Samelisant Explained
| Class: | Histamine H3 receptor inverse agonist
- Wakefulness-promoting agent
|
| Elimination Half-Life: | 23-34 hours |
| Cas Number: | 1394808-82-2 |
| Pubchem: | 60151477 |
| Iuphar Ligand: | 10232 |
| Drugbank: | DB14835 |
| Chemspiderid: | 64854818 |
| Unii: | 65V47O9NOP |
| Chembl: | 4297328 |
| Synonyms: | SUVN-G3031 |
| Iupac Name: | N-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-morpholin-4-ylacetamide |
| C: | 21 |
| H: | 31 |
| N: | 3 |
| O: | 3 |
| Smiles: | C1CC(C1)N2CCC(CC2)OC3=CC=C(C=C3)NC(=O)CN4CCOCC4 |
| Stdinchi: | 1S/C21H31N3O3/c25-21(16-23-12-14-26-15-13-23)22-17-4-6-19(7-5-17)27-20-8-10-24(11-9-20)18-2-1-3-18/h4-7,18,20H,1-3,8-16H2,(H,22,25) |
| Stdinchikey: | LNXDUSQEXVQFGP-UHFFFAOYSA-N |
Samelisant (; developmental code name SUVN-G3031) is an experimental wakefulness-promoting agent acting as a selective histamine H3 receptor inverse agonist which is under development for the treatment of narcolepsy.[1] [2] [3] [4] It was also under development for the treatment of cognition disorders and Parkinson's disease, but no recent development has been reported for these indications. As of June 2024, samelisant is in phase 2 clinical trials for the treatment of narcolepsy.[5]
See also
Notes and References
- Web site: Samelisant - Suven Life Sciences . AdisInsight . 12 June 2024 . 22 September 2024.
- Alhusaini M, Eissa N, Saad AK, Beiram R, Sadek B . Revisiting Preclinical Observations of Several Histamine H3 Receptor Antagonists/Inverse Agonists in Cognitive Impairment, Anxiety, Depression, and Sleep-Wake Cycle Disorder . Frontiers in Pharmacology . 13 . 861094 . 2022 . 35721194 . 9198498 . 10.3389/fphar.2022.861094 . free .
- Konofal E . From past to future: 50 years of pharmacological interventions to treat narcolepsy . Pharmacology, Biochemistry, and Behavior . 241 . 173804 . August 2024 . 38852786 . 10.1016/j.pbb.2024.173804 . free .
- Nirogi R, Jayarajan P, Benade V, Abraham R, Goyal VK . Hits and misses with animal models of narcolepsy and the implications for drug discovery . Expert Opinion on Drug Discovery . 19 . 6 . 755–768 . June 2024 . 38747534 . 10.1080/17460441.2024.2354293 .
- Nirogi R, Mudigonda K, Bhyrapuneni G, Muddana NR, Shinde A, Goyal VK, Pandey SK, Mohammed AR, Ravula J, Jetta S, Palacharla VR . Safety, Tolerability, and Pharmacokinetics of SUVN-G3031, a Novel Histamine-3 Receptor Inverse Agonist for the Treatment of Narcolepsy, in Healthy Human Subjects Following Single and Multiple Oral Doses . Clinical Drug Investigation . 40 . 7 . 603–615 . July 2020 . 32399853 . 10.1007/s40261-020-00920-8 .
