Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT6MSOK)

• DTT Name: 5-HT 1D receptor (HTR1D)
• Synonyms: Serotonin receptor 1D; Serotonin 1D alpha receptor; HTRL; HTR1DA; 5HT1D; 5-hydroxytryptamine receptor 1D; 5-HT1D receptor; 5-HT1D; 5-HT-1D-alpha; 5-HT-1D
• Gene Name: HTR1D
• DTT Type: Successful target; [1]
• Related Disease:
  Migraine [ICD-11: 8A80]
  Pituitary gland disorder [ICD-11: 5A60-5A61]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: 5HT1D_HUMAN
• TTD ID: T11072
• Sequence:
  MSPLNQSAEGLPQEASNRSLNATETSEAWDPRTLQALKISLAVVLSVITLATVLSNAFVL
  TTILLTRKLHTPANYLIGSLATTDLLVSILVMPISIAYTITHTWNFGQILCDIWLSSDIT
  CCTASILHLCVIALDRYWAITDALEYSKRRTAGHAATMIAIVWAISICISIPPLFWRQAK
  AQEEMSDCLVNTSQISYTIYSTCGAFYIPSVLLIILYGRIYRAARNRILNPPSLYGKRFT
  TAHLITGSAGSSLCSLNSSLHEGHSHSAGSPLFFNHVKIKLADSALERKRISAARERKAT
  KILGIILGAFIICWLPFFVVSLVLPICRDSCWIHPALFDFFTWLGYLNSLINPIIYTVFN
  EEFRQAFQKIVPFRKAS
• Function: Functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Regulates the release of 5-hydroxytryptamine in the brain, and thereby affects neural activity. May also play a role in regulating the release of other neurotransmitters. May play a role in vasoconstriction. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
• KEGG Pathway:
  cAMP signaling pathway (hsa04024)
  Neuroactive ligand-receptor interaction (hsa04080)
  Serotonergic synapse (hsa04726)
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Serotonin receptors (R-HSA-390666)

Molecular Interaction Atlas (MIA) of This DTT

7 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Almogran	DM7I64Z	Migraine	8A80	Approved	[2]
Eletriptan	DMW649X	Migraine	8A80	Approved	[3]
Frovatriptan	DM7RE8P	Migraine	8A80	Approved	[3]
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[4]
Rizatriptan	DMDJMA3	Migraine	8A80	Approved	[5]
Sumatriptan	DMVYXR8	Migraine	8A80	Approved	[1], [6], [7], [8], [9]
Zolmitriptan	DM1IB4Q	Migraine	8A80	Approved	[3]

5 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
FKB01MD	DM2O7NM	N. A.	N. A.	Phase 2	[10]
Neu-P11	DMIQDFW	Alzheimer disease	8A20	Phase 2	[11]
NXN-188	DMMBAIH	Migraine	8A80	Phase 2	[12]
TGBA01AD	DMJ2FTU	Mood disorder	6A60-6E23	Phase 2	[13]
Tonabersat	DMT4OPL	Epilepsy	8A60-8A68	Phase 2	[14], [15]

16 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alniditan	DMFE3CT	Migraine	8A80	Discontinued in Phase 3	[16], [15], [16]
Avitriptan	DM3SE2N	Migraine	8A80	Discontinued in Phase 3	[17], [15]
BMS-181101	DMT4VSE	Mood disorder	6A60-6E23	Discontinued in Phase 2	[18], [15]
CP-122288	DM3OJP0	Migraine	8A80	Discontinued in Phase 2	[19], [15]
Elzasonan hydrochloride	DM1EOC3	Mood disorder	6A60-6E23	Discontinued in Phase 2	[20]
IS-159	DMLQWFA	Migraine	8A80	Discontinued in Phase 2	[21]
PNU-142633	DMLK5IM	Migraine	8A80	Discontinued in Phase 2	[22], [15]
ALX-0646	DMNOZAI	Migraine	8A80	Discontinued in Phase 1	[15]
Tidembersat	DMTC4LP	Migraine	8A80	Discontinued in Phase 1	[15]
BMS-181885	DMYWI04	Migraine	8A80	Terminated	[18], [15]
GR-127935	DM01HLX	Major depressive disorder	6A70.3	Terminated	[24]
