Reseptor serotonin

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.^[1][2] Reseptor serotonin memperantarai neurotransmisi eksitatori (pemicuan) dan inhibitori (penghambatan) yang beraksi terhadap ligan alaminya.

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

.

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.^[3]

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.[4]	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.^[5] Jenis tertentu telah ditandai sebagai berikut:^[6][7][8]

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[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] Thermoregulasi[30] Vasokonstriksi[31]	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[32] (agonis parsial) Vortioxetine (agonis parsial efikasi tinggi)[33] Ziprasidone (agonis parsial, Ki = 3.4 nM)	BMY 7378 Cyanopindolol Iodocyanopindolol Lecozotan Methiothepin Methysergide[34] 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[35] (antagonist)
5-HT1B	1992	HTR1B			Tidak	Tidak	Tidak	Tidak	Addiksi[36] Aggressi[12] Ansietas[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 Dihydroergotamine Eltoprazine Ergotamine Methysergide RU 24969 TFMPP Triptans[32] (antimigraine[32]) Zolmitriptan Eletriptan Sumatriptan Vortioxetine (partial agonist, Ki = 33 nM)[33]	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[42][43] Autoreseptor Lokomosi[41] Vasokonstriksi	5-CT CP-135,807 Dihydroergotamine Ergotamine Methysergide Triptans[32] (antimigrain[32]) Almotriptan Eletriptan Frovatriptan Naratriptan Rizatriptan Sumatriptan Zolmitriptan Yohimbine	BRL-15572 GR-127,935 Ketanserin Metergoline Methiothepin Rauwolscine Ritanserin Vortioxetine (Ki = 54 nM)[33] 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)[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 Ergonovine Lisuride LSD Mescaline Myristicin PNU-22394 (agonis parsial)[50][51][52] Psilocin Psilocybin TFMPP (agonis parsial atau antagonis)	antipsikotik atipikal Clozapine[32] Olanzapine Quetiapine Risperidone Ziprasidone Aripiprazole Asenapine Amitriptyline Clomipramine Cyproheptadine Eplivanserin Etoperidone Haloperidol Hydroxyzine Iloperidone Ketanserin[32] (antihypertensive[32]) 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[53][54][55] Nafsu makan[56] Fungsi kardiovaskular Motilitas GI[57] Tidur[47] Vasokonstriksi	BW-723C86 Fenfluramine MDMA Norfenfluramine PNU-22394 (agonis parsial)[50][51][52] Ro60-0175	Agomelatine Asenapine BZP Ketanserin Methysergide Ritanserin RS-127,445 Tegaserod Yohimbine	Migrain (antagonis)
5-HT2C	1988	HTR2C							Addiksi. (modulasi secara potensial)[44] Ansietas[58][59][60] Nafsu makan Motilitas GI[61] Heteroreceptor for norepinephrine and dopamine Lokomosi Mood[59][60] Ereksi penis[62][63] Perilaku seksual[46] Tidur[64] Thermoregulasi[48] Vasokonstriksi	A-372,159 AL-38022A Aripiprazole Ergonovine Lorcaserin PNU-22394 (agonis penuh)[50][51][52] Ro60-0175 TFMPP Trazodone[32] (hypnotic[32]) YM-348	Agomelatine[32] (antidepressant[32]) Amitriptyline Asenapine Klomipramin Klozapin[32] (antipsychotic[32]) Siproheptadine Dimebolin Eltoprazine Etoperidone Fluoksetin Haloperidol Iloperidone Ketanserin[32] (antihypertensive[32]) Lisuride Methysergide[65] 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[66] Belajar[67] Memori[67] Muntah	2-Methyl-5-HT BZP Quipazine RS-56812	Alosetron Beberapa antimuntah[32] Dolasetron Ondansetron[32] Granisetron Tropisetron Klozapin Memantin Metoklopramid Mianserin Mirtazapin Olanzapin Quetiapine Vortioxetine (Ki = 3.7 nM)[33]	Antimuntah
5-HT4	1995	HTR4	Tidak			Tidak		Tidak	Ansietas[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 Cisaprid[32] (gastroprokinetik) Dazopride Metoklopramid Mosaprid Prucalopride RS-67333 Renzapride Tegaserod Zacopride	L-Lysine[68] Piboserod	Gastroprokinetik (misal Tegaserod)
5-HT5A	1994	HTR5A	Tidak		Tidak	Tidak	Tidak	Tidak	Autoreseptor Lokomosi[78] Tidur[79]	5-CT Ergotamine Valerenic Acid (partial agonist)[79]	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[80][81] Kognisi[82] Belajar[83] Memori[83] Mood[81][84]	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[85] 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[86][87] Autoreseptor Memori[88][89] Mood[86][87] Respirasi[26][90] Sleep[86][90][91] Thermoregulasi 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 (Ki = 19 nM)[33]	Antidepresan (antagonis) Ansiolitik (antagonis) Nootropik (antagonis)

Referensi

1. Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR, Humphrey PP (1994). "International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin)". Pharmacol. Rev. 46 (2): 157–203. PMID 7938165.
2. Frazer A, Hensler JG (1999). "Chapter 13: Serotonin Receptors". Dalam Siegel GJ, Agranoff BW, Albers RW, Fisher SK, Uhler MD. Basic Neurochemistry: Molecular, Cellular, and Medical Aspects. Philadelphia: Lippincott-Raven. hlm. 263–292. ISBN 0-397-51820-X. Diakses tanggal 2008-04-11.
3. Qi YX, Xia RY, Wu YS, Stanley D, Huang J, Ye GY (2014). "Larvae of the small white butterfly, Pieris rapae, express a novel serotonin receptor". J. Neurochem. 131: 767–77. doi:10.1111/jnc.12940. PMID 25187179.
4. Francken BJ, Jurzak M, Vanhauwe JF, Luyten WH, Leysen JE (1998). "The human 5-ht5A receptor couples to Gi/Go proteins and inhibits adenylate cyclase in HEK 293 cells". Eur J Pharmacol. 361 (2–3): 299–309. doi:10.1016/S0014-2999(98)00744-4. PMID 9865521.
5. Malenka RC, Nestler EJ, Hyman SE (2009). Sydor A, Brown RY, ed. Molecular Neuropharmacology: A Foundation for Clinical Neuroscience (edisi ke-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.
6. Glennon RA, Dukat M, Westkaemper RB (2000-01-01). "Serotonin Receptor Subtypes and Ligands". American College of Neurophyscopharmacology. Diarsipkan dari versi asli tanggal 21 April 2008. Diakses tanggal 2008-04-11.
7. "5-Hydroxytryptamine Receptors". IUPHAR Receptor Database. International Union of Basic and Clinical Pharmacology. Diakses tanggal 2008-04-11.
8. Wesolowska A (2002). "In the search for selective ligands of 5-HT₅, 5-HT₆ and 5-HT₇ serotonin receptors" (PDF). Polish Journal of Pharmacology. 54 (4): 327–41. PMID 12523486.
9. Tomkins DM, Higgins GA, Sellers EM (1994). "Low doses of the 5-HT1A agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH DPAT) increase ethanol intake". Psychopharmacology (Berl). 115 (1–2): 173–9. doi:10.1007/BF02244769. PMID 7862892.
10. Müller CP, Carey RJ, Huston JP, De Souza Silva MA (2007). "Serotonin and psychostimulant addiction: focus on 5-HT1A-receptors". Prog Neurobiol. 81 (3): 133–78. doi:10.1016/j.pneurobio.2007.01.001. PMID 17316955.
11. Carey RJ, DePalma G, Damianopoulos E, Shanahan A, Müller CP, Huston JP (2005). "Evidence that the 5-HT1A autoreceptor is an important pharmacological target for the modulation of cocaine behavioral stimulant effects". Brain Res. 1034 (1–2): 162–71. doi:10.1016/j.brainres.2004.12.012. PMID 15713268.
12. de Boer SF, Koolhaas JM (2005). "5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis". Eur J Pharmacol. 526 (1–3): 125–39. doi:10.1016/j.ejphar.2005.09.065. PMID 16310183.
13. Parks CL, Robinson PS, Sibille E, Shenk T, Toth M (1998). "Increased anxiety of mice lacking the serotonin1A receptor". Proceedings of the National Academy of Sciences of the United States of America. 195 (18): 10734–9. doi:10.1073/pnas.95.18.10734. PMC 27964 . PMID 9724773.
14. Ebenezer IS, Arkle MJ, Tite RM (1998). "8-Hydroxy-2-(di-n-propylamino)-tetralin inhibits food intake in fasted rats by an action at 5-HT1A receptors". Methods Find Exp Clin Pharmacol. 29 (4): 269–72. doi:10.1358/mf.2007.29.4.1075362. PMID 17609739.
15. Wouters W, Tulp MT, Bevan P (1998). "Flesinoxan lowers blood pressure and heart rate in cats via 5-HT1A receptors". Eur J Pharmacol. 149 (3): 213–23. doi:10.1016/0014-2999(88)90651-6. PMID 2842163.
16. Horiuchi J, McDowall LM, Dampney RA (2008). "Role of 5-HT(1A) receptors in the lower brainstem on the cardiovascular response to dorsomedial hypothalamus activation". Auton Neurosci. 142 (1–2): 71–6. doi:10.1016/j.autneu.2008.06.004. PMID 18667366.
17. 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.
18. Lucot JB. (1994). "Antiemetic effects of flesinoxan in cats: comparisons with 8-hydroxy-2-(di-n-propylamino)tetralin". Eur J Pharmacol. 253 (1–2): 53–60. doi:10.1016/0014-2999(94)90756-0. PMID 8013549.
19. Winstanley CA, Theobald DE, Dalley JW, Robbins TW (2005). "Interactions between serotonin and dopamine in the control of impulsive choice in rats: therapeutic implications for impulse control disorders". Neuropsychopharmacology. 30 (4): 669–682. doi:10.1038/sj.npp.1300610. PMID 15688093.
20. Ogren SO, Eriksson TM, Elvander-Tottie E, D'Addario C, Ekström JC, Svenningsson P, Meister B, Kehr J, Stiedl O (2008). "The role of 5-HT(1A) receptors in learning and memory". Behav. Brain Res. 195 (1): 54–77. doi:10.1016/j.bbr.2008.02.023. PMID 18394726.
21. Yasuno F, Suhara T, Nakayama T, Ichimiya T, Okubo Y, Takano A, Ando T, Inoue M, Maeda J, Suzuki K (2003). "Inhibitory effect of hippocampal 5-HT1A receptors on human explicit memory". Am J Psychiatry. 160 (2): 334–40. doi:10.1176/appi.ajp.160.2.334. PMID 12562581.
22. Kennett GA, Dourish CT, Curzon G (1987). "Antidepressant-like action of 5-HT1A agonists and conventional antidepressants in an animal model of depression". Eur J Pharmacol. 134 (3): 265–74. doi:10.1016/0014-2999(87)90357-8. PMID 2883013.
23. Bardin L, Tarayre JP, Malfetes N, Koek W, Colpaert FC (2003). "Profound, non-opioid analgesia produced by the high-efficacy 5-HT(1A) agonist F 13640 in the formalin model of tonic nociceptive pain". Pharmacology. 67 (4): 182–194. doi:10.1159/000068404. PMID 12595749.
24. 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.
25. Prow MR, Martin KF, Heal DJ (1996). "8-OH-DPAT-induced mydriasis in mice: a pharmacological characterisation". Eur J Pharmacol. 317 (1): 21–8. doi:10.1016/S0014-2999(96)00693-0. PMID 8982715.
26. Meyer LC, Fuller A, Mitchell D (February 2006). "Zacopride and 8-OH-DPAT reverse opioid-induced respiratory depression and hypoxia but not catatonic immobilization in goats". American Journal of Physiology. Regulatory, Integrative and Comparative Physiology. 290 (2): R405–13. doi:10.1152/ajpregu.00440.2005. PMID 16166206.
27. Popova NK, Amstislavskaya TG (2002). "Involvement of the 5-HT(1A) and 5-HT(1B) serotonergic receptor subtypes in sexual arousal in male mice". Psychoneuroendocrinology. 27 (5): 609–18. doi:10.1016/S0306-4530(01)00097-X. PMID 11965359.
28. Monti JM, Jantos H (1992). "Dose-dependent effects of the 5-HT1A receptor agonist 8-OH-DPAT on sleep and wakefulness in the rat". J Sleep Res. 1 (3): 169–175. doi:10.1111/j.1365-2869.1992.tb00033.x. PMID 10607047.
29. Thompson MR, Callaghan PD, Hunt GE, Cornish JL, McGregor IS (2007). "A role for oxytocin and 5-HT(1A) receptors in the prosocial effects of 3,4 methylenedioxymethamphetamine ("ecstasy")". Neuroscience. 146 (2): 509–14. doi:10.1016/j.neuroscience.2007.02.032. PMID 17383105.
30. Gudelsky GA, Koenig JI, Meltzer HY (1986). "Thermoregulatory responses to serotonin (5-HT) receptor stimulation in the rat. Evidence for opposing roles of 5-HT2 and 5-HT1A receptors". Neuropharmacology. 25 (12): 1307–13. doi:10.1016/0028-3908(86)90101-2. PMID 2951611.
31. Ootsuka Y, Blessing WW (2006). "Activation of 5-HT1A receptors in rostral medullary raphé inhibits cutaneous vasoconstriction elicited by cold exposure in rabbits". Brain Res. 1073–1074: 252–61. doi:10.1016/j.brainres.2005.12.031. PMID 16455061.
32. Pharmacology Corner > Serotonin (5-HT): receptors, agonists and antagonists By Flavio Guzmán, M.D. on 9/08/09
33. "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.
34. Saxena, PR; Lawang, A (Oct 1985). "A comparison of cardiovascular and smooth muscle effects of 5-hydroxytryptamine and 5-carboxamidotryptamine, a selective agonist of 5-HT1 receptors". Archives Internationales de Pharmacodynamie et de Thérapie. 277 (2): 235–52. PMID 2933009.
35. Cao BJ, Rodgers RJ (October 1998). "Comparative effects of novel 5-HT1A receptor ligands, LY293284, LY315712 and LY297996, on plus-maze anxiety in mice". Psychopharmacology. 139 (3): 185–94. doi:10.1007/s002130050703. PMID 9784072.
36. 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.
37. 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.
38. 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.
39. Tatarczynska E, Klodzinska A, Stachowicz K, Chojnacka-Wójcik E (2004). "Effects of a selective 5-HT1B receptor agonist and antagonists in animal models of anxiety and depression". Behav Pharmacol. 15 (8): 523–34. doi:10.1097/00008877-200412000-00001. PMID 15577451.
40. 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.
41. McCreary AC, Bankson MG, Cunningham KA (1999). "Pharmacological studies of the acute and chronic effects of (+)-3, 4-methylenedioxymethamphetamine on locomotor activity: role of 5-hydroxytryptamine(1A) and 5-hydroxytryptamine(1B/1D) receptors". J Pharmacol Exp Ther. 290 (3): 965–73. PMID 10454466.
42. Amital D, Fostick L, Sasson Y, Kindler S, Amital H, Zohar J (2005). "Anxiogenic effects of Sumatriptan in panic disorder: a double-blind, placebo-controlled study". Eur Neuropsychopharmacol. 15 (3): 279–82. doi:10.1016/j.euroneuro.2004.12.002. PMID 15820416.
43. 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.
44. Bubar MJ, Cunningham KA. Serotonin 5-HT2A and 5-HT2C receptors as potential targets for modulation of psychostimulant use and dependence. Curr Top Med Chem. 2006;6(18):1971-85.
45. 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.
46. 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.
47. Popa D, Léna C, Fabre V, Prenat C, Gingrich J, Escourrou P, Hamon M, Adrien J (2005). "Contribution of 5-HT2 receptor subtypes to sleep-wakefulness and respiratory control, and functional adaptations in knock-out mice lacking 5-HT2A receptors". J Neurosci. 25 (49): 11231–8. doi:10.1523/JNEUROSCI.1724-05.2005. PMID 16339018.
48. 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.
49. 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.
50. McCall, R. B.; Franklin, S. R.; Hyslop, D. K.; Knauer, C. S.; Chio, C. L.; Haber, C. L.; Fitzgerald, L. W. (2001). "PNU-22394, a 5-HT2C receptor agonist, reduced feeding in rodents and produces weight loss in humans" (Online). 27 (309.2). Presentation Number 309.2. Convention Center Exhibit Hall, Poster Board TT-45, San Diego, CA: Society for Neuroscience Abstracts. Diakses tanggal 18 July 2014.
51. Garfield AS, Heisler LK (2009). "Pharmacological targeting of the serotonergic system for the treatment of obesity". The Journal of Physiology. 587 (1): 49–60. doi:10.1113/jphysiol.2008.164152. PMC 2670022 . PMID 19029184.
52. Jensen, Anders A.; Plath, Niels; Pedersen, Martin Holst Friborg; Isberg, Vignir; et al. (2013). "Design, Synthesis, and Pharmacological Characterization of N- and O-Substituted 5,6,7,8-Tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol Analogues: Novel 5-HT2A/5-HT2C Receptor Agonists with Pro-Cognitive Properties". Journal of Medicinal Chemistry. 56 (3): 1211–1227. doi:10.1021/jm301656h. ISSN 0022-2623.
53. Kennett GA, Bright F, Trail B, Baxter GS, Blackburn TP (1996). "Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety". Br J Pharmacol. 117 (7): 1443–8. doi:10.1111/j.1476-5381.1996.tb15304.x. PMC 1909458 . PMID 8730737.
54. Duxon MS, Kennett GA, Lightowler S, Blackburn TP, Fone KC (1997). "Activation of 5-HT2B receptors in the medial amygdala causes anxiolysis in the social interaction test in the rat". Neuropharmacology. 36 (4–5): 601–8. doi:10.1016/S0028-3908(97)00042-7. PMID 9225285.
55. Kennett GA, Trail B, Bright F (1998). "Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated". Neuropharmacology. 37 (12): 1603–10. doi:10.1016/S0028-3908(98)00115-4. PMID 9886683.
56. Kennett GA, Ainsworth K, Trail B, Blackburn TP (1997). "BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats". Neuropharmacology. 36 (2): 233–9. doi:10.1016/S0028-3908(96)00171-2. PMID 9144661.
57. Borman RA, Tilford NS, Harmer DW, Day N, Ellis ES, Sheldrick RL, Carey J, Coleman RA, Baxter GS (2002). "5-HT(2B) receptors play a key role in mediating the excitatory effects of 5-HT in human colon in vitro". Br J Pharmacol. 135 (5): 1144–1151. doi:10.1038/sj.bjp.0704571. PMC 1573235 . PMID 11877320.
58. Kennett GA, Wood MD, Bright F, Trail B, Riley G, Holland V, Avenell KY, Stean T, Upton N, Bromidge S, Forbes IT, Brown AM, Middlemiss DN, Blackburn TP (1997). "SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist". Neuropharmacology. 36 (4–5): 609–20. doi:10.1016/S0028-3908(97)00038-5. PMID 9225286.
59. Millan MJ, Brocco M, Gobert A, Dekeyne A (2005). "Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade". Psychopharmacology (Berl). 177 (4): 448–58. doi:10.1007/s00213-004-1962-z. PMID 15289999.
60. Millan MJ, Brocco M, Gobert A, Dekeyne A (2008). "S32006, a novel 5-HT2C receptor antagonist displaying broad-based antidepressant and anxiolytic properties in rodent models". Psychopharmacology (Berl). 199 (4): 549–68. doi:10.1007/s00213-008-1177-9. PMID 18523738.
61. Fujitsuka N, Asakawa A, Hayashi M, Sameshima M, Amitani H, Kojima S, Fujimiya M, Inui A (2009). "Selective serotonin reuptake inhibitors modify physiological gastrointestinal motor activities via 5-HT2c receptor and acyl ghrelin". Biol Psychiatry. 65 (9): 748–759. doi:10.1016/j.biopsych.2008.10.031. PMID 19058784.
62. Millan MJ, Peglion JL, Lavielle G, Perrin-Monneyron S (1997). "5-HT2C receptors mediate penile erections in rats: actions of novel and selective agonists and antagonists". Eur J Pharmacol. 325 (1): 9–12. doi:10.1016/S0014-2999(97)89962-1. PMID 9151932.
63. Stancampiano R, Melis MR, Argiolas A (1994). "Penile erection and yawning induced by 5-HT1C receptor agonists in male rats: relationship with dopaminergic and oxytocinergic transmission". Eur J Pharmacol. 261 (1–2): 149–55. doi:10.1016/0014-2999(94)90313-1. PMID 8001637.
64. Frank MG, Stryker MP, Tecott LH (2002). "Sleep and sleep homeostasis in mice lacking the 5-HT2c receptor". Neuropsychopharmacology. 27 (5): 869–73. doi:10.1016/S0893-133X(02)00353-6. PMC 2452994 . PMID 12431861.
65. Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 187
66. Michel K, Zeller F, Langer R, Nekarda H, Kruger D, Dover TJ, Brady CA, Barnes NM, Schemann M (May 2005). "Serotonin excites neurons in the human submucous plexus via 5-HT3 receptors". National Center for Biotechnology Information. Diakses tanggal 10 October 2014.
67. Pitsikas N, Brambilla A, Borsini F (1994). "Effect of DAU 6215, a novel 5-HT3 receptor antagonist, on scopolamine-induced amnesia in the rat in a spatial learning task". Pharmacol Biochem Behav. 47 (1): 95–99. doi:10.1016/0091-3057(94)90116-3. PMID 8115433.
68. Smriga M, Torii K (2003). "L-Lysine acts like a partial serotonin receptor 4 antagonist and inhibits serotonin-mediated intestinal pathologies and anxiety in rats". Proceedings of the National Academy of Sciences of the United States of America. 100 (26): 15370–5. doi:10.1073/pnas.2436556100. PMC 307574 . PMID 14676321.
69. Kennett GA, Bright F, Trail B, Blackburn TP, Sanger GJ (1997). "Anxiolytic-like actions of the selective 5-HT4 receptor antagonists SB 204070A and SB 207266A in rats". Neuropharmacology. 36 (4–5): 707–12. doi:10.1016/S0028-3908(97)00037-3. PMID 9225297.
70. Jean A, Conductier G, Manrique C, Bouras C, Berta P, Hen R, Charnay Y, Bockaert J, Compan V (2007). "Anorexia induced by activation of serotonin 5-HT4 receptors is mediated by increases in CART in the nucleus accumbens". Proceedings of the National Academy of Sciences of the United States of America. 104 (41): 16335–40. doi:10.1073/pnas.0701471104. PMC 2042207 . PMID 17913892.
71. Compan V; Charnay, Y; Dusticier, N; Daszuta, A; Hen, R; Bockaert, J (2004). "Feeding disorders in 5-HT4 receptor knockout mice". J Soc Biol. 198 (1): 37–49. PMID 15146954.
72. Meneses A, Hong E (1997). "Effects of 5-HT4 receptor agonists and antagonists in learning". Pharmacol Biochem Behav. 56 (3): 347–51. doi:10.1016/S0091-3057(96)00224-9. PMID 9077568.
73. Fontana DJ, Daniels SE, Wong EH, Clark RD, Eglen RM (1997). "The effects of novel, selective 5-hydroxytryptamine (5-HT)4 receptor ligands in rat spatial navigation". Neuropharmacology. 36 (4–5): 689–96. doi:10.1016/S0028-3908(97)00055-5. PMID 9225295.
74. Fontana DJ, Daniels SE, Wong EH, Clark RD, Eglen RM (1998). "Role of 5-HT4 receptors in the mouse passive avoidance test". J Pharmacol Exp Ther. 286 (3): 1115–21. PMID 9732367.
75. Lucas, G.; Rymar, V. V.; Du, J.; Mnie-Filali, O.; Bisgaard, C.; Manta, S.; Lambas-Senas, L.; Wiborg, O.; Haddjeri, N.; Piñeyro, G.; Sadikot, A. F.; Debonnel, G. (2007). "Serotonin4 (5-HT4) Receptor Agonists Are Putative Antidepressants with a Rapid Onset of Action". Neuron. 55 (5): 712–725. doi:10.1016/j.neuron.2007.07.041. PMID 17785179.
76. Duman, R. S. (2007). "A Silver Bullet for the Treatment of Depression?". Neuron. 55 (5): 679–681. doi:10.1016/j.neuron.2007.08.011. PMID 17785173.
77. Manzke, T. (2003). "5-HT4(a) Receptors Avert Opioid-Induced Breathing Depression Without Loss of Analgesia". Science. 301 (5630): 226–229. doi:10.1126/science.1084674. ISSN 0036-8075. PMID 12855812.
78. Nelson DL (2004). "5-HT5 receptors". Curr Drug Targets CNS Neurol Disord. 3 (1): 53–8. doi:10.2174/1568007043482606. PMID 14965244.
79. Dietz BM, Mahady GB, Pauli GF, Farnsworth NR (2005). "Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro". Brain Res Mol Brain Res. 138 (2): 191–7. doi:10.1016/j.molbrainres.2005.04.009. PMID 15921820.
