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Antagonists

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C3025 (±)-Chlorpheniramine maleate salt ≥99% (perchloric acid titration) H1 Histamine receptor antagonist.
A3104 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)-(dimethylami<WBR>no)-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.
A7730 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.
SML0119 Acrivastine ≥98% (HPLC) Acrivastine is a second-generation antihistamine, an H1-receptor antagonist.
SML1590 Alcaftadine ≥98% (HPLC) Alcaftadine is a potent inverse agonist at H1, H2 and H4 histamine receptors. Alcaftadine is antiallergic agent that exhibit anti-inflammatory and mast cell stabilizing effects.
A7611 Azelastine hydrochloride ≥98% (HPLC) H1 histamine receptor antagonist; NF-kB activator.
SML1591 Buclizine dihydrochloride ≥98% (HPLC) Buclizine is a piperazine antihistamine and anticholinergic that exerts its antiemetic and antimotion sickness effects.
SML0329 Carcinine dihydrochloride ≥98% (HPLC) Carcinine (β-alanyl histamine) is a selective histamine H3 antagonist, 100-1000-fold selective for H3 over H2 and H1, that also functions as an antioxidant and as a chemical chaperone to reduce non-enzymatic glycation of proteins and maintain native folding of proteins.
C3618 Cetirizine dihydrochloride ≥98% (HPLC) Cetirizine hydrochloride is an orally active and selective H1-receptor antagonist. Antihistaminic; Piperazines. Non-sedating type histamine H1-receptor antagonist; major metabolite of hydroxyzine. Pharmacological activity resides primarily in the (R)-isomer.
C4522 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.
C6492 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.
C6848 Ciproxifan maleate ≥98% (HPLC), powder Potent, selective H3 histamine receptor antagonist.
SML0445 Clemastine fumarate salt ≥98% (HPLC) Clemastine fumarate is an antihistamine H1-antagonist and anticholinergic that also has antipruritic activity.
SML1447 Clemizole hydrochloride ≥98% (HPLC) Clemizole is a potent and preferring inhibitor of TRPC5 that efficiently blocks heterologously expressed homomeric TRPC5 channels as well as heteromeric TRPC1:TRPC5 channels. Clemizole is a potent and selective H1 histamine receptor antagonist. Clemizole inhibited binding of HCV RNA by NS4B inhibit HCV RNA replication in cell culture.
Clemizole is an antihistamine and an inhibitor of NS4B (nonstructural protein 4B) RNA of HCV (hepatitis C virus). Studies in Scn1α (sodium channel, voltage-gated, type I, α) Zebrafish mutant show that this drug has the potential as a therapeutic agent in Dravet Syndrome treatment.
C209 Clobenpropit dihydrobromide solid Selective H3 histamine receptor antagonist that crosses the blood-brain barrier.
SML0095 Conessine ≥97% (HPLC) Conessine is a plant steroid alkaloid that acts as a potent and specific antagonist of histamine H3 receptors (Ki = 5.37 and 24.5 nM for human and rat receptors, respectively). Conessine is 1860-fold selective for H3 over H4 and does not bind to H1 or H2 receptors. The molecule also binds to the human α2C4 adrenergic receptor (pKi = 7.98).
D2396 Dimenhydrinate  
D3630 Diphenhydramine hydrochloride ≥98% (HPLC) H1 histamine receptor antagonist
D7774 Diphenhydramine hydrochloride analytical standard  
D3775 Doxylamine succinate salt H1 histamine receptor antagonist; hypnotic.
Doxylamine suppresses histamine at the H1 receptor. It is associated with the short term management of insomnia and temporary relief of common cold symptoms. On the other hand, doxylamine intoxication is linked with rhabdomyolysis and secondary acute renal failure.
Studies in mice show that doxylamine induces liver microsomal cytochrome P450 and other enzymes involved in thyroxine (T4) metabolism. In combination with pyridoxine hydrochloride, this drug is used to treat morning sickness.
E9531 Ebastine ≥98% (HPLC), solid Ebastine is a non-sedating 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.
E5156 Epinastine hydrochloride ≥98% (HPLC), solid Epinastine hydrochloride is a non-sedating H1 histamine receptor antagonist.
