Histaminergics - Antagonists

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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.
 
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.
 
C3025 (±)-Chlorpheniramine maleate salt ≥99% (perchloric acid titration) H1 Histamine receptor antagonist.
human ... HRH1(3269)
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.
human ... HRH1(3269)
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.
human ... ABCB1(5243), CYP1A2(1544), CYP3A4(1576), HRH2(3274), SLC9A2(6549), SLC9A5(6553)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Slc9a1(24782), Slc9a3(24784), Slc9a5(192215)
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.
 
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).
 
D7571 Dimaprit dihydrochloride ≥98% (NMR) The histamine H2 receptor influences various cardiovascular responses, including vasodilation and cardiac rhythm, regulates gastric acid secretion, and also plays a role in the immune system by inhibiting antibody production, T cell proliferation and cytokine production. Histamine receptors are members of the GPCR family, and H2 mediates cell signaling via internalization and interaction with the GTPase dynamin.
 
D3630 Diphenhydramine hydrochloride ≥98% (HPLC) H1 histamine receptor antagonist
human ... HRH1(3269)
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.
human ... HRH1(3269)
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
human ... HRH2(3274)
F9427 Fexofenadine hydrochloride >98% (HPLC) Fexofenadine is a non-sedating H1 histamine receptor antagonist.
human ... HRH1(3269)
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.
human ... HRH1(3269), PDE7B(27115)
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.
human ... CYP3A4(1576), HRH1(3269), KCNH1(3756), KCNH2(3757), PTAFR(5724)
rat ... Hrh1(24448)
P6902   Pheniramine maleate salt H1 histamine receptor antagonist.
human ... HRH1(3269)
P4651 Promethazine hydrochloride H1 histamine receptor antagonist; CNS depressant; anticholinergic.
human ... HRH1(3269)
P5514 Pyrilamine maleate salt H1 histamine receptor antagonist.
human ... HRH1(3269)
R101 Ranitidine hydrochloride solid H2 histamine receptor antagonist; anti-ulcer agent.
human ... HRH2(3274)
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.
human ... HRH3(11255)
T6764 Triprolidine hydrochloride ≥99% H1 histamine receptor antagonist.
human ... HRH1(3269)