213027-19-1
213027-19-1 structure
- Name: Cipralisant
- Chemical Name: 5-[2-(5,5-dimethylhex-1-ynyl)cyclopropyl]-1H-imidazole
- CAS Number: 213027-19-1
- Molecular Formula: C14H20N2
- Molecular Weight: 216.32200
- Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
- Create Date: 2016-03-27 16:42:11
- Modify Date: 2025-08-25 11:41:09
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Cipralisant is a potent and selective histamine H3 receptor 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 entered in clinical trials for the treatment of attention-deficit hyperactivity disorder.
| Name | 5-[2-(5,5-dimethylhex-1-ynyl)cyclopropyl]-1H-imidazole |
|---|---|
| Synonyms | cipralisant |
| Description | Cipralisant is a potent and selective histamine H3 receptor 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 entered in clinical trials for the treatment of attention-deficit hyperactivity disorder. |
|---|---|
| Related Catalog | |
| Target |
pKi: 9.9 (Histamine H3 receptor)[1] Ki: 0.47 nM (Rat histamine H3 receptor)[2] |
| In Vitro | Cipralisant (GT-2331) is a potent histamine H3 receptor antagonist with a pKi of 9.9[1] and a Ki of 0.47 nM for rat histamine H3 receptor[2]. Cipralisant acts as a full agonist at the recombinant rat histamine H3 receptor in vitro, and potently inhibits forskolin-induced cAMP accumulation with an EC50 of 0.23 nM. Cipralisant increases the basal [35S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC50, 5.6 nM)[2]. |
| In Vivo | Cipralisant (GT-2331) acts as an antagonist of histamine H3 receptor, and blocks R-α-methylhistamine (a histamine H3 receptor agonist)-induced water intake at 10 mg/kg via oral administration in rats[2]. |
| References |
| Density | 1.03g/cm3 |
|---|---|
| Boiling Point | 386.7ºC at 760 mmHg |
| Molecular Formula | C14H20N2 |
| Molecular Weight | 216.32200 |
| Flash Point | 188.5ºC |
| Exact Mass | 216.16300 |
| PSA | 28.68000 |
| LogP | 3.34290 |
| Vapour Pressure | 7.72E-06mmHg at 25°C |
| Index of Refraction | 1.536 |