L-694247	DM2F4GT	Migraine	8A80	Terminated	[25], [15]
L-741604	DMNSH0V	N. A.	N. A.	Terminated	[26]
L-775606	DMJ37IX	N. A.	N. A.	Terminated	[27]
PNU-109291	DMZNM2K	Migraine	8A80	Terminated	[28], [15]
VR-147	DMLWQOP	Migraine	8A80	Terminated	[29], [15]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Donitriptan	DMA2K7C	Migraine	8A80	Preclinical	[23]

78 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[30]
(3-Chloro-phenyl)-piperazin-1-yl-methanone	DM7U02R	Discovery agent	N.A.	Investigative	[31]
1,2,3,4-Tetrahydro-naphthalen-2-ylamine	DMP4DLV	Discovery agent	N.A.	Investigative	[32]
1-((S)-2-aminopropyl)-1H-indazol-6-ol	DMU83KP	Discovery agent	N.A.	Investigative	[33]
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine	DM31CVR	Discovery agent	N.A.	Investigative	[31]
1-(2,5-Dimethoxy-phenyl)-piperazine	DMNETHQ	Discovery agent	N.A.	Investigative	[31]
1-(2,5-dimethoxyphenyl)propan-2-amine	DM043N8	Discovery agent	N.A.	Investigative	[34]
1-(2-Butoxy-phenyl)-piperazine	DMT5S2O	Discovery agent	N.A.	Investigative	[35]
1-(2-Ethoxy-phenyl)-piperazine	DM2P7YX	Discovery agent	N.A.	Investigative	[35]
1-(2-Fluoro-phenyl)-piperazine	DM94LID	Discovery agent	N.A.	Investigative	[35]
1-(2-Isopropoxy-phenyl)-piperazine	DM5KAH6	Discovery agent	N.A.	Investigative	[35]
1-(2-Methoxy-phenyl)-piperazine	DM3M4RA	Discovery agent	N.A.	Investigative	[35]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine	DMX5N3V	Discovery agent	N.A.	Investigative	[36]
1-(3-Fluoro-phenyl)-piperazine	DM2SNR0	Discovery agent	N.A.	Investigative	[35]
1-(3-Nitro-phenyl)-piperazine	DMMJC5E	Discovery agent	N.A.	Investigative	[35]
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine	DMCH6R1	Discovery agent	N.A.	Investigative	[31]
1-(7-Methoxy-naphthalen-2-yl)-piperazine	DM1MJCE	Discovery agent	N.A.	Investigative	[37]
1-Naphthalen-2-yl-piperazine	DMJK0MF	Discovery agent	N.A.	Investigative	[32]
1-naphthylpiperazine	DM6BIWK	Discovery agent	N.A.	Investigative	[38], [32]
2-(2,6-Dimethyl-benzyl)-4,5-dihydro-1H-imidazole	DM7JUK0	Discovery agent	N.A.	Investigative	[39]
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol	DMZNRFG	Discovery agent	N.A.	Investigative	[34]
2-(2-Methoxy-phenyl)-1-methyl-ethylamine	DMDI98B	Discovery agent	N.A.	Investigative	[34]
2-(3-Methoxy-phenyl)-1-methyl-ethylamine	DM4C9H2	Discovery agent	N.A.	Investigative	[34]
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine	DM79JVK	Discovery agent	N.A.	Investigative	[34]
2-(4-Bromo-phenyl)-1-methyl-ethylamine	DMB49UP	Discovery agent	N.A.	Investigative	[34]
2-(4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole	DM1A4BS	Discovery agent	N.A.	Investigative	[39]
2-(5-Nonyloxy-1H-indol-3-yl)-ethylamine	DM2TU6W	Discovery agent	N.A.	Investigative	[40]
2-(5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine	DM1AEK4	Discovery agent	N.A.	Investigative	[41]
2-methyl-5-HT	DM1S5CB	N. A.	N. A.	Investigative	[42]
2-Piperazin-1-yl-benzonitrile	DM742IJ	Discovery agent	N.A.	Investigative	[35]
