Serotonin receptor agonist

A serotonin receptor agonist is a compound that activates serotonin receptors, in a manner similar to serotonin.

Non-selective agonists: Psilocin and DMT are serotonin analogs found in certain plants or mushrooms. These compounds act on a variety of serotonin receptor types.

5-HT_1A agonists

Azapirones such as buspirone, gepirone, and tandospirone are 5-HT_1A agonists marketed primarily as anxiolytics, but also recently as antidepressants.

5-HT_1B agonists

Triptans such as sumatriptan, rizatriptan, and naratriptan, are 5-HT_1B receptor agonists that are used to abort migraine and cluster headache attacks.

5-HT_1D agonists

In addition to being 5-HT_1B agonists, triptans are also agonists at the 5-HT_1D receptor, which contributes to their antimigraine effect caused by vasoconstriction of blood vessels in the brain.

5-HT_1F agonists

LY-334,370 was a selective 5-HT_1F agonist that was being developed by Eli Lilly and Company for the treatment of migraine and cluster headaches. Development was halted however due to toxicity detected in animal test subjects. Lasmiditan has successfully completed Phase II clinical trials in early 2010.

5-HT_2A agonists

Psychedelic drugs like LSD, mescaline, and 2C-B, act as 5-HT_2A agonists. Their action at this receptor is responsible for their "psychedelic" effects. Some of these drugs, act as agonists for other 5HT receptor subtypes. Not all 5-HT_2A agonists are psychoactive.^[1]

5-HT_2C agonists

Lorcaserin is a thermogenic and anorectic weight-loss drug which acts as a selective 5-HT_2C agonist.

5-HT₄ agonists

Cisapride and Tegaserod are 5-HT₄ partial receptor agonist that were used to treat disorders of gastrointestinal motility. Prucalopride is a highly selective 5-HT₄ receptor agonist that can be used to treat certain disorders of gastrointestinal motility. Other 5-HT₄ agonists have shown potential to be nootropic type drugs via promoting acetylcholine release.

5-HT₇ agonists

AS-19 (drug) is a 5-HT₇ receptor agonist that has been used only in research.

References

^ Aghajanian, M.D., G.K. (1999). "Serotonin and Hallucinogens". Neuropharmacology. 21 (2S): 16S. doi:10.1016/s0893-133x(98)00135-3. {{cite journal}}: |access-date= requires |url= (help); Unknown parameter |coauthors= ignored (|author= suggested) (help)

External links

IUPHAR GPCR Database - 5-HT receptor family
MeSH list of agents 82017366
Serotonin+agonists at the U.S. National Library of Medicine Medical Subject Headings (MeSH)

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[1] Aghajanian, M.D., G.K. (1999). "Serotonin and Hallucinogens". Neuropharmacology. 21 (2S): 16S. doi:10.1016/s0893-133x(98)00135-3. {{cite journal}}: |access-date= requires |url= (help); Unknown parameter |coauthors= ignored (|author= suggested) (help)

[1]

v t e Anxiolytics (N05B)
5-HT_1ARTooltip 5-HT1A receptor agonists	Buspirone Gepirone Tandospirone
GABA_ARTooltip GABAA receptor PAMsTooltip positive allosteric modulators	Benzodiazepines: Adinazolam Alprazolam Bromazepam Camazepam Chlordiazepoxide Clobazam Clonazepam Clorazepate Clotiazepam Cloxazolam Diazepam^# Ethyl loflazepate Etizolam Fludiazepam Halazepam Ketazolam Lorazepam^# Medazepam Nordazepam Oxazepam Pinazepam Prazepam; Others: Alpidem^‡ Barbiturates (e.g., phenobarbital) Carbamates (e.g., meprobamate) Carisoprodol Chlormezanone^‡ Ethanol (alcohol) Etifoxine
Hypnotics	Zopiclone
Gabapentinoids (α₂δ VDCC blockers)	Gabapentin Gabapentin enacarbil Phenibut Pregabalin
Antidepressants	SSRIsTooltip Selective serotonin reuptake inhibitors (e.g., escitalopram) SNRIsTooltip Serotonin-norepinephrine reuptake inhibitors (e.g., duloxetine) SARIsTooltip Serotonin antagonist and reuptake inhibitors (e.g., trazodone) TCAsTooltip Tricyclic antidepressants (e.g., clomipramine^#) TeCAsTooltip Tetracyclic antidepressants (e.g., mirtazapine) MAOIsTooltip Monoamine oxidase inhibitors (e.g., phenelzine); Others: Agomelatine Bupropion Tianeptine Vilazodone Vortioxetine
Antipsychotics	Quetiapine Flupentixol
Sympatholytics (Antiadrenergics)	Alpha-1 blockers (e.g., prazosin) Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) Beta blockers (e.g., propranolol)
Others	Benzoctamine Cycloserine Fabomotizole Hydroxyzine Lorpiprazole Mebicar Mepiprazole Nicotine Opipramol Oxaflozane^‡ Phenaglycodol Phenibut Picamilon Selank Tiagabine Tofisopam Validolum
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

5-HT1A agonists

5-HT1B agonists

5-HT1D agonists

5-HT1F agonists

5-HT2A agonists

5-HT2C agonists

5-HT4 agonists

5-HT7 agonists

See also