Histamine serves as the endogenous ligand for the class of G protein-coupled receptors known as histamine receptors. The H1 receptor, H2 receptor, H3 receptor, and H4 receptor are the four recognized histamine receptors. A member of the family of G-protein-coupled receptors that resemble Rhodopsin is the histamine receptor H1. This receptor, specifically expressed in smooth muscles, vascular endothelial cells, the heart, and the central nervous system, is triggered by the biogenic amine histamine and is found throughout the body. Gs mediates the positive coupling of H2 receptors to adenylate cyclase. It is a strong inducer of cAMP synthesis, which activates Protein Kinase A. Histamine H3 receptors act as autoreceptors in presynaptic histaminergic neurons and regulate histamine turnover by feedback inhibition of histamine synthesis and release. They are expressed in the central nervous system and to a lesser extent the peripheral nervous system. It has been demonstrated that the mast cell chemotaxis and eosinophil shape change are both mediated by the histamine H4 receptor.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V2868 | Clemizole hydrochloride | 1163-36-6 | 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. |
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V18617 | Conessine | 546-06-5 | Conessine is anaturally occurring, steroidal alkaloid extracted froma number of plant species from the family Apocynaceae, including Holarrhena floribunda, Holarrhena antidysenterica and Funtumia elastica. |
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V56025 | CP19 | 1018148-68-9 | CP19 is a histamine receptor antagonist and an entry inhibitor for Ebola virus (EBOV) and Marburg virus (MARV), with IC50s of 3.4 μM and 29.5 μM respectively. |
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V1244 | Cyclizine 2HCl | 5897-18-7 | Cyclizine2HCl (Marezine; Ciclizina; Nautazine; Valoid; Neo-devomit),the dihydrochloride salt of cyclizine, is a potent and 1st generation histamine H1 receptor antagonist of the piperazine class with anticholinergic and antiemetic properties. |
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V1246 | Cyproheptadine HCl | 969-33-5 | Cyproheptadine HCl ( also known as Periactin; Eiproheptadine; Periactinol; Dronactin; Peritol), is a hydrochloride salt form of cyproheptadine that is used as an antimuscarinic and histamine receptor antagonist (antihistamine) to treat pituitary-dependent Cushing's syndrome, anorexia, pruritic dermatoses, and postgastrectomy dumping syndrome. |
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V5075 | Decloxizine HCl (UCB-1402; NSC289116) | 13073-96-6 | Decloxizine (UCB-1402; NSC289116) diHCl is a histamine type 1 receptor H1 antagonist. |
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V1242 | Desloratadine (Sch34117) | 100643-71-8 | 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. |
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V11731 | Diphenhydramine | 58-73-1 | Diphenhydramine HCl is a potent and first-generation histamine H1 receptor antagonist and an antiemetic that is used in various allergic conditions such as rhinitis, urticaria and conjunctivitis. |
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V1221 | Diphenhydramine HCl | 147-24-0 | Diphenhydramine HCl (Dabylen; PM255; PM-255; Debendrin; Difenhydramine), the hydrochloride salt of diphenhydramine, is a 1st-generation histamine H1 receptor antagonist which was approved as an antiemetic for treating various allergic conditions such as rhinitis, urticaria and conjunctivitis. |
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V1228 | Doxylamine Succinate | 562-10-7 | Doxylamine succinate (Decapryn; Unisom; Evigoa D), the succinate salt of Doxylamine, is an antihistamine drug that can be used as monotherapy (short-term sedative) or in combination with other drugs to relieve night-time allergy and cold. |
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V1213 | Ebastine (LAS-W 090; RP64305) | 90729-43-4 | Ebastine (formerly LAS-W 090; RP-64305; LAS W090; RP64305; Ebast, Ebatin, Ebatrol, Atmos, Ebet, Kestine, KestineLIO) is a long-acting and selective H1-histamine receptor antagonist used for the treatment of allergic conditions. |
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V3731 | Emedastine | 87233-61-2 | Emedastine is a novel, potent, high affinity, selective, second generation H1-receptor antagonist with pre-clinically well-documented anti-allergic effects. |
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V3730 | Emedastine Difumarate | 87233-62-3 | Emedastine is a novel, potent, high affinity, selective, second generation H1-receptor antagonist with pre-clinically well-documented anti-allergic effects. |
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V29268 | Epinastine (WAL801) | 80012-43-7 | Epinastine (also known as WAL-801CL HCl) is a potent antihistamine H1 without sedative activity and a mast cell stabilizer that is used in eye drops for the treatment of allergic conjunctivitis. |
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V1214 | Epinastine HCl (WAL801) | 108929-04-0 | Epinastine HCl (WAL801CL; Alesion; Elestat; Epinastine; Epinastin; WAL-801CL), the hydrochloride salt of epinastine, is a potent antagonist of histamine H1 receptors without sedative side effects. |
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V1223 | Famotidine (MK208) | 76824-35-6 | Famotidine (formerly YM-11170, MK208; MK-208, YM11170; Pepcid) is a competitive histamine H2–receptor antagonist with an IC50 of 0.6 mM. |
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V21005 | Fexofenadine | 83799-24-0 | Fexofenadine (MDL-16455A; MDL16455A; Allegra; Terfenidine carboxylate; Telfast) is a histamine H1 receptor antagonist (antihistamine agent) approved for the treatment of allergy symptoms such as hay fever, nasal congestion, and urticaria. |
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V30191 | Fexofenadine D6 | 548783-71-7 | 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. |
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V1217 | Fexofenadine HCl | 153439-40-8 | Fexofenadine HCl (formerly MDL-16455A; Allegra; Terfenidine carboxylate; Telfast) is a potent histamine H1 receptor antagonist (antihistamine agent) used in the treatment of allergy symptoms such as hay fever, nasal congestion, and urticaria. |
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V79407 | Fexofenadine-d3 (MDL-16455-d3; Terfenadine carboxylate-d3) | Fexofenadine-d3 is the deuterated form of Fexofenadine. |
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