← Mechanisms of action
HRH1
SINGLE PROTEINHomo sapiens
Preferred name: Histamine H1 receptor ChEMBL ↗
Linked proteins
Drugs acting on this target (77)
| Active Pharmaceutical Ingredient | Mechanism Type ▲ | Approval Status | API Type | Mechanism of Action |
|---|---|---|---|---|
| betahistine mesilate | Agonist | experimental | Small molecule | HRH1 agonist |
| histamine | Agonist | approved | Small molecule | HRH1 agonist |
| acrivastine (Semprex-D) | Antagonist | approved | Small molecule | HRH1 antagonist |
| alcaftadine (Lastacaft) | Antagonist | approved | Small molecule | HRH1 antagonist |
| alimemazine (temaril) | Antagonist | approved | Small molecule | HRH1 antagonist |
| antazoline (vasocon-a) | Antagonist | approved | Small molecule | HRH1 antagonist |
| antazoline phosphate (Vasocon A) | Antagonist | approved | Small molecule | HRH1 antagonist |
| astemizole (Hismanal) | Antagonist | withdrawn | Small molecule | HRH1 antagonist |
| azatadine (optimine) | Antagonist | approved | Small molecule | HRH1 antagonist |
| azelastine (astelin) | Antagonist | approved | Small molecule | HRH1 antagonist |
| bepotastine (bepreve) | Antagonist | approved | Small molecule | HRH1 antagonist |
| brompheniramine maleate (dimetane) | Antagonist | approved | Small molecule | HRH1 antagonist |
| buclizine | Antagonist | approved | Small molecule | HRH1 antagonist |
| carbinoxamine maleate (clistin) | Antagonist | approved | Small molecule | HRH1 antagonist |
| cetirizine (zyrtec) | Antagonist | approved | Small molecule | HRH1 antagonist |
| chlorpheniramine (ChlorTrimeton) | Antagonist | approved | Small molecule | HRH1 antagonist |
| chlorphenoxamine | Antagonist | experimental | Small molecule | HRH1 antagonist |
| cinnarizine (Stugeron) | Antagonist | experimental | Small molecule | HRH1 antagonist |
| clemastine (TAVIST) | Antagonist | approved | Small molecule | HRH1 antagonist |
| cyclizine lactate (marezine) | Antagonist | approved | Small molecule | HRH1 antagonist |
| cyproheptadine (periactin) | Antagonist | approved | Small molecule | HRH1 antagonist |
| desloratadine (clarinex) | Antagonist | approved | Small molecule | HRH1 antagonist |
| dexbrompheniramine (disomer) | Antagonist | approved | Small molecule | HRH1 antagonist |
| dexchlorpheniramine maleate (polaramine) | Antagonist | approved | Small molecule | HRH1 antagonist |
| dibenzepin hydrochloride | Antagonist | experimental | Small molecule | HRH1 antagonist |
| dimenhydrinate | Antagonist | approved | Small molecule | HRH1 antagonist |
| dimetindene | Antagonist | experimental | Small molecule | HRH1 antagonist |
| diphenhydramine (benadryl) | Antagonist | approved | Small molecule | HRH1 antagonist |
| diphenylpyraline (hispril) | Antagonist | approved | Small molecule | HRH1 antagonist |
| doxepin (sinequan) | Antagonist | approved | Small molecule | HRH1 antagonist |
| doxylamine | Antagonist | approved | Small molecule | HRH1 antagonist |
| Ebastine (kestine) | Antagonist | experimental | Small molecule | HRH1 antagonist |
| emedastine (emadine) | Antagonist | approved | Small molecule | HRH1 antagonist |
| epinastine (elestat) | Antagonist | approved | Small molecule | HRH1 antagonist |
| fexofenadine (allegra) | Antagonist | approved | Small molecule | HRH1 antagonist |
| fludiazepam | Antagonist | experimental | Small molecule | HRH1 antagonist |
| gsk-1004723 | Antagonist | experimental | Small molecule | Histamine H1 receptor antagonist |
