Reseptor Serotonin

Famili	Tipe	Mekanisme	Respon
5-HT₁	G_i/G_o-protein coupled.	Menurunkan level cAMP seluler.	Inhibitori
5-HT₂	G_q/G₁₁-protein coupled.	Meningkatkan level IP₃ dan DAG.	Eksitatori
5-HT₃	Ligand-gated Na⁺ and K⁺ cation channel.	depolariisasi membran plasma.	Eksitatori
5-HT₄	G_s-protein coupled.	Meningkatkan level cAMP seluler.	Eksitatori
5-HT₅	G_i/G_o-protein coupled.^[4]	Menurunkan level cAMP seluler.	Inhibitori
5-HT₆	G_s-protein coupled.	Meningkatkan level cAMP seluler.	Eksitatori
5-HT₇	G_s-protein coupled.	Meningkatkan level cAMP seluler.	Eksitatori

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-HT_1A	1987	HTR1A			Tidak	Tidak	Tidak	Tidak	Addiksi^[9]^[10]^[11] Aggresi^[12] Ansietas^[13] Nafsu makan^[14] Autoreseptor Tekanan darah^[15]^[16] Fungsi kardiovaskular^[17] Emesis^[18] Denyut jantung^[15]^[16] Impulsivitas^[19] Memori^[20]^[21] Mood^[22] Muntah^[18] Nosisepsi^[23] Ereksi penis^[24] Dilatasi pupil^[25] Respirasi^[26] Perilaku seksual^[27] Tidur^[28] Sosial^[29] Termoregulasi^[30] Vasokonstriksi^[31]	Selektif (untuk 5-HT_1A lebih dari reseptor 5-HT lainnya) Vilazodon (Viibryd) F-15,599 (senyawa untuk riset, sangat poten dan selektif untuk 5-HT_1A) Flesinoksan (poten, EC₅₀ = 24 nM) Gepiron (agonis parsial, K_i = 70 nM) Haloperidol Ipsapiron (agonis parsial, K_i = 12.1 nM) Kuetiapin Trazodon (SARI K_d = 78nM) Yohimbin (agonis parsial tidak selektif) Tandospiron (agonis parsial dan selektif) Nonselektif 5-CT (poten – K_i = 250±50 pM) 8-OH-DPAT (poten) Aripiprazol (antipsikotik atipikal) Asenapin (antipsikotik atipikal) Buspiron^[32] (agonis parsial) Vortioksetin (agonis parsial efikasi tinggi)^[33] Ziprasidon (agonis parsial, K_i = 3.4 nM)	BMY 7378 Sianopindolol Iodosianopindolol Lekozotan Metiotepin Metisergida^[34] NAN-190 Nebivolol Nefazodon WAY-100,135 WAY-100,635 Mefway	Analgesik (agonis) Antidepresan (agonis reseptor post-sinaptik dan antagonis autoreseptor pre-sinaptik sebagai antidepresan) Ansiolitik^[35] (antagonist)
5-HT_1B	1992	HTR1B			Tidak	Tidak	Tidak	Tidak	Addiksi^[36] Aggressi^[12] Kecemasan^[37]^[38]^[39] Autoreseptor Belajar^[40] Lokomosi^[41] Memori^[40] Mood^[39] Ereksi penis^[24] Perilaku seksual^[27] Vasokonstriksi	5-CT CGS-12066A CP-93,129 CP-94,253 Dihidroergotamin Eltoprazin Ergotamin Metisergida RU 24969 TFMPP Triptan^[32] (antimigrain^[32]) Zolmitriptan Eletriptan Sumatriptan Vortioksetin (agonis parsial, K_i = 33 nM)^[33]	Alprenolol AR-A000002 Asenapin Sianopindolol GR-127,935 Iodosianopindolol Isamoltan Metergolin Metiotepin Oksprenolol Pindolol Propranolol SB-216,641 Yohimbin	Migrain (mis. triptan)
5-HT_1D	1991	HTR1D			Tidak	Tidak	Tidak	Tidak	Ansietas^[42]^[43] Autoreseptor Lokomosi^[41] Vasokonstriksi	5-CT CP-135,807 Dihidroergotamin Ergotamin Metisergida Triptan^[32] (antimigrain^[32]) Almotriptan Eletriptan Frovatriptan Naratriptan Rizatriptan Sumatriptan Zolmitriptan Yohimbin	BRL-15572 GR-127,935 Ketanserin Metergolin Metiotepin Rauwolscine Ritanserin Vortioksetin (K_i = 54 nM)^[33] Ziprasidon	Migrain (mis. triptan)
5-HT_1E	1992	HTR1E			Tidak	Tidak	Tidak	Tidak		BRL-54443		Tidak diketahui
5-HT_1F	1993	HTR1F	Tidak		Tidak	Tidak	Tidak	Tidak	Migrain	BRL-54443 Lasmiditan LY-334,370 Naratriptan		Tidak diketahui
5-HT_2A	1988	HTR2A							Addiksi (modulasi secara potensial)^[44] Ansietas^[45] Nafsu makan Kognisi Imajinasi Belajar Memori Mood Persepsi Perilaku seksual^[46] Tidur^[47] Thermoregulasi^[48] Vasokonstriksi^[49]	25I-NBOMe (agonis penuh) 2C-B 5-MeO-DMT BZP Bufotenin DMT DOM Ergonovin Lisurida LSD Meskalin Myristicin PNU-22394 (agonis parsial)^[50]^[51]^[52] Psilosin Psilosibin TFMPP (agonis parsial atau antagonis)	antipsikotik atipikal Klozapin^[32] Olanzapin Kuetiapin Risperidon Ziprasidon Aripiprazol Asenapin Amitriptilin Klomipramin Siproheptadin Eplivanserin Etoperidon Haloperidol Hidroksizin Iloperidon Ketanserin^[32] (antihipertensi^[32]) Metisergida Mianserin Mirtazapin Nefazodon Pimavanserin Pizotifen Ritanserin Trazodon Yohimbin	Antipsikotik atipikal (antagonis) Psikedelik (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-HT_2B	1992	HTR2B							Kecemasan^[53]^[54]^[55] Nafsu makan^[56] Fungsi kardiovaskular Motilitas GI^[57] Tidur^[47] Vasokonstriksi	BW-723C86 Fenfluramin MDMA Norfenfluramin PNU-22394 (agonis parsial)^[50]^[51]^[52] Ro60-0175	Agomelatin Asenapin BZP Ketanserin Metisergida Ritanserin RS-127,445 Tegaserod Yohimbin	Migrain (antagonis)
5-HT_2C	1988	HTR2C							Addiksi. (modulasi secara potensial)^[44] Ansietas^[58]^[59]^[60] Nafsu makan Motilitas GI^[61] Heteroreseptor untuk norepinefrin dan dopamin Lokomosi Mood^[59]^[60] Ereksi penis^[62]^[63] Perilaku seksual^[46] Tidur^[64] Termoregulasi^[48] Vasokonstriksi	A-372,159 AL-38022A Aripiprazol Ergonovin Lorkaserin PNU-22394 (agonis penuh)^[50]^[51]^[52] Ro60-0175 TFMPP Trazodon^[32] (hipnotik^[32]) YM-348	Agomelatin^[32] (antidepresan^[32]) Amitriptilin Asenapin Klomipramin Klozapin^[32] (antipsikotik^[32]) Siproheptadin Dimebolin Eltoprazin Etoperidon Fluoksetin Haloperidol Iloperidone Ketanserin^[32] (antihipertensi^[32]) Lisurida Metisergida^[65] Mianserin Mirtazapin Nefazodon Olanzapin Paroksetin Kuetiapin Risperidon Ritanserin Tramadol Trazodon Ziprasidon	Antidepresan (misal agomelatin, fluoksetin, mirtazapin) Oreksigenik (misal mirtazapin, klozapin and olanzapin; antagonis) Anorektik (Lorkaserin) Antipsikotik (Vabikaserin; agonis)
5-HT₃	1993	HTR3A HTR3B HTR3C HTR3D HTR3E	Tidak			Tidak		Tidak	Adiksi Kecemasan Emesis Motilitas GI^[66] Belajar^[67] Memori^[67] Muntah	2-Methyl-5-HT BZP Kuipazin RS-56812	Alosetron Beberapa antimuntah^[32] Dolasetron Ondansetron^[32] Granisetron Tropisetron Klozapin Memantin Metoklopramid Mianserin Mirtazapin Olanzapin Kuetiapin Vortioksetin (K_i = 3.7 nM)^[33]	Antimuntah
5-HT₄	1995	HTR4	Tidak			Tidak		Tidak	Kecemasan^[68]^[69] Nafsu makan^[70]^[71] Motilitas GI Belajar^[72]^[73] Memori^[72]^[73]^[74] Mood^[75]^[76] Respirasi^[77]	5-MT BIMU-8 Cinitapride Kisaprida^[32] (gastroprokinetik) Dazoprida Metoklopramid Mosaprid Prukaloprida RS-67333 Renzaprida Tegaserod Zakoprida	L-Lysine^[68] Piboserod	Gastroprokinetik (misal Tegaserod)
5-HT_5A	1994	HTR5A	Tidak		Tidak	Tidak	Tidak	Tidak	Autoreseptor Lokomosi^[78] Tidur^[79]	5-CT Ergotamin Asam valerenat (agonis partial)^[79]	Asenapine Dimebolin Metiotepin Ritanserin SB-699,551 SB-699,551-A	Tidak ada selama ini
5-HT_5B	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	Kecemasan^[80]^[81] Kognisi^[82] Belajar^[83] Memori^[83] Mood^[81]^[84]	EMD-386,088 EMDT	Amitriptilin Aripiprazol Asenapin Klomipramin Klozapin Dimebolin EGIS-12233 Haloperidol Iloperidon MS-245 Olanzapin Ro04-6790 SB-258,585 SB-271,046^[85] SB-357,134 SB-399,885	Antidepresan (antagonis dan agonis) Anksiolitik (antagonis dan agonis) Nootropik (antagonis) Anorektik (antagonis)
5-HT₇	1993	HTR7				Tidak	Tidak	Tidak	Kecemasan^[86]^[87] Autoreseptor Memori^[88]^[89] Mood^[86]^[87] Respirasi^[26]^[90] Tidur^[86]^[90]^[91] Termoregulasi Vasokonstriksi	5-CT 8-OH-DPAT Aripiprazol (agonis parsial lemah)^[92] AS-19 E-55888 RA-7	Amitriptilin Asenapin Klomipramin Klozapin EGIS-12233 Haloperidol Iloperidon Imipramin Ketanserin Mirtazapin Olanzapin Ritanserin Risperidon SB-269,970 Vortioksetin (K_i = 19 nM)^[33]	Antidepresan (antagonis) Anksiolitik (antagonis) Nootropik (antagonis)

