antihistamine-1

Antihistamine-1 is an H1-antihistamine (Ki: 6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel (IC50s: 5.4 and 0.8 μM).

Epinastine (WAL801), a potent, selective, and orally-active antihistamine and mast cell stabilizer, functions as a histamine H1 receptor antagonist. It also inhibits IL-8 release from human eosinophils, showcasing antiallergic action [1] [2] [3] [4].

Diphenylpyraline hydrochloride (4-Diphenylmethoxy-1-methylpiperidine hydrochloride) is used in the treatment of Parkinsonism.It is a first-generation antihistamine with anticholinergic effects, functions as a dopamine reuptake inhibitor.

Cetirizine Impurity C, an impurity of Cetirizine, is related to the carboxylated metabolite of hydroxyzine. Cetirizine is a second-generation antihistamine acting as a specific, orally active, and long-acting antagonist of the histamine H1-receptor[1][2].

Phenyltoloxamine (Bistrimin) is an antihistamine with sedative and analgesic properties, and it exhibits strong Sigma-1 receptor binding affinity with a Ki of 160 nM [1] [2] [3].

Phenindamine (Nu 1504) is an H1-receptor antagonist with antihistamine properties[1].

Brompheniramine ((±)-Brompheniramine) is a potent, orally active alkylamine class antihistamine and a selective antagonist of the histamine H1 receptor (Kd = 6.06 nM). It has applications in the research of allergic rhinitis and exhibits anticholinergic, antidepressant, and anesthetic properties. Brompheniramine blocks calcium channels, sodium channels, and hERG channels with IC50 values of 16.12 μM, 21.26 μM, and 0.90 μM, respectively [1] [2] [3] [4].

Sequifenadine has the potential in researching of inflammatory eye disease with allergic symptoms that is a H1-antihistamine [1] [2].

Bromodiphenhydramine (Ambodryl) has antimicrobial activities which can be used in the cutaneous allergies research. Bromodiphenhydramine is an effective antihistamine that can inhibit a large number of Gram-negative and Gram-positive bacteria [1] [2] [3].

Cetirizine methyl ester, an impurity of Cetirizine, serves as a specific, orally active, and long-acting histamine H1-receptor antagonist. As a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, Cetirizine effectively counters allergic reactions [1].

Cetirizine Impurity C dihydrochloride, a specific impurity of Cetirizine, is associated with a second-generation antihistamine that serves as the carboxylated metabolite of hydroxyzine. This compound acts as a specific, orally active, and long-acting antagonist of the histamine H1-receptor [1] [2].

Dexbrompheniramine, an orally active H1 receptor antagonist (antihistamine), mitigates the impacts of the natural chemical histamine in the body. It is utilized in the study of hay fever and urticaria [1].

Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic activity. It is a selective antagonist of mycotoxins M1 receptors, exhibiting high (Ki=84 nM, M1 receptors) and low (Ki=1.65 μM, M2 receptors) affinity, with a 20-fold difference. Oxomemazine is an antihistamine and anticholinergic agent used in cough studies[1][2].