Enerisant

A detailed overview of the drug Enerisant

{{Drugbox | Verifiedfields = changed | verifiedrevid = 123456789 | IUPAC_name = (2S)-2-[[4-(2-[[2-(2,3-dihydro-1H-inden-2-yl)ethyl]amino]ethyl)phenoxy]methyl]morpholine | image = Enerisant_structure.png | width = 250 | tradename = Enerisant | legal_status = Investigational | routes_of_administration = Oral | bioavailability = High | protein_bound = 95% | metabolism = Hepatic | elimination_half-life = 12 hours | excretion = Renal }}

Enerisant is a novel pharmaceutical compound currently under investigation for its potential use in the treatment of various neurological disorders. It is classified as a selective histamine H3 receptor antagonist, which means it works by blocking the action of histamine at the H3 receptor sites in the brain. This mechanism of action is thought to enhance the release of neurotransmitters such as acetylcholine, norepinephrine, and dopamine, which can improve cognitive function and alertness.

Pharmacology

Enerisant is a selective antagonist of the H3 receptor, which is predominantly expressed in the central nervous system. By inhibiting the action of histamine at these receptors, Enerisant increases the release of several neurotransmitters that are involved in wakefulness and cognitive processes.

Mechanism of Action

The H3 receptor is an autoreceptor that modulates the release of histamine and other neurotransmitters. Enerisant binds to these receptors, preventing histamine from exerting its inhibitory effects. This results in increased neurotransmitter release, which can enhance cognitive function and promote wakefulness.

Pharmacokinetics

Enerisant is administered orally and has a high bioavailability. It is extensively metabolized in the liver, primarily by the cytochrome P450 enzyme system. The drug has a half-life of approximately 12 hours, allowing for once-daily dosing. It is primarily excreted through the kidneys.

Clinical Trials

Enerisant is currently in Phase II clinical trials for the treatment of narcolepsy and ADHD. Preliminary results have shown promise in improving wakefulness and cognitive performance in patients with these conditions.

Adverse Effects

Common side effects of Enerisant include headache, nausea, and insomnia. These effects are generally mild and transient. As with any investigational drug, long-term safety data are still being collected.

Potential Applications

Enerisant is being explored for its potential use in a variety of neurological and psychiatric disorders, including:

• Narcolepsy: Due to its wake-promoting effects.
• ADHD: For its potential to enhance attention and cognitive function.
• Cognitive Impairment: In conditions such as Alzheimer's disease.

Also see

• Histamine H3 receptor
• Narcolepsy
• Attention Deficit Hyperactivity Disorder
• Cognitive enhancers

Receptor Antagonists
Receptor Type	Example Antagonists
Adrenergic receptor	Propranolol, Prazosin
Cholinergic receptor	Atropine, Scopolamine
Dopamine receptor	Haloperidol, Clozapine
Histamine receptor	Ranitidine, Diphenhydramine
Serotonin receptor	Ondansetron, Risperidone
Glutamate receptor	Memantine, Ketamine
GABA receptor	Flumazenil, Bicuculline
Opioid receptor	Naloxone, Naltrexone
Angiotensin receptor	Losartan, Valsartan