ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist/inverse agonist developed by Abbott with stimulant and nootropic effects, and has been investigated as a treatment for ADHD, Alzheimer’s disease, and schizophrenia.
Lidocaine (Alphacaine; NSC-40030; NSC40030; Lignocaine), a local anesthetic and cardiac depressant used as an antiarrhythmia agent, is a potent and selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.
Lafutidine (formerly FRG-8813; FRG8813; trade name: Protecadin; Stogar) is a 2nd-generation histamine H2 receptor antagonist used to treat gastric ulcers, duodenal ulcers, and wounds in the stomach associated with chronic gastritis.
Tripelennamine HCl (Pyrinamine; Stanzamine; Tripelennamine; Pyribenzamine), the hydrochloride salt of Tripelennamine, is a potent histamine H1 receptor antagonist that has been widely used as an antipruritic agent.
Desloratadine (formerly SCH34117, NSC 675447; SCH-34117, NSC-675447; Clarinex; Neoclarityn; Descarboethoxyloratadine; Aerius) is the active metabolite of loratadine which is an anti-histamine drug of the tricyclic class used to treat allergies.
Clemizole hydrochloride (also known as AL 20 HCl, P 48 HCl, and/or Reactrol), is a potent inhibitor of transient receptor potential channel TRPC5 (Canonical transient receptor potential channel 5) and also an H1 histamine receptor antagonist.
Lodoxamide Tromethamide (U-42585E), the Tromethamide salt of Lodoxamide, is an antiallergic drug acting as a potent GPR35 agonist with an EC50 of 1.61 nM in a β-arrestin-2 interaction assay using CHO-K1 cells expressing the human receptor.
Nizatidine (Tazac, Axid, LY-139037, LY 139037, LY139037) is a potent histamine H2 receptor antagonist used in the treatment of peptic ulcer disease and gastroesophageal reflux disease.
Levodropropizine [(S)-(-)-Dropropizine; DF 526; DF-526; DF526; Levotuss], the S-isomer of dropropizine, is a histamine receptor inhibitor used as a cough suppressant.
Fexofenadine D6 is the hexa-deuterated form of Fexofenadine (MDL-16455A; Allegra; MDL16455A; Telfast), which is a histamine H1 receptor antagonist (antihistamine) approved for the treatment of allergy including hay fever, nasal congestion, and urticaria.