antihistamine

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).

Dimethindene (Dimetindeno) is a selective antagonist of H1 receptor and blocks K+ current. Dimethindene exhibits antihistamine and anticholinergic effects.

Vapitadine is a non-sedative antihistamine compound that relieves itching caused by atopic dermatitis.

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.

Fexofenadine (Carboxyterfenadine), an antihistamine pharmaceutical drug, is used to treat allergy symptoms, such as nasal congestion, hay fever, and urticaria. Compared to first-generation antihistamines, Fexofenadine is less able to pass the blood-brain barrier and cause sedation.

Azelastine (Azelastinum) is a phthalazine derivative, and is an histamine antagonist and mast cell stabilizer.

Thonzylamine hydrochloride (Resistab) is an anticholinergic and antihistamine used as an antipruritic.

Mianserin, an H1 receptor reverse agonist, is a psychoactive compound in the tetracyclic antidepressant (TeCA) treatment family. Mianserin has antidepressant, antianxiety, antiemetic, hypotrophic, hypnotic and antihistamine effects, and can be used as a combination of norepinephrine and specific serotonin to treat depression.

Azaphen (Pipofezin hydrochloride) is the reuptake of serotonin inhibitor.with antidepressant action and has sedative effects, suggesting antihistamine activity.

Cetirizine Impurity B dihydrochloride (De(carboxymethoxy) Cetirizine Acetic Acid Dihydrochloride) is an impurity of Cetirizine dihydrochloride. Cetirizine is a second-generation antihistamine. Cetirizine is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.

Noberastine (R 64947) is a novel histamine H1 antagonist with potent and specific peripheral antihistamine activity.

Oxatomide (Oxatomida) is a potent and orally active dual H1 histamine receptor and P2X7 receptor antagonist with antihistamine and antiallergic activity.Oxatomide can be used to block ATP-induced currents in the human P2X7 receptor with an IC50 value of 0.95 μM.Oxatomide has an inhibitory effect on ATP-induced Ca2+ inward currents with an IC50 value of 0.43 μM.Oxatomide inhibits 5-hydroxytryptamine. Oxatomide inhibits 5-hydroxytryptamine with an IC50 of 0.43 μM.Oxatomide is used in the treatment of immune system diseases and in the study of hypersensitivity reactions.

Dexchlorpheniramine Maleate (S-(+)-Chlorpheniramine maleate salt) is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria. It is the pharmacologically active dextrorotatory isomer of chlorpheniramine.

Azelastine hydrochloride (Astelin) is a phthalazinone derivative with antihistaminergic activity.

Antazoline hydrochloride (Phenazoline hydrochloride), a first-generation antihistamine, can bind to the histamine H1 receptor and block the action of endogenous histamine.

Olopatadine, an antihistamine, as well as anticholinergic and mast cell stabilizer, is used for the treatment of itching associated with allergic conjunctivitis (eye allergies). There is also a potential for Olopatadine to treat steroid rebound (red skin

Promethazine hydrochloride (Promethazine HCl) , the first-generation antihistamine, is a strong antagonist of the H1 receptor and a moderate antagonist of the mACh receptor, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.

Astemizole (Laridal) is a synthetic piperidinyl-benzimidazol derivative with antiallergic properties, acts as a reversible competitive inhibitor of histamine H1 receptors, with less anticholinergic effects compared to related agents. It is a long-acting, non-sedative antihistaminic used in the treatment of seasonal allergic rhinitis, asthma, allergic conjunctivitis, and chronic idiopathic urticaria.

Niaprazine is a histamine H1-receptor antagonist with marked sedative properties. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research[1][2]. Niaprazine exhibits a low affinity for the vesicular monoamine transporter and for D2, α2, β, H1 and mAch receptors. Niaprazine, particularly the (+)stereoisomer, has a higher affinity for α1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, but is poorly recognized by 5-HT1A and 5-HT1B binding sites[2]. Niaprazine (60 mg/kg; i.p.; once) treatment increases rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 min after treatment, and reduced them at 3-8 hr after treatment. Niaprazine also produces a short-lasting depletion of rat brain noradrenaline (NA) and dopamine (DA)[3]. Animal Model: Male Sprague-Dawley rats (150-200 g)[3] [1]. D Scherman, et al. Molecular pharmacology of niaprazine. Prog Neuropsychopharmacol Biol Psychiatry. 1988;12(6):989-1001. [2]. P G Rossi, et al. Niaprazine in the treatment of autistic disorder. J Child Neurol. 1999 Aug;14(8):547-50. [3]. P E Keane, et al. The effect of niaprazine on the turnover of 5-hydroxytryptamine in the rat brain. Neuropharmacology. 1982 Feb;21(2):163-9.

Brompheniramine maleate (Dimotane) is an antagonist against histamine H1 receptors.

