| S1847 |
Clemastine (HS-592) Fumarate
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Clemastine fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
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Journal of Cerebral Blood Flow & Metabolism, March 2026, 786-803
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Translational Research, June 2024, 40-50
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Neurochemical Research, February 2022, 503-515
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| S3037 |
Bepotastine Besilate
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Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
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iScience, 2024, 27(10):110862
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J Pers Med, 2022, 12(2)258
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Journal of Cellular Biochemistry, 2022, 673-690
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| S1358 |
Loratadine
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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.
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Anticancer Research, July 2019, 3767-3775
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Front Cell Infect Microbiol, 2024, 14:1358873
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BMC Pharmacol Toxicol, 2024, 25(1):25
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| S1357 |
Lidocaine
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Lidocaine (Alphacaine) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.
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ACS Applied Materials & Interfaces, March 09, 2023, 13892-13906
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Journal of Inflammation Research, June 17, 2025, 7907-7919
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Anticancer Research, July 15, 2019, 3767-3775
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| S2552 |
Azelastine HCl
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Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.
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Biomed Pharmacother, 2024, 176:116766
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UNIVERSITY OF PÉCS, 2023,
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Front Pharmacol, 2022, 13:861295
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| S2905 |
JNJ-7777120
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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.
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Front Microbiol, 2022, 13:802409
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J Assoc Res Otolaryngol, 2021, 10.1007/s10162-021-00803-5
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Neuropharmacology, 2020, 168:108028
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| S2044 |
Cyproheptadine HCl
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Cyproheptadine HCl(Periactin) is a hydrochloride salt form of cyproheptadine which is a histamine receptor antagonist.
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Anticancer Research, July 2019, 3767-3775
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Frontiers in Pharmacology, April 08 2025, 16:1539032
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Front Pharmacol, 2025, 16:1539032
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| S2078 |
Famotidine
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Famotidine (MK208) is a histamine H2–receptor antagonist with IC50 of 0.6 mM, commonly used to treat heartburn, GERD, ulcers, and other digestive conditions.
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BMC Pharmacology and Toxicology, October 22, 2021, 62
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Anticancer Research, July 2019, 3767-3775
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Calcified Tissue International, December 2021, 696-705
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| S1382 |
Mianserin HCl
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Mianserin (Bolvidon, Norval, Tolvon,ORG GB-94 HCl,Mianserin hydrochloride) is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression.
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Communications Medicine, 2025, 420
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Alzheimers Dement, 2023, 10.1002/alz.13090
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Proceedings of the National Academy of Sciences, 2021, e2026403118
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| S1801 |
Ranitidine Hydrochloride
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Ranitidine (AH19065) is a histamine H2-receptor antagonist, used to treat stomach or intestinal ulcers.
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Anticancer Research, July 2019, 3767-3775
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bioRxiv, 2023, Preprint
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Calcif Tissue Int, 2021, 109(6):696-705
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