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Antagonists

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Description
Biochem/physiol Actions
CAS Number
Product #
(±)-Brompheniramine maleate salt Antihistamine; H1 histamine receptor antagonist.
 980-71-2 B2390
(±)-Chlorpheniramine maleate salt ≥99% (perchloric acid titration) H1 Histamine receptor antagonist.
 113-92-8 C3025
3-(1H-Imidazol-4-yl)propyl di(p-fluorophenyl)methyl ether hydrochloride powder H3 histamine receptor antagonist.
 I160
A-331440 dihydrochloride ≥98% (HPLC), solid A-331440 dihydrochloride is a non-imidazole H3 histamine receptor antagonist. Presynaptic histamine H(3) receptors regulate release of histamine and other neurotransmitters, and histamine H(3) receptor antagonists enhance neurotransmitter release. A-331440 is a histamine H(3) receptor antagonist, which binds potently and selectively to both human and rat histamine H(3) receptors (K(i)=25 nM). Mice on a high-fat diet (45 kcal % lard) prior to 28-day oral b.i.d. dosing for measurement of obesity-related parameters. A-331440 administered at 0.5 mg/kg had no significant effect on weight, whereas 5 mg/kg decreased weight comparably to dexfenfluramine (10 mg/kg). A-331440 administered at 15 mg/kg reduced weight to a level comparable to mice on the low-fat diet. The two higher doses reduced body fat and the highest dose also normalized an insulin tolerance test. Both data shows that the histamine H(3) receptor antagonist, A-331440, has potential as an antiobesity agent.
 392338-13-5 (free base) A7730
A-331440 L-tartrate hydrate ≥98% (HPLC), solid Histamine affects homeostatic mechanisms, including food and water consumption, by acting on central nervous system (CNS) receptors. Presynaptic histamine H3 receptors regulate release of histamine and other neurotransmitters, and histamine H3 receptor antagonists enhance neurotransmitter release. A-331440 [4'-[3-(3(R)-(dimethylamino)-pyrrolidin-1-yl)-propoxy]-biphenyl-4-carbonitrile] is a histamine H3 receptor antagonist which binds potently and selectively to both human and rat histamine H3 receptors (Ki<=25 nM). Mice were stabilized on a high-fat diet (45 kcal % lard) prior to 28-day oral b.i.d. dosing for measurement of obesity-related parameters. A-331440 administered at 0.5 mg/kg had no significant effect on weight, whereas 5 mg/kg decreased weight comparably to dexfenfluramine (10 mg/kg). A-331440 administered at 15 mg/kg reduced weight to a level comparable to mice on the low-fat diet. The two higher doses reduced body fat and the highest dose also normalized an insulin tolerance test. These data show that the histamine H3 receptor antagonist, A-331440, has potential as an antiobesity agent.
 392338-13-5 (free base) A3104
Cetirizine dihydrochloride ≥98% (HPLC), solid Cetirizine hydrochloride is an orally active and selective H1-receptor antagonist. Antihistaminic; Piperazines. Nonsedating type histamine H1-receptor antagonist; major metabolite of hydroxyzine. Pharmacological activity resides primarily in the (R)-isomer.
 83881-52-1 C3618
Cimetidine H2 histamine receptor antagonist; I1 imidazoline receptor agonist; anti-ulcer agent. Blocks cancer metastasis by inhibiting the expression of E-selectin on the surface of endothelial cells, thus blocking tumor cell adhesion.
 51481-61-9 C4522
Ciproxifan hydrochloride ≥98% (HPLC), solid Ciproxifan belongs to a novel chemical series of histamine H3-receptor antagonists. In vitro, it behaved as a competitive antagonist at the H3 autoreceptor controlling 3H histamine release from synaptosomes and displayed similar Ki values (0.5-1.9 nM) at the H3 receptor controlling the electrically-induced contraction of guinea pig ileum or at the brain H3 receptor labeled with 125I-iodoproxyfan. Ciproxifan appears to be an orally bioavailable, extremely potent and selective H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders.
 C6492
Ciproxifan maleate ≥98% (HPLC), solid Potent, selective H3 histamine receptor antagonist.
 184025-19-2 C6848
Clemastine fumarate salt H1 histamine receptor antagonist.
 14976-57-9 C8903
Clemizole hydrochloride H1 histamine receptor antagonist.
 1163-36-6 C5040
Clobenpropit dihydrobromide solid Selective H3 histamine receptor antagonist that crosses the blood-brain barrier.
 145231-45-4 C209
Dimenhydrinate 523-87-5 D2396
Diphenhydramine hydrochloride ≥98% (TLC) H1 histamine receptor antagonist
 147-24-0 D3630
Diphenhydramine hydrochloride Sigma Reference Standard 147-24-0 D7774
Doxylamine succinate salt H1 histamine receptor antagonist; hypnotic.
 562-10-7 D3775
Ebastine ≥98% (HPLC), solid New Ebastine is a nonsedating histamine H1 receptor antagonist, which inhibits allergen-induced bronchospasm in conscious guinea pigs. Unlike other compounds in this category, ebastine does not prolong the QT interval at up to five times the recommended therapeutic dose.
 90729-43-4 E9531
Epinastine hydrochloride ≥98% (HPLC), solid Epinastine hydrochloride is a non-sedating H1 histamine receptor antagonist drug.
 108929-04-0 E5156
Famotidine H2 histamine receptor antagonist; anti-ulcer agent
 76824-35-6 F6889
Fexofenadine hydrochloride >98% (HPLC) Fexofenadine is a non-sedating H1 histamine receptor antagonist.
 153439-40-8 F9427
JNJ7777120 ≥98% (HPLC), solid JNJ7777120 is a potent, selective non-imidazole H4 histamine receptor antagonist.
 459168-41-3 J3770
Ketotifen fumarate salt H1 histamine receptor antagonist.
 34580-14-8 K2628
Levocabastine hydrochloride ≥99% (HPLC), solid Non-peptide histamine H1 receptor antagonist; neurotensin NTS2 receptor ligand.
 79547-78-7 L3042
Loratadine >98% (HPLC), powder Non-sedating histamine H1-receptor antagonist.
 79794-75-5 L9664
Methapyrilene hydrochloride H1 histamine receptor antagonist. Potent liver carcinogen in rats.
 135-23-9 M9125
Pheniramine maleate salt H1 histamine receptor antagonist.
 132-20-7 P6902
Phenyltoloxamine citrate salt 1176-08-5 P8404
Promethazine hydrochloride H1 histamine receptor antagonist; CNS depressant; anticholinergic.
 58-33-3 P4651
Pyrilamine maleate salt H1 histamine receptor antagonist.
 59-33-6 P5514
Ranitidine hydrochloride solid H2 histamine receptor antagonist; anti-ulcer agent.
 66357-59-3 R101
S-(+)-Chlorpheniramine maleate salt H1 histamine receptor antagonist; active isomer.
 2438-32-6 C4915
SKF-95282 dimaleate salt solid, >98% (HPLC) H2 Histamine receptor antagonist.
 104076-39-3 S5317
Thioperamide maleate solid Potent and selective H3 histamine receptor antagonist that crosses the blood-brain barrier.
 148440-81-7 T123
Triprolidine hydrochloride ≥99% H1 histamine receptor antagonist.
 6138-79-0 T6764

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