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Histamine Receptor Histamine Receptor

Cat.No.  Name Information
M41848 H4R antagonist 3 H4R antagonist 3 is a histamine-4 receptor antagonist with an EC50 of <10 mM.
M41847 H4R antagonist 2 H4R antagonist 2, a Furo[3,2-d]pyrimidine derivative, is a potent H4R antagonist.
M41846 Dothiepin Dothiepin (Dosulepin; Dothep) is an antidepressant agent with sedative/anxiolytic activity.
M41845 4-Methylhistamine hydrochloride 4-Methylhistamine (hydrochloride) is a potent, high affinity H4 receptor agonist Ki of 7 nM.
M41844 CP19 CP19, a histamine receptor antagonist, is an entry inhibitor against both Ebolavirus (EBOV) and Marburgvirus (MARV) with IC50s of 3.4 μM and 29.5 μM, respectively.
M41843 S 38093 hydrochloride S 38093 hydrochloride is a brain-penetrant, orally active antagonist of H3 receptor, with Kis of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.
M40966 Toreforant Toreforant is an orally active histamine H4 receptor antagonist that may be used in studies related to psoriasis.
M38960 Panaxydiol Panaxydiol exhibits histamine-release inhibition activity.
M30935 PF-03654746  PF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration. PF-03654746 reduces allergen-induced nasal symptoms, might be a novel therapeutic strategy to further explore allergic rhinitis. PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD).
M30758 (R)-(-)-α-Methylhistamine dihydrobromide (R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrobromide can enhance memory retention, attenuates memory impairment in rats.
M30621 Levocabastine Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).
M30611 Roxatidine acetate Roxatidine acetate is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity.
M30579 (R)-(-)-α-Methylhistamine dihydrochloride (R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats.
M30568 Dimethothiazine Dimethothiazine (Dimetotiazine; Fonazine) is an orally active tricyclic anti-histamine, anti-5-HT agent with a high activity against decerebrate rigidity, a little sedative activity and little soporific action. Dimethothiazine can reduce or abolish the effects of both static and dynamic fusimotor activity on the muscle spindle in decerebrate cat. Dimethothiazine can be used to research hemicrania and spasticity.
M30560 JNJ10191584 JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively.
M30546 Repirinast Repirinast (MY-5116) is an orally active anti-allergic agent. Repirinast inhibits histamine release. Repirinast can be used in the research of bronchial asthma.
M30354 Oxatomide Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin.
M30278 JNJ-10181457  JNJ-10181457 is a selective non-imidazole histamine H3 receptor antagonist that normalizes acetylcholine neurotransmission.
M30241 Mebhydrolin Mebhydrolin is a specific histamine H1 receptor antagonist.
M30200 Fenspiride Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.




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