| Cat.No. | Name | Information |
|---|---|---|
| M29397 | Cipralisant maleate | Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full 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 (maleate) has the potential for attention-deficit hyperactivity disorder research. |
| M29275 | Cipralisant | Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full 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 the potential for attention-deficit hyperactivity disorder research. |
| M28635 | Rupatadine | Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria. |
| M28586 | LML134 | LML134 (compound 18b) 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. |
| M28480 | Clobenpropit dihydrobromide | Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis. |
| M28477 | Iodophenpropit dihydrobromide | Iodophenpropit dihydrobromide is a potent and selective histamine H3 receptor antagonist. The binding of [125I]Iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM). |
| M28323 | Samelisant free base | Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders. |
| M28322 | Samelisant | Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders. |
| M27871 | Seliforant | Seliforant (SENS-111) is a selective and orally histamine H4 receptor antagonist. |
| M27690 | Zolantidine dimaleate | Zolantidine dimaleate (SKF 95282 dimaleate) is a potent, selective and cross the blood-brain barrier histamine H2 antagonist. Zolantidine dimaleate induces antinociception. |
| M27689 | PF-03654746 Tosylate | PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. PF-03654746 Tosylate reduces allergen-induced nasal symptoms. PF-03654746 Tosylate has potential for treatment of human cognitive disorders, improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD). |
| M27614 | Irdabisant | Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment. |
| M27613 | Irdabisant hydrochloride | Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. |
| M20991 | Levocetirizine | Levocetirizine (LCZ, (R)-Cetirizine), the R-enantiomer of cetirizine, is an antagonist of histamine H(1) receptor. |
| M20988 | Promethazine | Promethazine is a potent histamine H1 receptor antagonist. Promethazine is a medication used in the management and treatment of allergic conditions, nausea and vomiting, motion sickness, and sedation. Promethazine exhibits antiparasitic properties. |
| M20927 | Betahistine mesylate | Betahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator. |
| M20813 | Cyclizine | Cyclizine is a piperazine first-generation antagonist of histamine 1 receptor. |
| M20574 | Thonzylamine | Thonzylamine is an antihistamine and anticholinergic drug. |
| M20520 | Chloropyramine hydrochloride | Chloropyramine hydrochloride is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects. |
| M20516 | Ranitidine | Ranitidine is a histamine H2-receptor antagonist that inhibits stomach acid production. |
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