Histamine Receptor
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| FB10831 | VUF 10460 | 1028327-66-3 | VUF 10460 is a selective agonist of histamine H4 receptor with pKi of 8.22. |
| FB00591 | Triprolidine HCl | 6138-79-0 | Triprolidine Hydrochloride is the first generation histamine H1 antagonist used in allergic rhinitis. |
| FB00118 | Thioperamide | 106243-16-7 | Thioperamide is a potent HRH4 antagonist and selective HRH3 antagonist capable of crossing the blood–brain barrier. |
| FB03737 | Setastine | 64294-95-7 | Setastine is an antihistamine used to treat allergies and rhinitis. |
| FB11275 | S 38093 HCl | 1222097-72-4 | S 38093 is an inverse agonist of H3 receptor. |
| FB11676 | S 38093 | 862896-30-8 | S 38093 is a brain-penetrant antagonist/inverse agonist of H3 receptors. |
| FB17266 | PU-02 | 313984-77-9 | PU-02 is an antagonist of serotonin (5-HT) receptor subtype 5-HT3. |
| FB08054 | Promethazine HCl | 58-33-3 | Promethazine HCl is the effective antagonist of the H1 receptor and moderate antagonist of mACh receptor. |
| FB04924 | Pitolisant Oxalate | 362665-57-4 | Pitolisant oxalate is a potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). |
| FB09742 | Pitolisant | 362665-56-3 | Pitolisant is a potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). |
| FB06924 | Pitolisant HCl | 903576-44-3 | Pitolisant HCl is an inverse agonist of human H3 receptor with Ki of 0.16 nM. |
| FB08432 | Pirolate | 55149-05-8 | Pirolate (CP-32,387) is an antihistamine drug with a tricyclic chemical structure which was patented as an "antiallergen". |
| FB09953 | Osthole | 484-12-8 | Osthole, an O-methylated coumarin, is a histamine H1 receptor inhibitior. It exhibits immunomodulatory, antioxidative and anti-inflammatory activities. |
| FB07679 | N-omega-Acetylhistamine | 673-49-4 | N-acetylhistamine is a histamine metabolite. N-acetylhistamine can be used as a potential biomarker of histidine metabolism for anaphylactoid reactions. |
| FB01972 | Mizolastine 2HCl | 1056596-82-7 | Mizolastine 2HCl is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. |
| FB03008 | Mebhydrolin | 524-81-2 | Mebhydrolin is a specific histamine H1 receptor antagonist. |
| FB05091 | Marmin | 14957-38-1 | Marmin, a natural product isolated and purified from the herbs of Citrus maxima with potent anti-ulcer, antibacterial, fungicidal, and algicidal properties, can inhibit contraction of the guinea-pig tracheal smooth muscle, especially by interfering histamine receptor, inhibiting the histamine release from mast, inhibiting intracellular Ca2+ release from the intracellular store and the Ca2+ influx through voltage-dependent Ca2+ channels, is potential to develop as antihistamine agents, especially as histamine H1 receptor antagonists by interacting with amino acid residues, Asp107, Lys179, Lys191, Asn198, and Trp428 of histamine H1 receptor, shows a cell-growth inhibitory effect against L1210 and K562 in vitro. |
| FB16770 | LML-134 | 1542135-76-1 | LML134 is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders. |
| FB09822 | Ketotifen Fumarate | 34580-14-8 | Ketotifen fumarate is a noncompetitive H1 receptor antagonist and mast cell stabilizer that is used to treat asthma. |
| FB11002 | JNJ10181457 | 544707-19-9 | JNJ10181457 is a histamine H3 receptor inverse agonist that regulates in vivo microglial functions and improves depression-like behaviours in mice. |
| FB08517 | JNJ-7777120 | 459168-41-3 | JNJ-7777120 is a selective antagonist of histamine-4 receptor (H4R) with Ki of 4 ± 1 nM. |
| FB16478 | JNJ-5207852 | 398473-34-2 | JNJ-5207852 is a novel, non-imidazole histamine H3 receptor antagonist, with high affinity at the rat (pKi=8.9) and human (pKi=9.24) H3 receptor. |
| FB09118 | Hydroxyzine | 68-88-2 | Hydroxyzine is a histamine H1-receptor antagonist. |
| FB11761 | H3R-IN-1 HCl | 2319790-07-1 | H3R-IN-1 HCl is a histamine receptor 3 (H3R) inverse agonist. |