| hydroxyzine (vistaril) | Antagonist | approved | Small molecule | HRH1 antagonist |
| ketotifen (zaditor) | Antagonist | approved | Small molecule | HRH1 antagonist |
| levocabastine (livostin) | Antagonist | approved | Small molecule | HRH1 antagonist |
| levocetirizine (xyzal) | Antagonist | approved | Small molecule | HRH1 antagonist |
| loratadine (claritin) | Antagonist | approved | Small molecule | HRH1 antagonist |
| ly2624803 | Antagonist | experimental | Small molecule | HRH1 antagonist |
| meclizine (antivert) | Antagonist | approved | Small molecule | HRH1 antagonist |
| mepyramine | Antagonist | approved | Small molecule | HRH1 antagonist |
| methapyrilene | Antagonist | experimental | Small molecule | HRH1 antagonist |
| methapyrilene fumarate | Antagonist | experimental | Small molecule | HRH1 antagonist |
| methdilazine (tacaryl) | Antagonist | approved | Small molecule | HRH1 antagonist |
| mirtazapine (remeron) | Antagonist | approved | Small molecule | HRH1 antagonist |
| Mizolastine (zolistan) | Antagonist | experimental | Small molecule | Histamine H1 receptor antagonist |
| nipolazin | Antagonist | experimental | Small molecule | Histamine H1 receptor antagonist |
| olopatadine (patanol) | Antagonist | approved | Small molecule | HRH1 antagonist |
| orphenadrine hydrochloride (disipal) | Antagonist | approved | Small molecule | HRH1 antagonist |
| phenindamine | Antagonist | experimental | Small molecule | Histamine H1 receptor antagonist |
| pheniramine (Tripoton) | Antagonist | approved | Small molecule | HRH1 antagonist |
| promethazine hydrochloride (phenergan) | Antagonist | approved | Small molecule | HRH1 antagonist |
| propiomazine (largon) | Antagonist | approved | Small molecule | HRH1 antagonist |
| rupatadine | Antagonist | experimental | Small molecule | HRH1 antagonist |
| terfenadine (Seldane) | Antagonist | approved | Small molecule | HRH1 antagonist |
| thenalidine | Antagonist | experimental | Small molecule | HRH1 antagonist |
| theophylline (synophylate) | Antagonist | approved | Small molecule | Histamine H1 receptor antagonist |
| trimipramine (surmontil) | Antagonist | approved | Small molecule | HRH1 antagonist |
| tripelennamine | Antagonist | approved | Small molecule | HRH1 antagonist |
| triprolidine (Actidil) | Antagonist | approved | Small molecule | HRH1 antagonist |
| vapitadine dihydrochloride | Antagonist | experimental | Small molecule | HRH1 antagonist |
| Mizolastine (zolistan) | Binding agent | experimental | Small molecule | HRH1 binding agent |
| norketotifen | Blocker | experimental | Small molecule | HRH1 blocker |
| chlorcyclizine | Inhibitor | experimental | Small molecule | HRH1 inhibitor |
| gsk-1004723 | Inhibitor | experimental | Small molecule | HRH1 inhibitor |
| mebhydrolin napadisilate | Inhibitor | experimental | Small molecule | HRH1 inhibitor |
| methylpropanolamine | Inhibitor | experimental | Small molecule | HRH1 inhibitor |
| oxomemazine | Inhibitor | experimental | Small molecule | HRH1 inhibitor |
| phenyltoxamine | Inhibitor | experimental | Small molecule | HRH1 inhibitor |
| rev131 | Inhibitor | experimental | Small molecule | HRH1 inhibitor |
| sparc1102 | Inhibitor | experimental | Small molecule | HRH1 inhibitor |
| bilastine | Inverse agonist | experimental | Small molecule | HRH1 inverse agonist |
| Ebastine (kestine) | Inverse agonist | experimental | Small molecule | Histamine H1 receptor inverse agonist |