H₁ Receptor Agonist

Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.

N-Methylhistamine dihydrochloride (Nα-Methylhistamine dihydrochloride) is a non-selective Histamine receptor agonist. N-Methylhistamine dihydrochloride activates histamine H₁, H₂ and H₃ receptors; it stimulates central H₁ receptors by activating sympathetic α and β adrenergic receptors to inhibit intestinal transit, exerts dose-dependent inhibition on intestinal transit, reduces histamine turnover in mouse brains, and increases gastric acid secretion without altering plasma gastrin concentrations. N-Methylhistamine dihydrochloride produces a pH-dependent, voltage-independent potentiating effect on acid-sensing ion channel 1a, and shows no significant activity toward homologous ASIC2a channels. N-Methylhistamine dihydrochloride can be used in studies related to Helicobacter pylori infection.

HTMT (dimaleate) is a potent histamine H1 and H2 receptor agonist. HTMT (dimaleate) is 4 x 10⁴ times more active than histamine in H2-mediated effects in natural suppressor cells.

Loratadine-d₅ is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.

Loratadine-d₄ is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.

H3R antagonist 5 (Compound 1b) is a selective histamine H3 receptor inverse agonist with a IC₅₀ of 0.54 nM and the ability to cross the blood-brain barrier. H3R antagonist 5 can be used in central nervous system-related research.

UR-AK49 (compound 11) is a human histamine H1 and H2 receptor agonist. UR-AK49 has an EC₅₀ of 23 nM in a GTPase assay with hH2R-Gsalpha fusion protein expressed in Sf9 insect cells. UR-AK49 can be used in neuro-related research.

Emedastine difumarate is an orally active, selective and high affinity histamine H₁ receptor antagonist with a K_i value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.

Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties.