5-HT1A

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The 5-HT_1A receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). It is a G protein-coupled receptor (GPCR) that is coupled to G_i/G_o and mediates inhibitory neurotransmission. HTR1A denotes the human gene encoding for the receptor.

Распределение в организме

| deadurl= no}}</ref> The 5-HT_1A receptors in the raphe nucleus are largely somatodendritic autoreceptors, whereas those in other areas such as the hippocampus are postsynaptic receptors.

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Физиологическая роль

Нейромодуляция

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5-HT_1A autoreceptor desensitization and increased 5-HT_1A receptor postsynaptic activation via general increases in serotonin levels by serotonin precursor supplementation, serotonin reuptake inhibition, or monoamine oxidase inhibition has been shown to be a major mediator in the therapeutic benefits of most mainstream antidepressant supplements and pharmaceuticals, including serotonin precursors like L-tryptophan and 5-HTP, selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), tetracyclic antidepressants (TeCAs), and monoamine oxidase inhibitors (MAOIs). 5-HT_1A receptor activation likely plays a significant role in the positive effects of serotonin releasing agents (SRAs) like MDMA («Ecstasy») as well.

5-HT_1A receptors in the dorsal raphe nucleus are co-localized with neurokinin 1 (NK₁) receptors and have been shown to inhibit the release of substance P, their endogenous ligand. In addition to being antidepressant and anxiolytic in effect, 5-HT_1A receptor activation has also been demonstrated to be antiemetic and analgesic, and all of these properties may be mediated in part or full, depending on the property in question, by NK₁ receptor inhibition. Consequently, novel NK₁ receptor antagonists are now in use for the treatment of nausea and emesis, and are also being investigated for the treatment of anxiety and depression.

5-HT_1A receptor activation has been shown to increase dopamine release in the medial prefrontal cortex, striatum, and hippocampus, and may be useful for improving the symptoms of schizophrenia and Parkinson's disease. As mentioned above, some of the atypical antipsychotics are 5-HT_1A receptor partial agonists, and this property has been shown to enhance their clinical efficacy. Enhancement of dopamine release in these areas may also play a major role in the antidepressant and anxiolytic effects seen upon postsynaptic activation of the 5-HT_1A receptor.

Activation of 5-HT_1A receptors has been demonstrated to impair certain aspects of memory (affecting declarative and non-declarative memory functions) and learning (due to interference with memory-encoding mechanisms), by inhibiting the release of glutamate and acetylcholine in various areas of the brain. 5-HT_1A activation are known to improve cognitive functions associated with the prefrontal cortex, possibly via inducing prefrontal cortex dopamine and acetylcholine release. Conversely, 5-HT_1A receptor antagonists such as lecozotan have been shown to facilitate certain types of learning and memory in rodents, and as a result, are being developed as novel treatments for Alzheimer's disease.

Other effects of 5-HT_1A activation that have been observed in scientific research include:

• Decreased aggression
• Increased sociability
• Decreased impulsivity
• Inhibition of drug-seeking behavior
• Facilitation of sex drive and arousal
• Inhibition of penile erection
• Diminished food intake
• Prolongation of REM sleep latency
• Reversal of opioid-induced respiratory depression.

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Лиганды

Агонисты

• 8-OH-DPAT
• Alnespirone
• Befiradol
• Eptapirone
• F-15,599
• Lesopitron
• MKC-242
• LY-293,284
• Osemozotan (partial at postsynaptic receptors)
• Repinotan
• U-92,016-A

Парциальные агонисты

• 5-Carboxamidotryptamine (5-CT)
• 5-Methoxytryptamine (5-MT)
• 5-MeO-DMT
• Adatanserin
• alpha-Ethyltryptamine (αET)
• alpha-Methyltryptamine (αMT)
• Aripiprazole
• Asenapine
• Bay R 1531
• Befiradol
• Binospirone
• Bufotenin
• Buspirone
• Cannabidiol
• Clozapine
• Dihydroergotamine
• Ebalzotan
• Eltoprazine
• Ergotamine
• Etoperidone
• F-11,461
• F-12,826
• F-13,714
• F-14,679
• Flesinoxan
• Flibanserin
• Ginkgo Biloba
• Gepirone
• Haloperidol
• Ipsapirone
• Lisuride
• Lurasidone
• LY-301,317
• LSD
• MDMA
• Naluzotan
• NBUMP
• Nefazodone
• Olanzapine
• Perospirone
• Piclozotan
• Psilocin
• Psilocybin
• Quetiapine
• Rauwolscine
• RU-24,969
• S-15,535
• Sarizotan
• SSR-181,507
• Sunepitron
• Tandospirone
• Tiospirone
• Trazodone
• Trifluoromethylphenylpiperazine
• Urapidil
• Vortioxetine
• Vilazodone
• Xaliproden
• Yohimbine
• Zalospirone
• Ziprasidone

Антагонисты

• Alprenolol
• AV-965
• BMY-7,378
• Cyanopindolol
• Dotarizine
• Flopropione
• GR-46,611
• Iodocyanopindolol
• Isamoltane]
• Lecozotan
• Methiothepin
• Methysergide
• MPPF
• NAN-190
• Oxprenolol
• Pindobind
• Pindolol
• Propranolol
• Risperidone
• Robalzotan
• SB-649,915
• SDZ-216,525
• Spiperone
• Spiramide
• Spiroxatrine
• UH-301
• WAY-100,135
• WAY-100,635
• Xylamidine
• Mefway

См. также

• Серотониновые рецепторы
• 5-HT₁-рецептор
• 5-HT₂-рецептор
• 5-HT₃-рецептор
• 5-HT₅-рецептор
• 5-HT₆-рецептор
• 5-HT₇-рецептор

Для дополнительного чтения

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• Panesar, Kiran 5-HT1A Receptors in Psychopharmacology  (неопр.). Web Article. Psychopharmacology Institute. Дата обращения: 11 апреля 2013.

Ссылки

• 5-HT_1A  (неопр.). IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.