Reseptor serotonin

.

The 5-HT_1B adalah salah satu contoh reseptor serotonin metabotropik. Ini adalah struktur kristalografi dalam representasi pita

Reseptor serotonin atau juga dikenal sebagai reseptor 5-hidroksitriptamin atau reseptor 5-HT adalah kelompok dari reseptor terhubung-protein G dan reseptor kanal ion (ligand-gated ion channels, LGIC) yang ditemukan pada sistem saraf pusat dan sistem saraf tepi. Reseptor serotonin memperantarai neurotransmisi eksitatori (pemicuan) dan inhibitori (penghambatan) yang beraksi terhadap ligan alaminya.

Klasifikasi

Dengan pengecualian dari reseptor 5-HT3, semua reseptor serotonin termasuk dalam reseptor terhubung-protein G yang mengaktifkan kaskade kurir kedua untuk menghasilkan respons eksitatori atau inhibitori (penghambatan). Pada tahun 2014 sebuah reseptor 5-HT novel dideskripsikan yang diisolasi dari kupu-kupu putih kecil, Pieris rapae, dan diberi nama pr5-HT8. Kesamaan relatif antara reseptor ini dengan kelas reseptor 5-HT lainnya bersifat rendah dan tidak terdapat pada mamalia.

Famili

Famili	Tipe	Mekanisme	Respon
5-HT1	Gi/Go-protein coupled.	Menurunkan level cAMP seluler.	Inhibitori
5-HT2	Gq/G11-protein coupled.	Meningkatkan level IP3 dan DAG.	Eksitatori
5-HT3	Ligand-gated Na^+ and K^+ cation channel.	depolariisasi membran plasma.	Eksitatori
5-HT4	Gs-protein coupled.	Meningkatkan level cAMP seluler.	Eksitatori
5-HT5	Gi/Go-protein coupled.	Menurunkan level cAMP seluler.	Inhibitori
5-HT6	Gs-protein coupled.	Meningkatkan level cAMP seluler.	Eksitatori
5-HT7	Gs-protein coupled.	Meningkatkan level cAMP seluler.	Eksitatori

Subtipe

Tujuh kelas reseptor serotonin mencakup total 14 reseptor serotonin dikenal. Jenis tertentu telah ditandai sebagai berikut:

Gambaran Reseptor Serotonin
Reseptor	Kloning pertama kali	Gen	Distribusi	Fungsi	Agonis	Antagonis reseptor	Obat-obat yang beraksi pada reseptor
			Pembuluh darah					SSP	Saluran GI	Platelet	PNS	Otot polos
5-HT1A	1987	HTR1A			Tidak	Tidak	Tidak	Tidak	Addiksi Aggresi Ansietas Nafsu makan Autoreseptor Tekanan darah Fungsi kardiovaskular Emesis Denyut jantung Impulsivitas Memori Mood Muntah Nosisepsi Ereksi penis Dilatasi pupil Respirasi Perilaku seksual Tidur Sosial Thermoregulasi Vasokonstriksi	Selektif (untuk 5-HT1A lebih dari reseptor 5-HT lainnya) Vilazodone (Viibryd) F-15,599 (senyawa untuk riset, sangat poten dan selektif untuk 5-HT1A) Flesinoxan (poten, EC50 = 24 nM) Gepirone (agonis parsial, Ki = 70 nM) Haloperidol Ipsapirone (agonis parsial, Ki = 12.1 nM) Quetiapine Trazodone (SARI Kd = 78nM) Yohimbine (agonis parsial tidak selektif) Tandospirone (agonis parsial dan selektif) Nonselektif 5-CT (poten – Ki = 250±50 pM) 8-OH-DPAT (poten) Aripiprazole (antipsikotik atipikal) Asenapine (antipsikotik atipikal) Buspirone (agonis parsial) Vortioxetine (agonis parsial efikasi tinggi) Ziprasidone (agonis parsial, Ki = 3.4 nM)	BMY 7378 Cyanopindolol Iodocyanopindolol Lecozotan Methiothepin Methysergide NAN-190 Nebivolol Nefazodone WAY-100,135 WAY-100,635 Mefway	Analgesik (agonis) Antidepresan (agonis reseptor post-sinaptik dan antagonis autoreseptor pre-sinaptik sebagai antidepresan) Ansiolitik (antagonist)
5-HT1B	1992	HTR1B			Tidak	Tidak	Tidak	Tidak	Addiksi Aggressi Ansietas Autoreseptor Belajar Lokomosi Memori Mood Ereksi penis Perilaku seksual Vasokonstriksi	5-CT CGS-12066A CP-93,129 CP-94,253 Dihydroergotamine Eltoprazine Ergotamine Methysergide RU 24969 TFMPP Triptans (antimigraine) Zolmitriptan Eletriptan Sumatriptan Vortioxetine (partial agonist, Ki = 33 nM)	Alprenolol AR-A000002 Asenapine Cyanopindolol GR-127,935 Iodocyanopindolol Isamoltane Metergoline Methiothepin Oxprenolol Pindolol Propranolol SB-216,641 Yohimbine	Migrain (e.g. triptans)
5-HT1D	1991	HTR1D			Tidak	Tidak	Tidak	Tidak	Ansietas Autoreseptor Lokomosi Vasokonstriksi	5-CT CP-135,807 Dihydroergotamine Ergotamine Methysergide Triptans (antimigrain) Almotriptan Eletriptan Frovatriptan Naratriptan Rizatriptan Sumatriptan Zolmitriptan Yohimbine	BRL-15572 GR-127,935 Ketanserin Metergoline Methiothepin Rauwolscine Ritanserin Vortioxetine (Ki = 54 nM) Ziprasidone	Migrain (e.g. triptans)
5-HT1E	1992	HTR1E			Tidak	Tidak	Tidak	Tidak	BRL-54443	Tidak diketahui
5-HT1F	1993	HTR1F	Tidak		Tidak	Tidak	Tidak	Tidak	Migrain	BRL-54443 Lasmiditan LY-334,370 Naratriptan	Tidak diketahui
5-HT2A	1988	HTR2A							Addiksi (modulasi secara potensial) Ansietas Nafsu makan Kognisi Imajinasi Belajar Memori Mood Persepsi Perilaku seksual Tidur Thermoregulasi Vasokonstriksi	25I-NBOMe (agonis penuh) 2C-B 5-MeO-DMT BZP Bufotenin DMT DOM Ergonovine Lisuride LSD Mescaline Myristicin PNU-22394 (agonis parsial) Psilocin Psilocybin TFMPP (agonis parsial atau antagonis)	antipsikotik atipikal Clozapine Olanzapine Quetiapine Risperidone Ziprasidone Aripiprazole Asenapine Amitriptyline Clomipramine Cyproheptadine Eplivanserin Etoperidone Haloperidol Hydroxyzine Iloperidone Ketanserin (antihypertensive) Methysergide Mianserin Mirtazapine Nefazodone Pimavanserin Pizotifen Ritanserin Trazodone Yohimbine	Antipsikotik atipikal (antagonis) Psychedelics (agonis parsial) NaSSAs (antidepresan dan ansiolitik; mereka beraksi sebagai antagois pada situs ini) Pengobatan sindrom serotonin (antagonis; misal siproheptadin) Membantu tidur (antagonis; misal trazodone)
