H₁ Receptor

H₁ Receptor Related Products (138):

By Type:	Pan (21) Selective (23)
By Effects:	Ligand (1) Inhibitors (19) Agonists (8) Antagonists (105) Modulators (4)

Cat. No.	Product Name	Effect	Purity

HY-B0801AS

Fexofenadine-d₁₀ hydrochloride	Inhibitor
Fexofenadine-d₁₀ (hydrochloride) is deuterium labeled Fexofenadine (hydrochloride). Fexofenadine hydrochloride (MDL-16455 hydrochloride), a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial (person aged ≥16 years)[1].

HY-W062109

Olopatadine	Antagonist
Olopatadine is an orally active and selective histamine 1 (H₁) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis.

HY-B1589AS

Carbinoxamine-d₆ maleate	Antagonist
Carbinoxamine-d₆ (maleate) is the deuterium labeled Carbinoxamine maleate salt. Carbinoxamine maleate salt is a histamine H1 receptor antagonist.

HY-14939A

Vapitadine hydrochloride	Antagonist
Vapitadine hydrochloride (Compound 3a) is a selective, orally active and nonsedating antihistamine agent, which exhibits a good binding affinity with human cloned histamine H1 receptor with a K_i of 19 nM. Vapitadine hydrochloride decreases the histamine-induced lethality (ED₅₀ is 0.056-1.2 mg/kg), antagonizes the cutaneous reactions to histamine (ED₅₀ is 0.51-1.4 mg/kg) in rats.

HY-17428B

Tripelennamine citrate	Antagonist
Tripelennamine citrate, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine citrate lessens the allergic response of the organism caused by histamine. Tripelennamine citrate can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions.

HY-B0548AS2

Hydroxyzine-d₈ dihydrochloride	Antagonist
Hydroxyzine-d₈ (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder[1][2].

HY-B0352S2

Mirtazapine-d₄	Antagonist
Mirtazapine-d₄ is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].

HY-B0524AS1

Betahistine-¹³C,d₃ dihydrochloride	Modulator
Betahistine-¹³C,d₃ (dihydrochloride) is the ¹³C- and deuterium labeled Betahistine (dihydrochloride). Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].

HY-B1397C

Cyclizine hydrochloride	Antagonist
Cyclizine hydrochloride, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine hydrochloride can be used for the research of nausea, vomiting, and dizziness.

HY-B1397A

Cyclizine dihydrochloride	Antagonist
Cyclizine dihydrochloride, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine dihydrochloride can be used for the research of nausea, vomiting, and dizziness.

HY-13511AS

Rupatadine-d₄ fumarate	Antagonist
Rupatadine-d₄ fumarate is a deuterium labeled Rupatadine fumarate. Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with K_i values of 0.55/0.1 μM (rabbit platelet membranes/guinea pig cerebellum membranes).

HY-117501

Dexchlorpheniramine	Antagonist
Dexchlorpheniramine is an potent and blood-brain barrier (BBB) penetrant histamine 1 (H1) receptor antagonist with anticholinergic properties. Dexchlorpheniramine can be used for researching allergies.

HY-164010

SUN-1334H free base	Inhibitor
SUN-1334H free base is an orally active inhibitor for histamine H1 receptor, with an IC₅₀ of 20.3 nM and K_i of 9.7 nM. SUN-1334H free base inhibits histamine-induced contractions of isolated guinea-pig ileum with an IC₅₀ of 0.198 μM. SUN-1334H free base inhibits histamine-induced bronchoconstriction in guinea pigs, histamine-induced skin wheals in beagle dogs, and ovalbumin-induced rhinitis in guinea pigs.

HY-A0027AS

Fenspiride-d₅	Antagonist
Fenspiride-d₅ is the deuterium labeled Fenspiride. Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases[1][2][3].

HY-B1397B

Cyclizine lactate	Antagonist
Cyclizine lactate, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine lactate can be used for the research of nausea, vomiting, and dizziness.

HY-B0548AS1

Hydroxyzine-d₄ dihydrochloride	Antagonist	≥98.0%
Hydroxyzine-d₄ (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder[1][2].

HY-10121B

Asenapine citrate	Antagonist
Asenapine citrate, an atypical antipsychotic, is an antagonist of serotonin receptors (pK_i: 8.4-10.5), adrenoceptors (pK_i: 8.9-9.5), dopamine receptors (pK_i: 8.9-9.4) and histamine receptors (pK_i: 8.2-9.0). Asenapine citrate can be used in the research of schizophrenia and bipolar disorder.

HY-B0971A

Pheniramine	Antagonist
Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects.

HY-A0027A

Fenspiride	Antagonist
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC₅₀ values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.

HY-106957

Efletirizine	Antagonist
Efletirizine (EFZ) is an orally active antihistamine with high selectivity and affinity to the H₁-receptor. Efletirizine can be used for allergic disease research.

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