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5-HT receptor

Serotonin The serotonin receptors, also known as 5-hydroxytryptamine receptors or 5-HT receptors, are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems.[1][2] They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand. The serotonin receptors modulate the release of many neurotransmitters, including glutamate, GABA, dopamine, epinephrine / norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin, cortisol, corticotropin, and substance P, among others. The serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, and thermoregulation. The serotonin receptors are the target of a variety of pharmaceutical and illicit drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.[3]

Classification
With the exception of the 5-HT3 receptor, a ligand-gated ion channel, all other serotonin receptors are G protein-coupled receptors that activate an intracellular second messenger cascade to produce an excitatory or inhibitory response.

Families
Family Type 5-HT1 Gi/Go-protein coupled. 5-HT2 Gq/G11-protein coupled. Ligand-gated Na+ and K+ cation channel. 5-HT4 Gs-protein coupled. 5-HT3 Mechanism Decreasing cellular levels of cAMP. Increasing cellular levels of IP3 and DAG. Depolarizing plasma membrane. Increasing cellular levels of cAMP. Potential Inhibitory Excitatory Excitatory Excitatory

5-HT5 Gi/Go-protein coupled.[4] 5-HT6 Gs-protein coupled. 5-HT7 Gs-protein coupled.

Decreasing cellular levels of cAMP. Increasing cellular levels of cAMP. Increasing cellular levels of cAMP.

Inhibitory Excitatory Excitatory

[edit] Subtypes
Within these general classes of serotonin receptors, a number of specific types have been characterized:[5][6][7] Overview of Serotonin Receptors Rece Distribu Gene(s) Function ptor tion Addiction
[8][9][10]

Agonists

Antagonists

Aggressio n[11] Anxiety[12] Appetite[13


]

Blood Pressure[14]
[15]

5-CT 8-OH-DPAT Aripiprazole Buspirone[31] (anxiolytic and antidepressant)


[31]

5HT1A

HTR 1A

B lo o d V es se ls C N S

Cardiovasc ular Function[16


]

Emesis[17] Heart Rate[14][15] Impulsivit y[18] Memory[19


][20]

Mood[21] Nausea[17] Nociceptio n[22] Penile Erection[23] Pupil Dilation[24] Respiratio n[25] Sexual Behavior[2

Cannabidiol Clozapine Dihydroergota mine Eltoprazine Ergotamine Flesinoxan Flibanserin Gepirone Ipsapirone Methysergide Nefazodone Psilocin Quetiapine RU 24969 Tandospirone Trazodone Urapidil Xaliproden Yohimbine Ziprasidone

Alprenolol Asenapine BMY 7378 Cyanopindolol Iodocyanopindol ol Lecozotan Methiothepin NAN-190 Nebivolol Oxprenolol Pindolol Propanolol Robalzotan S15535 Spiperone TFMPP UH-301 WAY-100,135 WAY-100,635 Mefway

6]

Sleep[27] Sociability
[28]

Thermoreg ulation[29] Vasoconstr iction[30] Addiction


[32]

5HT1B

HTR 1B

B lo o d V es se ls C N S

Aggressio n[11] Anxiety[33]


[34][35]

Learning[36
]

Locomotio n[37] Memory[36


]

Mood[35] Penile Erection[23] Sexual Behavior[2


6]

Vasoconstr iction

5-CT CP-93,129 CP-94,253 Dihydroergota mine Eltoprazine Ergotamine Methysergide RU 24969 TFMPP Triptans[31] (antimigraine[3 1] ) o Zolmitr iptan o Eletript an o Sumatr iptan 5-CT Dihydroergota mine Ergotamine Methysergide Triptans[31] (antimigraine[3 1] ) o Almotr iptan o Eletript an o Frovatr iptan o Naratri ptan

Alprenolol AR-A000002 Asenapine Cyanopindolol GR 127935 Iodocyanopindol ol Isamoltane Metergoline Methiothepin Oxprenolol Pindolol Propanolol SB-216,641 Yohimbine

5HT1D

HTR 1D

B lo o d V es se ls C N S

Anxiety[38]
[39]

Locomotio n[37] Vasoconstr iction

BRL-15572 GR 127935 Ketanserin Metergoline Methiothepin Rauwolscine Ritanserin

Rizatri ptan o Sumatr iptan o Zolmitr iptan Yohimbine

5HT1e puta tive rece ptor

HTR 1E

B lo o d V es se ls C N S C N S B lo o d V es se ls C N S G I T ra ct Pl at el et s P

Eletriptan Methysergide Tryptamine

Methiothepin

5HT1F

HTR 1F

Migraine

LY334370 COL-144

5HT2A

HTR 2A

Addiction (potentiall y modulatin g) [40] Anxiety[41] Appetite Cognition Imaginatio n Learning Memory Mood Perception Sexual Behavior[4
2]

Sleep[43] Thermoreg ulation[44] Vasoconstr

2C-B 5-MeO-DMT BZP Bufotenin DMT DOM Ergonovine Lisuride LSD Mescaline Myristicin Psilocin Psilocybin TFMPP (partial agonist or antagonist) Yohimbine

