Irdabisant
Pharmaceutical compound
From Wikipedia, the free encyclopedia
Irdabisant (INN, USAN; developmental code name CEP-26401) is a histamine H3 receptor antagonist and inverse agonist which was under development for the treatment of cognition disorders but was never marketed.[1][3][4][5][6][7] It was specifically under development for the treatment of cognitive problems in people with schizophrenia and Alzheimer's disease.[3] The drug is taken orally.[1][2]
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| Other names | CEP-26401; CEP26401 |
| Routes of administration | Oral[1] |
| Drug class | Histamine H3 receptor antagonist; Wakefulness-promoting agent; Nootropic |
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| Onset of action | 3–6 hours (Tmax)[2] |
| Elimination half-life | 24–60 hours[2] |
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| Formula | C18H23N3O2 |
| Molar mass | 313.401 g·mol−1 |
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It shows high affinity for the histamine H3 receptor (Ki = 2.0 nM) and shows strong selectivity for this receptor over the other histamine receptors and several hundred other targets.[5][6][2] The drug produces wakefulness-promoting effects in both rodents and humans.[6][7] Irdabisant is said to cause "the same energizing and happy feeling as modafinil, but with a more relaxed undertone".[7] In addition however, it dose-dependently disrupts sleep in humans, with side effects including insomnia and headache.[2] The drug can also cause cognitive impairment, perhaps via sleep deprivation, at higher doses.[2] The time to peak levels is 3 to 6 hours and its elimination half-life is 24 to 60 hours.[2]
The chemical synthesis of irdabisant has been described.[5] Analogues of irdabisant have been described.[8][9][10][11]
Irdabisant was under development by Cephalon (since acquired by Teva Pharmaceutical).[1][3] It reached phase 1 clinical trials prior to the discontinuation of its development.[1][3]