5-HT2B	1992	HTR2B							Ansietas Nafsu makan Fungsi kardiovaskular Motilitas GI Tidur Vasokonstriksi	BW-723C86 Fenfluramine MDMA Norfenfluramine PNU-22394 (agonis parsial) Ro60-0175	Agomelatine Asenapine BZP Ketanserin Methysergide Ritanserin RS-127,445 Tegaserod Yohimbine	Migrain (antagonis)
5-HT2C	1988	HTR2C							Addiksi. (modulasi secara potensial) Ansietas Nafsu makan Motilitas GI Heteroreceptor for norepinephrine and dopamine Lokomosi Mood Ereksi penis Perilaku seksual Tidur Thermoregulasi Vasokonstriksi	A-372,159 AL-38022A Aripiprazole Ergonovine Lorcaserin PNU-22394 (agonis penuh) Ro60-0175 TFMPP Trazodone (hypnotic) YM-348	Agomelatine (antidepressant) Amitriptyline Asenapine Klomipramin Klozapin (antipsychotic) Siproheptadine Dimebolin Eltoprazine Etoperidone Fluoksetin Haloperidol Iloperidone Ketanserin (antihypertensive) Lisuride Methysergide Mianserin Mirtazapin Nefazodon Olanzapin Paroksetin Quetiapine Risperidon Ritanserin Tramadol Trazodone Ziprasidone	Antidepresan (misal agomelatin, fluoksetin, mirtazapin) Oreksigenik (misal mirtazapin, klozapin and olanzapin; antagonis) Anorektik (Lorcaserin) Antipsikotik (Vabicaserin; agonis)
5-HT3	1993	HTR3A HTR3B HTR3C HTR3D HTR3E	Tidak			Tidak		Tidak	Addiksi Asietas Emesis Motilitas GI Belajar Memori Muntah	2-Methyl-5-HT BZP Quipazine RS-56812	Alosetron Beberapa antimuntah Dolasetron Ondansetron Granisetron Tropisetron Klozapin Memantin Metoklopramid Mianserin Mirtazapin Olanzapin Quetiapine Vortioxetine (Ki = 3.7 nM)	Antimuntah
5-HT4	1995	HTR4	Tidak			Tidak		Tidak	Ansietas Nafsu makan Motilitas GI Belajar Memori Mood Respirasi	5-MT BIMU-8 Cinitapride Cisaprid (gastroprokinetik) Dazopride Metoklopramid Mosaprid Prucalopride RS-67333 Renzapride Tegaserod Zacopride	L-Lysine Piboserod	Gastroprokinetik (misal Tegaserod)
5-HT5A	1994	HTR5A	Tidak		Tidak	Tidak	Tidak	Tidak	Autoreseptor Lokomosi Tidur	5-CT Ergotamine Valerenic Acid (partial agonist)	Asenapine Dimebolin Methiothepin Ritanserin SB-699,551 SB-699,551-A	Tidak ada selama ini
5-HT5B	1993	HTR5BP	Tidak	Tidak	Tidak	Tidak	Tidak	Tidak	Functions in rodents, pseudogene in humans	tidak ada selama ini
5-HT6	1993	HTR6	Tidak		Tidak	Tidak	Tidak	Tidak	Ansietas Kognisi Belajar Memori Mood	EMD-386,088 EMDT	Amitriptilin Aripiprazol Asenapin Klomipramine Klozapin Dimebolin EGIS-12233 Haloperidol Iloperidone MS-245 Olanzapin Ro04-6790 SB-258,585 SB-271,046 SB-357,134 SB-399,885	Antidepressant (antagonis dan agonis) Anxiolytic (antagonis dan agonis) Nootropic (antagonis) Anorectic (antagonis)
5-HT7	1993	HTR7				Tidak	Tidak	Tidak	Ansietas Autoreseptor Memori Mood Respirasi Sleep Thermoregulasi Vasokonstriksi	5-CT 8-OH-DPAT Aripiprazol (agonis parsial lemah) AS-19 E-55888 RA-7	Amitriptilin Asenapin Klomipramin Klozapin EGIS-12233 Haloperidol Iloperidon Imipramin Ketanserin Mirtazapin Olanzapin Ritanserin Risperidon SB-269,970 Vortioksetin (Ki = 19 nM)	Antidepresan (antagonis) Ansiolitik (antagonis) Nootropik (antagonis)

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