2-Piperazin-1-yl-phenol	DMQT9OK	Discovery agent	N.A.	Investigative	[31]
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one	DMKGIQ1	Discovery agent	N.A.	Investigative	[31]
5,6-dichloro-3,4-dihydroquinazolin-2-amine	DMN1S35	Discovery agent	N.A.	Investigative	[43]
5-amino-3-(N-methylpiperidin-4-yl)-1H-indole	DMJKQ5I	Discovery agent	N.A.	Investigative	[27]
5-chloro-3,4-dihydroquinazolin-2-amine	DMKEFJ0	Discovery agent	N.A.	Investigative	[43]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine	DM7FZU2	Discovery agent	N.A.	Investigative	[43]
5-CT	DM260KD	Discovery agent	N.A.	Investigative	[4]
5-Ethyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole	DMK57W2	Discovery agent	N.A.	Investigative	[44]
5-Isopropyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole	DMXGRMB	Discovery agent	N.A.	Investigative	[44]
7-methoxy-1-naphthylpiperazine	DM3MXI5	Discovery agent	N.A.	Investigative	[37]
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline	DMQIFZC	Discovery agent	N.A.	Investigative	[32]
8-Methoxy-2-piperazin-1-yl-quinoline	DMNWC29	Discovery agent	N.A.	Investigative	[32]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine	DMK6U2V	Discovery agent	N.A.	Investigative	[43]
8-Methoxy-quinolin-2-ylamine	DMHZ5SB	Discovery agent	N.A.	Investigative	[32]
9-OH-risperidone	DMGORXQ	Discovery agent	N.A.	Investigative	[45]
AGROCLAVINE	DMT9FJZ	Discovery agent	N.A.	Investigative	[46]
alpha-methyl-5-HT	DMCAYXF	Discovery agent	N.A.	Investigative	[42]
BRL-15572	DMM61Y2	Discovery agent	N.A.	Investigative	[47]
Brolamfetamine	DMC4PF0	Discovery agent	N.A.	Investigative	[34]
bufotenine	DMD1SY9	Discovery agent	N.A.	Investigative	[42]
Chlorophenylpiperazine	DMOA8L2	Discovery agent	N.A.	Investigative	[35]
dipropyl-5-CT	DM9VKXC	Discovery agent	N.A.	Investigative	[38]
EDMT	DMS3AXK	Discovery agent	N.A.	Investigative	[48]
Etisulergine	DMKH8TC	Discovery agent	N.A.	Investigative	[49]
L-747201	DMBPWSJ	Discovery agent	N.A.	Investigative	[50]
L-760790	DMA9VDN	Discovery agent	N.A.	Investigative	[26]
L-772,405	DM5O0CM	Discovery agent	N.A.	Investigative	[51]
lysergic acid	DM4MGAQ	Discovery agent	N.A.	Investigative	[42]
lysergol	DM1OHF8	Discovery agent	N.A.	Investigative	[38]
m-chlorophenylpiperazine	DMM1J2D	Discovery agent	N.A.	Investigative	[4]
MPDT	DMYX31S	Discovery agent	N.A.	Investigative	[48]
PHENYLPIPERAZINE	DMWAK1R	Discovery agent	N.A.	Investigative	[32]
Quipazine	DMPY6IG	Discovery agent	N.A.	Investigative	[32]
SB 216641	DMB3R4Z	Discovery agent	N.A.	Investigative	[47]
SB 272183	DMOLNQX	Discovery agent	N.A.	Investigative	[52]
SB 649915	DM21Z6H	Discovery agent	N.A.	Investigative	[53]
SB 714786	DMGHRY0	Discovery agent	N.A.	Investigative	[53]
Serotonin	DMOFCRY	Discovery agent	N.A.	Investigative	[27]
TFMPP	DMAC8TP	Discovery agent	N.A.	Investigative	[4], [31]
WAY-466	DMMOH51	Discovery agent	N.A.	Investigative	[54]
[125I]GTI	DMSYT5P	Discovery agent	N.A.	Investigative	[55]
[2-(5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine	DMOZ73L	Discovery agent	N.A.	Investigative	[44]
