Proteins > 5-hydroxytryptamine receptor 1D
Page last updated: 2024-08-07 16:20:16
5-hydroxytryptamine receptor 1D
A 5-hydroxytryptamine receptor 1D that is encoded in the genome of human. [PRO:WCB, UniProtKB:P28221]
Synonyms
5-HT-1D;
5-HT1D;
Serotonin 1D alpha receptor;
5-HT-1D-alpha;
Serotonin receptor 1D
Research
Bioassay Publications (86)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (1.16) | 18.7374 |
| 1990's | 32 (37.21) | 18.2507 |
| 2000's | 38 (44.19) | 29.6817 |
| 2010's | 11 (12.79) | 24.3611 |
| 2020's | 4 (4.65) | 2.80 |
Compounds (84)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tryptamine | Homo sapiens (human) | Ki | 0.0610 | 1 | 1 |
| 8-hydroxy-2-(di-n-propylamino)tetralin | Homo sapiens (human) | Ki | 0.1395 | 2 | 2 |
| 1-(1-naphthyl)piperazine | Homo sapiens (human) | Ki | 0.0062 | 2 | 2 |
| 2-methyl-5-ht | Homo sapiens (human) | Ki | 1.2200 | 1 | 1 |
| 5-(nonyloxy)tryptamine | Homo sapiens (human) | Ki | 0.0160 | 1 | 1 |
| methylbufotenin | Homo sapiens (human) | IC50 | 0.0490 | 1 | 1 |
| 5-methoxytryptamine | Homo sapiens (human) | Ki | 0.0054 | 1 | 1 |
| alpha-methylserotonin | Homo sapiens (human) | Ki | 0.1500 | 1 | 1 |
| cgs 12066 | Homo sapiens (human) | IC50 | 0.0350 | 1 | 1 |
| ketanserin | Homo sapiens (human) | IC50 | 3.5100 | 3 | 3 |
| mianserin | Homo sapiens (human) | IC50 | 0.3802 | 2 | 2 |
| 1-(3-trifluoromethylphenyl)piperazine | Homo sapiens (human) | IC50 | 0.6100 | 1 | 1 |
| naratriptan | Homo sapiens (human) | Ki | 0.0023 | 1 | 1 |
| oxymetazoline | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| 4-iodoclonidine | Homo sapiens (human) | Ki | 0.0500 | 1 | 1 |
| prazosin | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| rizatriptan | Homo sapiens (human) | IC50 | 0.0452 | 2 | 2 |
| rizatriptan | Homo sapiens (human) | Ki | 0.0193 | 3 | 3 |
| sumatriptan | Homo sapiens (human) | IC50 | 0.3091 | 8 | 8 |
| sumatriptan | Homo sapiens (human) | Ki | 0.0077 | 12 | 12 |
| tolazoline | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
| xylometazoline | Homo sapiens (human) | Ki | 0.0007 | 2 | 2 |
| lysergic acid diethylamide | Homo sapiens (human) | Ki | 0.0039 | 1 | 1 |
| ergotamine | Homo sapiens (human) | Ki | 0.0032 | 4 | 5 |
| indopan | Homo sapiens (human) | Ki | 1.8926 | 1 | 2 |
| 5-methyltryptamine | Homo sapiens (human) | Ki | 0.0064 | 1 | 1 |
| penfluridol | Homo sapiens (human) | Ki | 3.5600 | 1 | 1 |
| zolmitriptan | Homo sapiens (human) | IC50 | 0.0028 | 1 | 1 |
| zolmitriptan | Homo sapiens (human) | Ki | 0.0019 | 3 | 3 |
| frovatriptan | Homo sapiens (human) | Ki | 0.0044 | 1 | 1 |
| xylonidine | Homo sapiens (human) | Ki | 2.0750 | 1 | 1 |
| way 100635 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| gr 127935 | Homo sapiens (human) | IC50 | 0.0520 | 1 | 1 |
| gr 127935 | Homo sapiens (human) | Ki | 0.0034 | 5 | 5 |
| 5-methoxy 3-(1,2,3,6-tetrahydro-4-pyridinyl)1h indole | Homo sapiens (human) | IC50 | 0.0390 | 1 | 1 |
| pramipexole | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| sb 204070a | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| cp 93129 | Homo sapiens (human) | IC50 | 2.2000 | 1 | 1 |
| gr 55562 | Homo sapiens (human) | Ki | 0.7000 | 1 | 1 |
| cp 122288 | Homo sapiens (human) | IC50 | 0.0072 | 1 | 1 |
| harmalan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| n,n-di-n-propylserotonin | Homo sapiens (human) | IC50 | 0.8200 | 2 | 2 |
| piboserod | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 8-(di-n-propylamino)-6,7,8,9-tetrahydro-3h-benz(e)indole-1-carbaldehyde | Homo sapiens (human) | Ki | 0.1730 | 1 | 1 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 0.0490 | 1 | 1 |
| 1-methyl-6-methoxy-dihydro-beta-carboline | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| n-(1-methyl-5-indolyl)-n'-(3-methyl-5-isothiazolyl)urea | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| sb-224289 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| sb-224289 | Homo sapiens (human) | Ki | 0.5012 | 1 | 1 |
| harmine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| ly 344864 | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
| l 745870 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| ly 334370 | Homo sapiens (human) | Ki | 0.3323 | 3 | 3 |
| sb 258719 | Homo sapiens (human) | Ki | 3.1623 | 1 | 1 |
| sb 271046 | Homo sapiens (human) | Ki | 0.2512 | 1 | 1 |
| gr 46611 | Homo sapiens (human) | Ki | 0.0522 | 2 | 2 |
| 1-(3-(5-(1,2,4-triazol-4-yl)-1h-indol-3-yl)propyl)-4-(2-(3-fluorophenyl)ethyl)piperazine | Homo sapiens (human) | IC50 | 0.0006 | 6 | 6 |
| 8-hydroxy-2-(di-n-propylamino)tetralin, (r)-isomer | Homo sapiens (human) | Ki | 0.4010 | 2 | 2 |
| sb 269970 | Homo sapiens (human) | Ki | 5.7924 | 2 | 2 |
| 2-ethyl-5-methoxy-n,n-dimethyltryptamine | Homo sapiens (human) | IC50 | 1.4000 | 1 | 1 |
| 2-ethyl-5-methoxy-n,n-dimethyltryptamine | Homo sapiens (human) | Ki | 0.2900 | 1 | 1 |
| 5-methoxy-2-phenyl-n,n-dimethyltryptamine | Homo sapiens (human) | Ki | 6.2250 | 1 | 1 |
| ms-245 | Homo sapiens (human) | Ki | 0.7200 | 1 | 1 |
| n-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide | Homo sapiens (human) | Ki | 3.9811 | 1 | 1 |