F6889 Famotidine H2 histamine receptor antagonist; anti-ulcer agent
F9427 Fexofenadine hydrochloride >98% (HPLC) Fexofenadine is a non-sedating H1 histamine receptor antagonist.
SML0500 GSK334429 hydrochloride ≥98% (HPLC) GSK334429 is a selective histamine H3 receptor antagonist. H3 antagonists increase the release of brain histamine, ACh, NE and DA neurotransmitters that modulate cognitive processes. Studies look at their analgesic efffects including efficacy for neuropathic pain.
J3830 JNJ 10191584 maleate salt ≥98% (HPLC) JNJ 10191584 maleate is a highly selective histamine H4 receptor silent antagonist.
J3770 JNJ7777120 ≥98% (HPLC) JNJ7777120 is a potent, selective non-imidazole H4 histamine receptor antagonist.
K2628   Ketotifen fumarate salt H1 histamine receptor antagonist.
SML1611 Lafutidine ≥98% (HPLC) Lafutidine is a second generation H2 histamine receptor antagonist. Lafutidine has been used clinically to treat ulcers and gastro-esophageal reflux disease (GERD). Lafutidine has also been investigated as a treatment against peripheral neuropathy and for its protective stomach effects during cancer chemotherapies and long term ibuprofen use.
L3042 Levocabastine hydrochloride ≥99% (HPLC), solid Non-peptide histamine H1 receptor antagonist; neurotensin NTS2 receptor ligand.
L7795 Levocetirizine dihydrochloride ≥98% (HPLC) Levocetirizine hydrochloride is a nonsedating antihistamine. It is a histamine H1-receptor antagonist, the active isomer of cetirizine. Levocetirizine has high bioavailability, high affinity for and occupancy of the H1 receptor.
L9664 Loratadine ≥98% (HPLC), powder Loratadine is a non-sedating histamine H1-receptor antagonist. Shown to inhibit the two-pore domain potassium channel K2P18.1 (also called TRESK or KCNK18).
Non-sedating histamine H1-receptor antagonist.
SML1025   Lorcainide hydrochloride ≥98% (HPLC) Lorcainide is a Class 1c antiarrhythmic agent that blocks open fast acting voltage-gated sodium channels (subtype Nav1.5). Data shows that Lorcainide is a potent, selective antagonists/inverse agonists of human and rat H3 histamine receptors.
SML0950   Meclizine dihydrochloride ≥97% (HPLC) Meclizine is a potent histamine H1 receptor antagonist that is widely used as antiemetic. Recently, meclizine was identified as an inhibitor of hepstin. Also, meclizine is a potent inhibitor of mitochondrial respiration through inhibition of cytosolic CTP:phosphoethanolamine cytidylyltransferase (Pcyt2).
SML0107 Pemirolast potassium ≥98% (HPLC) Pemirolast potassium is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent. It Inhibits chemical mediator release from tissue mast cells and has recently also been shown to inhibit the release of peptides including substance P, neurokinin (NK) A, and calcitonin gene-related peptide (CGRP) from sensory nerves. It has been used for the treatment of allergic conjunctivitis prophylaxis of for pulmonary hypersensitivity reactions to drugs such as paclitaxel
P6902   Pheniramine maleate salt H1 histamine receptor antagonist.
P8404 Phenyltoloxamine citrate salt  
P4651 Promethazine hydrochloride H1 histamine receptor antagonist; CNS depressant; anticholinergic.
P5514 Pyrilamine maleate salt H1 histamine receptor antagonist.
R101 Ranitidine hydrochloride solid H2 histamine receptor antagonist; anti-ulcer agent.
C4915 S-(+)-Chlorpheniramine maleate salt H1 histamine receptor antagonist; active isomer.
Chlorpheniramine maleate is clinically used as a topical ointment to treat skin disorders such as sunburn, urticaria, angioedema, pruritus and insect bites.
T123 Thioperamide maleate salt solid Potent and selective H3 histamine receptor antagonist that crosses the blood-brain barrier.
Thioperamide is a potent and selective H3 histamine receptor antagonist that crosses the blood-brain barrier. It affects the central histaminergic system and decreases the duration of seizures and convulsions in mice. It also improves learning deficit induced by other drugs such as scopolamine.
T6764 Triprolidine hydrochloride ≥99% H1 histamine receptor antagonist.