Enerisant

Pharmaceutical compound From Wikipedia, the free encyclopedia

Enerisant (INNTooltip International Nonproprietary Name; developmental code name TS-091) 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]

Other namesTS-091
Routes of
administrationBy mouth
Protein binding31.0–31.7%[1]
Elimination half-life8 hours[1]
Quick facts Clinical data, Other names ...
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
  • [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)
  • C[C@@H]1CCCN1CCCOC2=CC=C(C=C2)N3C=C(C=N3)C(=O)N4CCOCC4
  • 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
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Pharmacology

Pharmacodynamics

Enerisant functions as a potent and highly selective antagonist/inverse agonist of the histamine H3 receptor. This mechanism of action is similar to that of pitolisant, a currently approved H3 receptor antagonist/inverse agonist for narcolepsy; however, enerisant has demonstrated greater affinity and selectivity for the H3 receptor in preclinical studies.[1][2][3][4][5] By blocking H3 receptors, enerisant increases histamine release from histaminergic neurons, leading to stimulation of postsynaptic histamine H1 receptors, a key mechanism in promoting wakefulness[1][3][4]

Pharmacokinetics

Enerisant exhibits minimal metabolism in humans and is primarily eliminated unchanged via renal excretion. After oral administration, it rapidly absorbs and exhibits dose-dependent plasma concentrations. Within 48 hours, 64.5-89.9% of the administered dose is recovered unchanged in urine. Plasma protein binding is approximately 31.0–31.7% in humans.[1][5]

See also

References

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