| FB10302 | GSK189254A | 720690-73-3 | GSK189254A is a potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively. |
| FB00062 | Famotidine | 76824-35-6 | Famotidine is antagonist of histamine H2–receptor with IC50 of 0.6 mM that used to treat heartburn and other digestive conditions. |
| FB07752 | Epinastine | 80012-43-7 | Epinastine is mast cell stabilizer and antihistamine that is used to treat allergic conjunctivitis. |
| FB03530 | Diphenylpyraline HCl | 132-18-3 | Diphenylpyraline HCl is a first-generation antihistamine with anticholinergic effects, acts as a dopamine reuptake inhibitor, shows to be useful in the treatment of Parkinsonism. |
| FB00057 | Cyclizine | 82-92-8 | Cyclizine, a piperazine derivative, is an antihistaminic antiemetic that is useful in the prevention and treatment of nausea and vomiting associated with motion sickness. |
| FB12142 | Cyclizine 2HCl | 5897-18-7 | Cyclizine is a histamine H1 receptor antagonist of the piperazine class. |
| FB00058 | Cyclizine HCl | 303-25-3 | Cyclizine HCl is a piperazine derivative with anti-emetic activity that is useful in the prevention and treatment of nausea and vomiting associated with motion sickness. |
| FB11264 | Clobenpropit Dihydrobromide | 145231-35-2 | Clobenpropit hydrobromide is a selective histamine H3 receptor antagonist that crosses the blood-brain barrier, inhibiting histamine binding in rat brain. |
| FB04026 | Ciproxifan | 184025-18-1 | Ciproxifan is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes. |
| FB03365 | Cipralisant | 213027-19-1 | Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has entered in clinical trials for the treatment of attention-deficit hyperactivity disorder. |
| FB15319 | Chlorcyclizine HCl | 14362-31-3 | Chlorcyclizine hydrochloride is a histamine H1 antagonist. |
| FB16471 | Bromazine HCl | 1808-12-4 | Bromazine hydrochloride is an antagonist of histamine H1 receptor. |
| FB11789 | BMY-25271 | 78441-82-4 | BMY-25271 is a histamine H2 receptor antagonist. |
| FB16386 | Betahistine | 5638-76-6 | Betahistine is a histamine analog and H1 receptor agonist. |
| FB08413 | Betahistine 2HCl | 5579-84-0 | Betahistine 2HCl is histamine H3 receptor inhibitor with IC50 of 1.9 μM. It is an antivertigo drug. |
| FB15554 | Bepotastine | 125602-71-3 | Bepotastine is a non-sedating and selective antagonist of the histamine 1 (H1) receptor. |
| FB06961 | Bavisant | 929622-08-2 | Bavisant is a highly selective, orally active antagonist of the human H3 receptor with a mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. |
| FB02260 | Bavisant 2HCl H2O | 1103522-80-0 | Bavisant HCl is a highly selective, orally active antagonist of the human H3 receptor with a mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. |
| FB06962 | Bavisant 2HCl | 929622-09-3 | Bavisant HCl is a highly selective, orally active antagonist of the human H3 receptor with a mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. |
| FB08734 | Azelastine | 58581-89-8 | Azelastine is a potent, second-generation, selective, histamine antagonist. |
| FB00120 | Azelastine HCl | 79307-93-0 | Azelastine HCl is a selective antagonist of histamine receptor used in the treatment of rhinitis. |
| FB11862 | Antihistamine-1 | 1186430-60-3 | Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively. |
| FB02571 | Antazoline HCl | 2508-72-7 | Antazoline HCl is a antihistamine with anticholinergic properties. It is used to relieve nasal congestion. |
| FB16887 | ACV 1 | 740980-24-9 | ACV 1 is neuronal nicotinic receptor antagonist of α9α10, α6/α3β2β3, α6/α3β4, α3β4 and α3β2 subtypes with IC50s of 19, 140, 980, 4200 and 7300 nM, respectively. |
| FB12859 | 5-Hydroxyindole-3-acetic acid | 54-16-0 | 5-Hydroxyindole-3-acetic acid (5-HIAA), the major metabolite of serotonin, is a histamine H1 receptor antagonist and can be used to treat allergies. |
| FB17260 | 4I | 930478-88-9 | 5-HT3 antagonist-4i is a 5-HT3 receptor antagonist which modulates the serotonergic system. |