[3H]5-CT	DMEAHFZ	Discovery agent	N.A.	Investigative	[56]
[3H]5-HT	DMYJXV7	Discovery agent	N.A.	Investigative	[16]
[3H]8-OH-DPAT	DM4KCYU	Discovery agent	N.A.	Investigative	[57]
[3H]eletriptan	DMDTYRV	Discovery agent	N.A.	Investigative	[58]
[3H]GR 125,743	DM4URBO	Discovery agent	N.A.	Investigative	[56]
[3H]sumatriptan	DM3MBGV	Discovery agent	N.A.	Investigative	[58]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Major depressive disorder	6A20	Pre-frontal cortex	4.57E-01	-0.02	-0.15

References

• [1] Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.
• [2] Efficacy and tolerability of subcutaneous almotriptan for the treatment of acute migraine: a randomized, double-blind, parallel-group, dose-finding study. Clin Ther. 2001 Nov;23(11):1867-75.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [4] Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol Pharmacol. 1991 Aug;40(2):143-8.
• [5] An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210.
• [6] 5-Hydroxytryptamine(1F) receptors do not participate in vasoconstriction: lack of vasoconstriction to LY344864, a selective serotonin(1F) receptor agonist in rabbit saphenous vein. J Pharmacol Exp Ther. 1999 Sep;290(3):935-9.
• [7] 5-Hydroxytryptamine receptor agonists for the abortive treatment of vascular headaches block mast cell, endothelial and platelet activation within the rat dura mater after trigeminal stimulation. Brain Res. 1992 Jun 26;583(1-2):137-49.
• [8] Novel approaches to the treatment of nausea and vomiting. Dig Dis. 1999;17(3):125-32.
• [9] Serotonin in migraine: theories, animal models and emerging therapies. Prog Drug Res. 1998;51:219-44.
• [10] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [11] Clinical pipeline report, company report or official report of Neurim Pharmaceuticals.
• [12] Company report (NeurAxon)
• [13] Company report (Fabrekramer)
• [14] The potential anti-migraine compound SB-220453 does not contract human isolated blood vessels or myocardium; a comparison with sumatriptan. Cephalalgia. 2000 Jul;20(6):538-45.
• [15] Sustained pain relief with dihydroergotamine in migraine is potentially due to persistent binding to 5-HT1B and 5-HT1D receptors. . The Journal of Headache and Pain 201314(Suppl 1):P75.
• [16] Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol. 1998 Apr;123(8):1655-65.
• [17] Safety trial with the 5HT1B/1D agonist avitriptan (BMS-180048) in patients with migraine who have experienced pressure, tightness, and/or pain in the chest, neck, and/or throat following sumatriptan.Cephalalgia. 1998 Oct;18(8):546-51.
• [18] Sensitive triple-quadrupole mass spectrometric assay for the determination of BMS-181885, a 5-HT1 agonist, in human plasma following solid phase extraction. Biomed Chromatogr. 1999 Oct;13(6):425-30.
• [19] The 5-HT1D receptor antagonist GR-127,935 prevents inhibitory effects of sumatriptan but not CP-122,288 and 5-CT on neurogenic plasma extravasation within guinea pig dura mater. Neuropharmacology. 1997 Jan;36(1):83-91.