Atypical antipsychotics o Clozapin e[31] o Olanzapi ne o Quetiapi ne o Risperid one o Ziprasid one Aripiprazole Asenapine Amitriptyline Clomipramine Cyproheptadine Eplivanserin Etoperidone Iloperidone Ketanserin[31] (antihypertensiv

N S S m o ot h M u sc le B lo o d V es se ls C N S G I T ra ct Pl at el et s P N S S m o ot h M u sc le

iction[45]

e[31]) Methysergide Mianserin Mirtazapine Nefazodone Pimavanserin Pizotifen Ritanserin Trazodone

Anxiety[46]
[47][48]

Appetite[49
]

5HT2B

HTR 2B

Cardiovasc ular Function GI Motility[50] Sleep[43] Vasoconstr iction

BW-723C86 Fenfluramine MDMA Norfenflurami ne Ro60-0175

Agomelatine Asenapine BZP Ketanserin Methysergide Ritanserin Tegaserod Yohimbine

5HT2C

HTR 2C

B lo o d V es se ls C N S G I T ra ct Pl at el et s P N S S m o ot h M u sc le C N S G I T ra ct P N S

Addiction. (potentiall y modulatin g)[40] Anxiety[51]


[52][53]

Appetite GI Motility[54] Locomotio n Mood[52][53


]

Penile Erection[55]
[56]

Sexual Behavior[4
2]

A-372,159 AL-38022A Aripiprazole Ergonovine Lorcaserin Ro60-0175 TFMPP Trazodone[31] (hypnotic[31]) YM-348

Sleep[57] Thermoreg ulation[44] Vasoconstr iction

Agomelatine[31] (antidepressant[3 1] ) Amitriptyline Asenapine Clomipramine Clozapine[31] (antipsychotic[31] ) Cyproheptadine Dimebolin Eltoprazine Etoperidone Fluoxetine Iloperidone Ketanserin[31] (antihypertensiv e[31]) Lisuride Methysergide[58] Mianserin Mirtazapine Nefazodone Olanzapine Quetiapine Risperidone Ritanserin Trazodone Ziprasidone

5HT3

HTR 3A HTR 3B HTR 3C HTR 3D HTR 3E

Addiction Anxiety Emesis GI Motility Learning[59


]

Memory[59
]

2-Methyl-5HT BZP Quipazine RS-56812

Nausea

Alosetron Several antiemetics[31] o Dolasetr on o Ondanset ron[31] o Granisetr on o Tropisetr on Clozapine

Memantine Metoclopramide Mianserin Mirtazapine Olanzapine Quetiapine

Anxiety[60]
[61]

5HT4

HTR 4

C N S G I T ra ct P N S

Appetite[62
][63]

GI Motility Learning[64
][65]

Memory[64
][65][66]

Mood
]

[67][68

Respiratio n[25][69]

5-MT BIMU-8 Cinitapride Cisapride[31] (gastroprokine tic) Dazopride Metocloprami de Mosapride Prucalopride RS-67333 Renzapride Tegaserod Zacopride

L-Lysine[60] Piboserod

5HT5A

HTR 5A

C N S

Locomotio n[70] Sleep[71]

5-CT Ergotamine Valerenic Acid[71]

Asenapine Dimebolin Methiothepin Ritanserin SB-699,551 SB-699,551-A Amitriptyline Aripiprazole Asenapine Clomipramine Clozapine Dimebolin EGIS-12233 Iloperidone MS-245 Olanzapine Ro04-6790 SB-258,585 SB-271,046[77] SB-357,134 SB-399,885

Anxiety[72]
[73]

Cognition[
74]

5HT6

HTR 6

C N S

Learning[75
]

EMD-386,088 EMDT

Memory[75
]

Mood[73][76
]

5HT7

HTR 7

B lo o d V es se ls C N S G I T ra ct

Anxiety[78]
[79]

Memory[80
][81]

Mood[78][79
]

Respiratio n[25][82] Sleep[78][82]


[83]

5-CT 8-OH-DPAT AS-19

Thermoreg ulation Vasoconstr iction

Amitriptyline Aripiprazole Asenapine Clomipramine Clozapine EGIS-12233 Iloperidone Imipramine Ketanserin Mirtazapine Olanzapine Ritanserin Risperidone SB-269,970

Note that there is no 5-HT1C receptor since, after the receptor was cloned and further characterized, it was found to have more in common with the 5-HT2 family of receptors and was redesignated as the 5-HT2C receptor. Note that there is also no 5-HT5B receptor, as it exists only in mice and rats and not in humans or monkeys. Very nonselective agonists of 5-HT receptor subtypes include ergotamine (an antimigraine), which activates 5-HT1A, 5-HT1D, 5-HT1B, D2 and norepinephrine receptors.[31] LSD (a psychedelic) is a 5-HT1A, 5-HT2A, 5-HT2C, 5-HT5A, 5-HT5, 5-HT6 agonist.[3

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