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↑ Malenka RC, Nestler EJ, Hyman SE (2009). Sydor A, Brown RY (ed.). Molecular Neuropharmacology: A Foundation for Clinical Neuroscience (Edisi 2nd). New York: McGraw-Hill Medical. hlm. 4. ISBN 978-0-07-148127-4. Similarly, little is known about which of serotonin's 14 known receptors must be activated to achieve an antidepressant response.

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↑ Nalivaiko E, Ootsuka Y, Blessing WW (2005). "Activation of 5-HT1A receptors in the medullary raphe reduces cardiovascular changes elicited by acute psychological and inflammatory stresses in rabbits". Am J Physiol Regul Integr Comp Physiol. 289 (2): R596 – R604. doi:10.1152/ajpregu.00845.2004. PMID 15802554.

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1 2 Millan MJ, Perrin-Monneyron S (1997). "Potentiation of fluoxetine-induced penile erections by combined blockade of 5-HT1A and 5-HT1B receptors". Eur J Pharmacol. 321 (3): 11–3. doi:10.1016/S0014-2999(97)00050-2. PMID 9085055.

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1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 Pharmacology Corner > Serotonin (5-HT): receptors, agonists and antagonists By Flavio Guzmán, M.D. on 9/08/09

1 2 3 4 5 "BRINTELLIX™ (vortioxetine) tablets for oral use. Full Prescribing Information, Section 12.2 (Pharmacodynamics)." Takeda Pharmaceuticals America Inc. and Lundbeck, 2013. Revised September 2013. Diarsipkan 2019-09-18 di Wayback Machine.

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↑ Harrison AA, Parsons LH, Koob GF, Markou A (1999). "RU 24969, a 5-HT1A/1B agonist, elevates brain stimulation reward thresholds: an effect reversed by GR 127935, a 5-HT1B/1D antagonist". Psychopharmacology (Berl). 141 (3): 242–50. doi:10.1007/s002130050831. PMID 10027505.

↑ Chojnacka-Wójcik E, Klodzinska A, Tatarczynska E (2005). "The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action". J Pharm Pharmacol. 57 (2): 253–7. doi:10.1211/0022357055399. PMID 15720791.

↑ Lin D, Parsons LH (2002). "Anxiogenic-like effect of serotonin(1B) receptor stimulation in the rat elevated plus-maze". Pharmacol Biochem Behav. 71 (4): 581–7. doi:10.1016/S0091-3057(01)00712-2. PMID 11888549.

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1 2 Eriksson TM, Madjid N, Elvander-Tottie E, Stiedl O, Svenningsson P, Ogren SO (2008). "Blockade of 5-HT 1B receptors facilitates contextual aversive learning in mice by disinhibition of cholinergic and glutamatergic neurotransmission". Neuropharmacology. 54 (7): 1041–50. doi:10.1016/j.neuropharm.2008.02.007. PMID 18394658.

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↑ Feuerstein TJ, Hüring H, van Velthoven V, Lücking CH, Landwehrmeyer GB (1996). "5-HT1D-like receptors inhibit the release of endogenously formed [3H]GABA in human, but not in rabbit, neocortex". Neurosci Lett. 209 (3): 210–4. doi:10.1016/0304-3940(96)12637-9. PMID 8736648.

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↑ Schreiber R, Melon C, De Vry J (1998). "The role of 5-HT receptor subtypes in the anxiolytic effects of selective serotonin reuptake inhibitors in the rat ultrasonic vocalization test". Psychopharmacology (Berl). 135 (4): 383–91. doi:10.1007/s002130050526. PMID 9539263.

1 2 Popova NK, Amstislavskaya TG (2002). "5-HT2A and 5-HT2C serotonin receptors differentially modulate mouse sexual arousal and the hypothalamo-pituitary-testicular response to the presence of a female". Neuroendocrinology. 76 (1): 28–34. doi:10.1159/000063681. PMID 12097814.

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1 2 Mazzola-Pomietto P, Aulakh CS, Tolliver T, Murphy DL (1997). "Functional subsensitivity of 5-HT2A and 5-HT2C receptors mediating hyperthermia following acute and chronic treatment with 5-HT2A/2C receptor antagonists". Psychopharmacology (Berl). 130 (2): 144–51. doi:10.1007/s002130050222. PMID 9106912.

↑ Blessing WW, Seaman B (2003). "5-hydroxytryptamine(2A) receptors regulate sympathetic nerves constricting the cutaneous vascular bed in rabbits and rats". Neuroscience. 117 (4): 939–948. doi:10.1016/S0306-4522(02)00810-2. PMID 12654345.

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