80. Wesolowska A (February 2008). "The anxiolytic-like effect of the selective 5-HT6 receptor antagonist SB-399885: the impact of benzodiazepine receptors". European Journal of Pharmacology. 580 (3): 355–60. doi:10.1016/j.ejphar.2007.11.022. PMID 18096153.
81. Wesolowska A, Nikiforuk A (April 2007). "Effects of the brain-penetrant and selective 5-HT6 receptor antagonist SB-399885 in animal models of anxiety and depression". Neuropharmacology. 52 (5): 1274–83. doi:10.1016/j.neuropharm.2007.01.007. PMID 17320917.
82. Hirst WD, Stean TO, Rogers DC, Sunter D, Pugh P, Moss SF, Bromidge SM, Riley G, Smith DR, Bartlett S, Heidbreder CA, Atkins AR, Lacroix LP, Dawson LA, Foley AG, Regan CM, Upton N (December 2006). "SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models". European Journal of Pharmacology. 553 (1–3): 109–19. doi:10.1016/j.ejphar.2006.09.049. PMID 17069795.
83. Perez-García G, Meneses A (July 2005). "Oral administration of the 5-HT6 receptor antagonists SB-357134 and SB-399885 improves memory formation in an autoshaping learning task". Pharmacology, Biochemistry, and Behavior. 81 (3): 673–82. doi:10.1016/j.pbb.2005.05.005. PMID 15964617.
84. Wesolowska A, Nikiforuk A (March 2008). "The selective 5-HT(6) receptor antagonist SB-399885 enhances anti-immobility action of antidepressants in rats". European Journal of Pharmacology. 582 (1–3): 88–93. doi:10.1016/j.ejphar.2007.12.013. PMID 18234190.
85. "Target Schizophrenia – Possible future developments". The Association of the British Pharmaceutical Industry. Diarsipkan dari versi asli tanggal 2008-06-12. Diakses tanggal 2008-04-11.
86. Hedlund PB, Huitron-Resendiz S, Henriksen SJ, Sutcliffe JG (November 2005). "5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern". Biological Psychiatry. 58 (10): 831–7. doi:10.1016/j.biopsych.2005.05.012. PMID 16018977.
87. Wesolowska A, Nikiforuk A, Stachowicz K, Tatarczynska E (September 2006). "Effect of the selective 5-HT7 receptor antagonist SB 269970 in animal models of anxiety and depression". Neuropharmacology. 51 (3): 578–86. doi:10.1016/j.neuropharm.2006.04.017. PMID 16828124.
88. Gasbarri A, Cifariello A, Pompili A, Meneses A (December 2008). "Effect of 5-HT(7) antagonist SB-269970 in the modulation of working and reference memory in the rat". Behavioural Brain Research. 195 (1): 164–70. doi:10.1016/j.bbr.2007.12.020. PMID 18308404.
89. Liy-Salmeron G, Meneses A (2008). "Effects of 5-HT drugs in prefrontal cortex during memory formation and the ketamine amnesia-model". Hippocampus. 18 (9): 965–74. doi:10.1002/hipo.20459. PMID 18570192.
90. Bonaventure P, Kelly L, Aluisio L, Shelton J, Lord B, Galici R, Miller K, Atack J, Lovenberg TW, Dugovic C (2007). "Selective blockade of 5-hydroxytryptamine (5-HT)7 receptors enhances 5-HT transmission, antidepressant-like behavior, and rapid eye movement sleep suppression induced by citalopram in rodents". J Pharmacol Exp Ther. 321 (2): 690–8. doi:10.1124/jpet.107.119404. PMID 17314195.
91. Thomas DR, Melotto S, Massagrande M, Gribble AD, Jeffrey P, Stevens AJ, Deeks NJ, Eddershaw PJ, Fenwick SH, Riley G, Stean T, Scott CM, Hill MJ, Middlemiss DN, Hagan JJ, Price GW, Forbes IT (2003). "SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats". Br J Pharmacol. 139 (4): 705–14. doi:10.1038/sj.bjp.0705290. PMC 1573887 . PMID 12812993.
92. Davies MA, Sheffler DJ, Roth BL. Aripiprazole: A Novel Atypical Antipsychotic Drug With a Uniquely Robust Pharmacology. CNS Drug Reviews [Internet]. 2004 [cited 2013 Aug 4];10(4):317–36. Available from: http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2004.tb00030.x/pdf