• [20] DOI: 10.1002/9781118541203.xen439
• [21] Pronounced effect of caprylocaproyl macrogolglycerides on nasal absorption of IS-159, a peptide serotonin 1B/1D-receptor agonist. Clin Pharmacol Ther. 2000 Aug;68(2):114-21.
• [22] Further characterization of the 5-HT1 receptors mediating cardiac sympatho-inhibition in pithed rats: pharmacological correlation with the 5-HT1B a... Naunyn Schmiedebergs Arch Pharmacol. 2004 Feb;369(2):220-7.
• [23] Donitriptan, but not sumatriptan, inhibits capsaicin-induced canine external carotid vasodilatation via 5-HT1B rather than 5-HT1D receptors.Br J Pharmacol.2006 Sep;149(1):82-91.
• [24] GR127935: a potent and selective 5-HT1D receptor antagonist.Behav Brain Res.1996;73(1-2):157-61.
• [25] L-694,247: a potent 5-HT1D receptor agonist. Br J Pharmacol. 1993 Nov;110(3):1196-200.
• [26] 3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents. J Med Chem. 1999 Feb 25;42(4):691-705.
• [27] Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-pip... J Med Chem. 2008 Jun 26;51(12):3609-16.
• [28] Role of 5-HT(1) receptor subtypes in the modulation of pain and synaptic transmission in rat spinal superficial dorsal horn. Br J Pharmacol. 2012 Mar;165(6):1956-65.
• [29] US patent application no. 2010,0112,050, Dosage form for insertion into the mouth.
• [30] Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
• [31] Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents. J Med Chem. 1986 May;29(5):630-4.
• [32] 5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. J Med Chem. 1986 Nov;29(11):2375-80.
• [33] 1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. J Med Chem. 2006 Jan 12;49(1):318-28.
• [34] 5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues. J Med Chem. 1986 Feb;29(2):194-9.
• [35] Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy. J Med Chem. 1989 May;32(5):1052-6.
• [36] The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine. Bioorg Med Chem. 2007 Nov 1;15(21):6659-66.
• [37] 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. J Med Chem. 1997 Nov 21;40(24):3974-8.
• [38] Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta. Proc Natl Acad Sci U S A. 1992 Apr 15;89(8):3630-4.
• [39] 2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4697-9.
• [40] 5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist. J Med Chem. 1994 Sep 2;37(18):2828-30.
• [41] 5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine. Bioorg Med Chem Lett. 2000 May 1;10(9):903-5.
• [42] Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan. Mol Pharmacol. 1996 Dec;50(6):1567-80.
• [43] Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61.
• [44] 5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists. Bioorg Med Chem Lett. 2000 Aug 7;10(15):1707-9.
• [45] Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.
• [46] Ergolines as selective 5-HT1 agonists. J Med Chem. 1988 Aug;31(8):1512-9.
• [47] SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20.
• [48] 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
• [49] Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-... J Med Chem. 1985 Oct;28(10):1540-2.
• [50] Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents. J Med Chem. 1997 Oct 24;40(22):3501-3.
• [51] 3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists. J Med Chem. 1999 Dec 2;42(24):4981-5001.
• [52] SB-272183, a selective 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptor antagonist in native tissue. Br J Pharmacol. 2001 Jul;133(6):797-806.
• [53] Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. J Med Chem. 2005 May 19;48(10):3478-80.
• [54] Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. J Med Chem. 2005 Jan 27;48(2):353-6.
• [55] Autoradiographic characterisation and localisation of 5-HT1D compared to 5-HT1B binding sites in rat brain. Naunyn Schmiedebergs Arch Pharmacol. 1993 Jun;347(6):569-82.
• [56] Serotonin 5-HT1B and 5-HT1D receptors form homodimers when expressed alone and heterodimers when co-expressed. FEBS Lett. 1999 Jul 30;456(1):63-7.
• [57] Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1999 Jun;359(6):447-53.
• [58] Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol. 1999 Mar 5;368(2-3):259-68.