Propiomazine Hydrochloride is an antihistamine that blocks H1 receptors.

Tofenacin (free base) is an antidepressant drug with a tricyclic-like structure. It acts as a serotonin-norepinephrine reuptake inhibitor, and based on its close relation to orphenadrine, may also possess anticholinergic and antihistamine properties. Tofenacin is also the major active metabolite of orphenadrine and likely plays a role in its beneficial effects against depressive symptoms seen in Parkinson's disease patients.

Alcaftadine is a novel antihistamine for preventing allergic conjunctivitis.

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.

Dothiepin HCl is a Tricyclic antidepressant (TCA), acting as a serotonin–norepinephrine reuptake inhibitor (SNRI) and also having other activities including antihistamine, antiadrenergic, antiserotonergic, anticholinergic, and sodium channel-blocking effects.

Oxetorone fumarate is a serotonin antagonist, antihistamine, and alpha-blocker. It was used as an antimigraine drug.

Antazoline has antihistamine and anticholinergic effects.It used to treat a variety of arrhythmias.

Alimemazine D6 is a deuterium-labeled Alimemazine. Alimemazine is an antihistamine.

Cetirizine D4 dihydrochloride is a deuterium-labeled Cetirizine. Cetirizine is a second-generation antihistamine and a long-acting histamine H1-receptor antagonist.

Epinastine hydrochloride (WAL-801CL HCl) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.

Diafen NN is an antihistamine agent.

Brompheniramine ((±)-Brompheniramine) is a potent and orally active alkylamine class antihistamine. Brompheniramine is a selective antagonist of histamine H1 receptor (Kd = 6.06 nM). Brompheniramine can be used in the research of allergic rhinitis that has anticholinergic, antidepressant and anesthetic properties. Brompheniramine can block the calcium channels, sodium channels, and hERG channels with IC 50 s of 16.12 μM, 21.26 μM, and 0.90 μM, respectively [1] [2] [3] [4].

Buclizine is an orally active antihistamine, antiallergic compound. buclizine is also a strong teratogen in rats and exhibits antitumour effects.

Mianserin-d3 is a deuterated compound of Mianserin. Mianserin has a CAS number of 24219-97-4. Mianserin, an H1 receptor reverse agonist, is a psychoactive compound in the tetracyclic antidepressant (TeCA) treatment family. Mianserin has antidepressant, antianxiety, antiemetic, hypotrophic, hypnotic and antihistamine effects, and can be used as a combination of norepinephrine and specific serotonin to treat depression.

Bilastine-d6 is a deuterated compound of Bilastine. Bilastine has a CAS number of 202189-78-4. Bilastine is a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action.

Bilastine-d4 is a deuterated compound of Bilastine. Bilastine has a CAS number of 202189-78-4. Bilastine is a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action.

Cetirizine Impurity D is an impurity of Cetirizine. Cetirizine is a second-generation antihistamine that acts as a specific, orally active, and long-acting antagonist of the histamine H1-receptor. Cetirizine exhibits antiallergic properties and inhibits eosinophil chemotaxis in response to allergies.

Captodiame is an antihistamine agent.

(S)-Azelastine is an antihistamine which has been shown to down-regulate H1R, M1R and M3R levels. This compound has also been shown to inhibit HNEpC proliferation.

AHR-14310C is a long-acting and nonsedating H1-antihistamine.

Phenindamine Tartrate is an antihistamine and anticholinergic drug closely related to cyproheptadine. It is used to treat symptoms of the common cold and allergies, such as sneezing, itching, rashes, and hives.

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

Propiomazine is an orally active antihistamine agent that possesses sedative properties. It finds utility in insomnia research [1] [2].

Cinnarizine D8 is a deuterium-labeled Cinnarizine which is an antihistamine and a calcium channel blocker.

Chlophedianol hydrochloride, a centrally acting cough suppressant, is used in the treatment of dry cough. It has antihistamine and local anesthetic properties, and may have anticholinergic effects at high doses.

Ebastine (Kestine) (trade names Evastin, Kestine, Ebastel, Aleva) is a non-sedating H1 antihistamine. It does not penetrate the blood-brain barrier and thus allows an effective block of the H1 receptor in peripheral tissue without a central side effect, i. e not causing sedation or drowsiness.

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

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

(R)-Azelastine hydrochloride is an antihistamine which has been shown to down-regulate H1R, M1R and M3R levels. This compound has also been shown to inhibit HNEpC proliferation.

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

Pipofezine(Azafen or Azaphen) is a potent inhibitor of the reuptake of serotonin. IC50 Value: Target: SSRIs Pipofezine is a tricyclic antidepressant (TCA) approved in Russia for the treatment ofdepression. In addition to its antidepressant action, pipofezine has sedative effects as well, indicating antihistamine activity.