Chemistry:Enerisant
Enerisant (INN; 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]
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
- ↑ 1.0 1.1 1.2 1.3 Cite error: Invalid
<ref>tag; no text was provided for refs namedpmid33910470 - ↑ 2.0 2.1 "What respiratory physicians should know about narcolepsy and other hypersomnias". Breathe (Sheffield, England) 18 (3): 220157. September 2022. doi:10.1183/20734735.0157-2022. PMID 36865656.
- ↑ 3.0 3.1 3.2 "Optimal dose determination of enerisant (TS-091) for patients with narcolepsy: two randomized, double-blind, placebo-controlled trials". BMC Psychiatry 22 (1). February 2022. doi:10.1186/s12888-022-03785-7. PMID 35193545.
- ↑ 4.0 4.1 "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. 2022. doi:10.3389/fphar.2022.861094. PMID 35721194.
- ↑ 5.0 5.1 "Update on Randomized Controlled Trials in CNS Hypersomnias". Current Sleep Medicine Reports 9 (2): 101–109. 17 February 2023. doi:10.1007/s40675-023-00249-6. ISSN 2198-6401.
 |  |
