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Histamine Receptor

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Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S1847 Clemastine (HS-592) Fumarate Clemastine fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
Nat Commun, 2025, 16(1):1709
Nat Commun, 2025, 16(1):6382
Biomed Pharmacother, 2025, 185:117916
Verified customer review of Clemastine (HS-592) Fumarate
S3037 Bepotastine Besilate Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
iScience, 2024, 27(10):110862
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1358 Loratadine Loratadine is a histamine H1 receptor antagonist, used to treat allergies. This compound also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
Front Cell Infect Microbiol, 2024, 14:1358873
BMC Pharmacol Toxicol, 2024, 25(1):25
Cancer Cell, 2022, S1535-6108(22)00312-9
S2552 Azelastine HCl Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.
Biomed Pharmacother, 2024, 176:116766
UNIVERSITY OF PÉCS, 2023,
Front Pharmacol, 2022, 13:861295
S1357 Lidocaine Lidocaine (Alphacaine) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.
J Inflamm Res, 2025, 18:7907-7919
Cell Rep, 2022, 38(10):110468
Exp Ther Med, 2021, 21(5):424
S2905 JNJ-7777120 JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.
Front Microbiol, 2022, 13:802409
J Assoc Res Otolaryngol, 2021, 10.1007/s10162-021-00803-5
Neuropharmacology, 2020, 168:108028
S2044 Cyproheptadine HCl Cyproheptadine HCl(Periactin) is a hydrochloride salt form of cyproheptadine which is a histamine receptor antagonist.
Front Pharmacol, 2025, 16:1539032
World J Gastroenterol, 2023, 29(20):3103-3118
Cell Rep, 2020, 21;31(3):107548
S1291 Cetirizine DiHCl Cetirizine DiHCl (Zyrtec, Reactine,UCB P071) is an antihistamine.
Viruses, 2024, 16(10)1559
Environ Toxicol Chem, 2021, 10.1002/etc.5018
J Allergy Clin Immunol, 2017, 139(4):1253-1265
Verified customer review of Cetirizine DiHCl
S1845 Cimetidine Cimetidine (SKF-92334), a histamine congener, competitively inhibits histamine binding to histamine H2 receptors.
Cell Rep, 2021, 34(10):108832
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931
S1890 Nizatidine Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.
Gastroenterology, 2022, 162(4):1210-1225
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931

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