Enerisant

Enerisant
Clinical data
Other namesTS-091
Routes of
administration		By mouth
Pharmacokinetic data
Protein binding31.0–31.7%[1]
Elimination half-life8 hours[1]
ExcretionKidney (64.5–89.9%)[1]
Identifiers
IUPAC name
  • [1-[4-[3-[(2R)-2-methylpyrrolidin-1-yl]propoxy]phenyl]pyrazol-4-yl]-morpholin-4-ylmethanone
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
Chemical and physical data
FormulaC22H30N4O3
Molar mass398.507 g·mol−1
3D model (JSmol)
SMILES
  • C[C@@H]1CCCN1CCCOC2=CC=C(C=C2)N3C=C(C=N3)C(=O)N4CCOCC4
InChI
  • InChI=1S/C22H30N4O3/c1-18-4-2-9-24(18)10-3-13-29-21-7-5-20(6-8-21)26-17-19(16-23-26)22(27)25-11-14-28-15-12-25/h5-8,16-18H,2-4,9-15H2,1H3/t18-/m1/s1
  • Key:IABXVJILZYNSTM-GOSISDBHSA-N

Enerisant is an experimental drug under investigation as a potential treatment for narcolepsy. It is a member of the histamine H3 receptor antagonist/inverse agonist class of medications.[1][2][3]

  1. ^ a b c d Terasaka S, Hachiuma K, Mano Y, Onishi K, Kitajima I, Nishino I, Endo H (July 2021). "Drug-drug interaction potential and clinical pharmacokinetics of enerisant, a novel potent and selective histamine H3 receptor antagonist". Xenobiotica. 51 (7): 786–795. doi:10.1080/00498254.2021.1918361. PMID 33910470.
  2. ^ Klaus S, Carolan A, O'Rourke D, Kennedy B (September 2022). "What respiratory physicians should know about narcolepsy and other hypersomnias". Breathe (Sheffield, England). 18 (3): 220157. doi:10.1183/20734735.0157-2022. PMC 9973529. PMID 36865656.
  3. ^ Inoue Y, Uchiyama M, Umeuchi H, Onishi K, Ogo H, Kitajima I, Matsushita I, Nishino I, Uchimura N (February 2022). "Optimal dose determination of enerisant (TS-091) for patients with narcolepsy: two randomized, double-blind, placebo-controlled trials". BMC Psychiatry. 22 (1): 141. doi:10.1186/s12888-022-03785-7. PMC 8862520. PMID 35193545.
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