| 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| l 772405 | Homo sapiens (human) | IC50 | 0.0382 | 4 | 4 |
| l 772405 | Homo sapiens (human) | Ki | 0.0009 | 1 | 1 |
| sb258741 | Homo sapiens (human) | Ki | 3.1623 | 1 | 1 |
| 5-chloro-2,3-dihydro-6-(4-methylpiperazin-1-yl)-1-(4-(pyridin-4-yl)naphth-1-ylaminocarbonyl)-1h-indole | Homo sapiens (human) | Ki | 0.0015 | 2 | 2 |
| vn2222 | Homo sapiens (human) | Ki | 2.6500 | 1 | 1 |
| pnu 109291 | Homo sapiens (human) | Ki | 0.0009 | 3 | 3 |
| sb-656104-a | Homo sapiens (human) | Ki | 0.0251 | 1 | 1 |
| sb-649915 | Homo sapiens (human) | Ki | 0.0016 | 5 | 5 |
| meridianin a | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| barettin | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| col-144 | Homo sapiens (human) | Ki | 0.5920 | 1 | 1 |
| td-5108 | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 2.1115 | 2 | 5 |
| tegaserod | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 8, Issue:11, 1998
Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 8, Issue:11, 1998
5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.Journal of medicinal chemistry, , Nov-21, Volume: 40, Issue:24, 1997
1-(2-Aminoethyl)-3-methyl-8,9-dihydropyrano[3,2-e]indole: a rotationally restricted phenolic analog of the neurotransmitter serotonin and agonist selective for serotonin (5-HT2-type) receptors.Journal of medicinal chemistry, , Oct-02, Volume: 35, Issue:20, 1992
Serotonin receptor binding affinities of several hallucinogenic phenylalkylamine and N,N-dimethyltryptamine analogues.Journal of medicinal chemistry, , Volume: 21, Issue:8, 1978
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.Journal of medicinal chemistry, , Volume: 33, Issue:8, 1990
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.Journal of medicinal chemistry, , Dec-02, Volume: 42, Issue:24, 1999
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 2.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.Journal of medicinal chemistry, , Volume: 33, Issue:8, 1990
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.Journal of medicinal chemistry, , Feb-11, Volume: 42, Issue:3, 1999
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
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-piperidinyl)-1H-indol-5-yl]benzamide.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
3-(2-pyrrolidin-1-ylethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity human 5-HT(1B/1D) ligands.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
Design, synthesis and biological activity of novel dimethyl-[2-[6-substituted-indol-1-yl]-ethyl]-amine as potent, selective, and orally-bioavailable 5-HT(1D) agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
(R)-3-(N-methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity h5-HT1B/1D ligands.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 13, Issue:20, 2003
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.Journal of medicinal chemistry, , Mar-01, Volume: 44, Issue:5, 2001
5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine.Bioorganic & medicinal chemistry letters, , May-01, Volume: 10, Issue:9, 2000
5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.Bioorganic & medicinal chemistry letters, , Aug-07, Volume: 10, Issue:15, 2000
Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.Journal of medicinal chemistry, , Feb-25, Volume: 42, Issue:4, 1999
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.Journal of medicinal chemistry, , Feb-25, Volume: 42, Issue:4, 1999
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.Journal of medicinal chemistry, , Dec-02, Volume: 42, Issue:24, 1999
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.Journal of medicinal chemistry, , Feb-11, Volume: 42, Issue:3, 1999
Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist.Bioorganic & medicinal chemistry letters, , Mar-17, Volume: 8, Issue:6, 1998
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Serotonin dimers: application of the bivalent ligand approach to the design of new potent and selective 5-HT(1B/1D) agonists.Journal of medicinal chemistry, , Dec-06, Volume: 39, Issue:25, 1996
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.Journal of medicinal chemistry, , Nov-22, Volume: 39, Issue:24, 1996
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist.Journal of medicinal chemistry, , Sep-02, Volume: 37, Issue:18, 1994
2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands.Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 14, Issue:18, 2004
Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands.Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 14, Issue:18, 2004
Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
A novel potential therapeutic avenue for autism: design, synthesis and pharmacophore generation of SSRIs with dual action.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 21, Issue:22, 2011
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.Bioorganic & medicinal chemistry, , Oct-01, Volume: 19, Issue:19, 2011
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.Journal of medicinal chemistry, , Mar-01, Volume: 44, Issue:5, 2001
Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist.Bioorganic & medicinal chemistry letters, , Mar-17, Volume: 8, Issue:6, 1998
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
New selective and potent 5-HT(1B/1D) antagonists: chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenylsulfonamides.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function bJournal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.Journal of medicinal chemistry, , Volume: 33, Issue:8, 1990
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.Journal of medicinal chemistry, , Volume: 33, Issue:8, 1990
New selective and potent 5-HT(1B/1D) antagonists: chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenylsulfonamides.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function bJournal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
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-piperidinyl)-1H-indol-5-yl]benzamide.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 14, Issue:24, 2004
Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
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-piperidinyl)-1H-indol-5-yl]benzamide.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.Journal of medicinal chemistry, , Feb-25, Volume: 42, Issue:4, 1999
Enhancement of oral absorption in selective 5-HT1D receptor agonists: fluorinated 3-[3-(piperidin-1-yl)propyl]indoles.Journal of medicinal chemistry, , Jul-16, Volume: 41, Issue:15, 1998
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Discovery of G Protein-Biased Antagonists against 5-HTJournal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 15, Issue:19, 2005
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Design, synthesis and biological activity of novel dimethyl-[2-[6-substituted-indol-1-yl]-ethyl]-amine as potent, selective, and orally-bioavailable 5-HT(1D) agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.Journal of medicinal chemistry, , Dec-02, Volume: 42, Issue:24, 1999
Enhancement of oral absorption in selective 5-HT1D receptor agonists: fluorinated 3-[3-(piperidin-1-yl)propyl]indoles.Journal of medicinal chemistry, , Jul-16, Volume: 41, Issue:15, 1998
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Identification of a potent and selective 5-HT1B receptor antagonist.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 15, Issue:19, 2005
Research progress in biological activities of isochroman derivatives.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
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-piperidinyl)-1H-indol-5-yl]benzamide.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.Journal of medicinal chemistry, , May-22, Volume: 51, Issue:10, 2008
Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 18, Issue:20, 2008
Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 17, Issue:18, 2007
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 17, Issue:4, 2007
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 26, Issue:3, 2016
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Enables
This protein enables 2 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled serotonin receptor activity | molecular function | Combining with the biogenic amine serotonin and transmitting the signal across the membrane by activating an associated G-protein. Serotonin (5-hydroxytryptamine) is a neurotransmitter and hormone found in vertebrates and invertebrates. [GOC:ai] |
| neurotransmitter receptor activity | molecular function | Combining with a neurotransmitter and transmitting the signal to initiate a change in cell activity. [GOC:jl, GOC:signaling] |
Located In
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
Involved In
This protein is involved in 8 target(s):
| Target | Category | Definition |
|---|
| adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| intestine smooth muscle contraction | biological process | A process in which force is generated within smooth muscle tissue, resulting in a change in muscle geometry. This process occurs in the intestine. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. The intestine is the section of the alimentary canal from the stomach to the anal canal. It includes the large intestine and small intestine. [GOC:mtg_muscle, MA:0001539, MSH:D007422] |
| regulation of locomotion | biological process | Any process that modulates the frequency, rate or extent of locomotion of a cell or organism. [GOC:ems] |
| vasoconstriction | biological process | A decrease in the diameter of blood vessels, especially arteries, due to constriction of smooth muscle cells that line the vessels, and usually causing an increase in blood pressure. [GOC:pr, ISBN:0192800752] |
| regulation of behavior | biological process | Any process that modulates the frequency, rate or extent of behavior, the internally coordinated responses (actions or inactions) of whole living organisms (individuals or groups) to internal or external stimuli. [GOC:go_curators, GOC:pr] |
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| adenylate cyclase-inhibiting serotonin receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by serotonin binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |