamine-induced acid secretion and cAMP formation. BL 6341A can be used in research of gastric acid secretion related diseases, such as gastric ulcer or gastroesophageal reflux.

Arpromidine (BU-E-50) is the agonist for histamine H2 receptor and the antagonist for histamine H1 receptor. Arpromidine exhibits positive inotropic effect with less risks in causing arrhythmias. Arpromidine can be used in research of congestive heart failure.

ADS1017 is the antagonist for histamine receptor and muscarinic receptor, that exhibits good affinities to hH3R, hH4R, hM2R and hM4R with pKi of 6.8, 5.5, 7.4 and 7.2. ADS1017 exhibits analgesic and anti-allodynic efficacy in mice Capsaicin-or Oxaliplatin-induced pain models.

(S)-Cetirizine dihydrochloride ((S)-P071) is an orally active antagonist of the histamine H1 receptor with a Ki value of 39.1 nM. (S)-Cetirizine dihydrochloride exerts anti-allergic activity by binding to the histamine H1 receptor and blocking the action of histamine. (S)-Cetirizine dihydrochloride is promising for research of allergic diseases such as allergic rhinitis.

(-)-Brompheniramine is a H1 receptor antagonist with antiallergic activity.

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.

Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin.

Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor.

Dimaprit dihydrochloride is a selective histamine H2 receptor agonist, it also inhibits nNOS with an IC50 of 49 μM. Dimaprit dihydrochloride can stimulate gastric acid secretion.

UR-MB-69 is a potent agonist of histamine H2 receptor (H2R) dopamine receptor D3R with pKi of 8.69 and 8.06, respectively.

RGH-235 is a potent, selective, and orally active H3 receptor antagonist/inverse agonist with high affinity (Ki=3.0-9.2 nM, depending on species), without affinity to H1, H2 or H4 receptors.

NLX-204 is a potent and selective ERK1/2 phosphorylation-preferring serotonin 5 HT1A receptor agonist with pKi = 10.19. NLX-204 displayed high selectivity in the SafetyScreen44 panel (including hERG channel), high solubility, metabolic stability, and Caco-2 penetration and did not block CYP3A4, CYP2D6 isoenzymes, or P-glycoprotein. Preliminary in vivo studies confirmed its promising pharmacokinetic profile. NLX-204 also robustly stimulated ERK1/2 phosphorylation in rat cortex and showed highly potent (MED = 0.16 mg/kg) and efficacious antidepressant-like activity, totally eliminating immobility in the rat Porsolt test.

ST-1006 is a potent histamine H4 receptor agonist with a pKi value of 7.94. ST-1006 has anti-inflammatory effect.

Immepip is a H3 agonist. Immepip can reduce cortical histamine release. Immepip can be used for the research of neurological diseases.

Rupatadine is a dual histamine H1 and PAF antagonist

Pitolisant Hcl(BF2.649;Ciproxidine ) is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).

Fexofenadine is a third-generation antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever, nasal congestion, and urticaria.

Cetirizine 2Hcl, 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.

Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.

Cetirizine methyl ester is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist.

Cipralisant (GT-2331) enantiomer is the enantiomer of Cipralisant, Cipralisant is an orally active, potent, selective, and high affinity histamine H3 receptor antagonist (rat Ki=0.47 nM).

ST-1006 maleate is a potent histamine H4 receptor agonist with a pKi value of 7.94. ST-1006 maleate has anti-inflammatory effect.

Dimethindene maleate is a selective histamine H1 antagonist with antihistamine effects. Dimethindene maleate can be used for the research of hypersensitivity reactions.

Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent Sigma-1 receptor binding affinity (Ki: 160 nM).

Methapyrilene is a histamine antagonist, a pyridine chemical with anticholinergic activity. Methapyrilene can cause target organ-specific epigenetic alterations, such as a decrease in DNA methylation levels. Methapyrilene induces hepatocellular carcinoma in rats.

Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).

Dimethindene is a potent, selective histamine H1 antagonist. Dimethindene impairs cutaneous wound healing (WH). Dimethindene can block K+ currents.

Phenindamine (Nu 1504) is an antihistamine.