Proteins > 5-hydroxytryptamine receptor 1A
Page last updated: 2024-08-07 15:48:10
5-hydroxytryptamine receptor 1A
A 5-hydroxytryptamine receptor 1A that is encoded in the genome of human. [PRO:WCB, UniProtKB:P08908]
Synonyms
5-HT-1A;
5-HT1A;
G-21;
Serotonin receptor 1A
Research
Bioassay Publications (306)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 2 (0.65) | 18.7374 |
| 1990's | 42 (13.73) | 18.2507 |
| 2000's | 102 (33.33) | 29.6817 |
| 2010's | 125 (40.85) | 24.3611 |
| 2020's | 35 (11.44) | 2.80 |
Compounds (221)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 8-hydroxy-2-(di-n-propylamino)tetralin | Homo sapiens (human) | IC50 | 0.0012 | 9 | 9 |
| 8-hydroxy-2-(di-n-propylamino)tetralin | Homo sapiens (human) | Ki | 0.1603 | 46 | 46 |
| 1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | Ki | 1.0295 | 2 | 2 |
| 1-(1-naphthyl)piperazine | Homo sapiens (human) | Ki | 0.0092 | 2 | 2 |
| 1-(3-chlorophenyl)piperazine | Homo sapiens (human) | Ki | 0.0420 | 1 | 1 |
| 5-(nonyloxy)tryptamine | Homo sapiens (human) | Ki | 0.3150 | 1 | 1 |
| 5-carboxamidotryptamine | Homo sapiens (human) | Ki | 0.0004 | 4 | 4 |
| methylbufotenin | Homo sapiens (human) | IC50 | 0.0150 | 1 | 1 |
| 5-methoxytryptamine | Homo sapiens (human) | Ki | 0.0032 | 1 | 1 |
| alpha-methylserotonin | Homo sapiens (human) | IC50 | 0.0196 | 1 | 1 |
| alpha-methylserotonin | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
| alprenolol | Homo sapiens (human) | IC50 | 0.6300 | 1 | 1 |
| alprenolol | Homo sapiens (human) | Ki | 0.0216 | 1 | 1 |
| theophylline | Homo sapiens (human) | Ki | 86.0000 | 1 | 1 |
| amoxapine | Homo sapiens (human) | Ki | 0.2210 | 1 | 1 |
| bmy 7378 | Homo sapiens (human) | Ki | 0.0009 | 14 | 14 |
| buspirone | Homo sapiens (human) | IC50 | 0.0250 | 1 | 1 |
| buspirone | Homo sapiens (human) | Ki | 0.0195 | 27 | 28 |
| cgs 12066 | Homo sapiens (human) | IC50 | 0.0468 | 2 | 2 |
| chlorpromazine | Homo sapiens (human) | Ki | 0.6730 | 1 | 1 |
| cirazoline | Homo sapiens (human) | Ki | 0.0347 | 1 | 1 |
| cisapride | Homo sapiens (human) | Ki | 0.7943 | 1 | 1 |
| clonidine | Homo sapiens (human) | Ki | 3.2359 | 1 | 1 |
| ebastine | Homo sapiens (human) | IC50 | 0.0470 | 1 | 1 |
| haloperidol | Homo sapiens (human) | IC50 | 1.5000 | 1 | 1 |
| haloperidol | Homo sapiens (human) | Ki | 2.3410 | 5 | 5 |
| imipramine | Homo sapiens (human) | Ki | 3.7300 | 1 | 3 |
| ketanserin | Homo sapiens (human) | Ki | 0.0035 | 1 | 1 |
| methiothepin | Homo sapiens (human) | Ki | 0.1293 | 5 | 5 |
| mianserin | Homo sapiens (human) | IC50 | 0.3981 | 2 | 2 |
| mianserin | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
| mirtazapine | Homo sapiens (human) | Ki | 0.0180 | 2 | 2 |
| nan 190 | Homo sapiens (human) | IC50 | 0.0030 | 3 | 4 |
| nan 190 | Homo sapiens (human) | Ki | 0.0307 | 3 | 3 |
| naratriptan | Homo sapiens (human) | Ki | 0.0450 | 1 | 1 |
| ondansetron | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| pindolol | Homo sapiens (human) | Ki | 0.0594 | 4 | 4 |
| prazosin | Homo sapiens (human) | Ki | 0.9525 | 4 | 4 |
| propranolol | Homo sapiens (human) | IC50 | 3.9811 | 1 | 1 |
| quetiapine | Homo sapiens (human) | Ki | 0.2889 | 5 | 5 |
| quipazine | Homo sapiens (human) | IC50 | 1.4454 | 2 | 2 |
| risperidone | Homo sapiens (human) | Ki | 0.3184 | 8 | 8 |
| rizatriptan | Homo sapiens (human) | IC50 | 0.3572 | 2 | 2 |
| rizatriptan | Homo sapiens (human) | Ki | 0.2165 | 2 | 2 |
| ropinirole | Homo sapiens (human) | Ki | 1.7060 | 1 | 1 |
| spiperone | Homo sapiens (human) | Ki | 0.0172 | 1 | 1 |
| sumatriptan | Homo sapiens (human) | IC50 | 0.4496 | 2 | 2 |
| sumatriptan | Homo sapiens (human) | Ki | 0.3574 | 8 | 8 |
| trazodone | Homo sapiens (human) | Ki | 0.1180 | 1 | 1 |
| urapidil | Homo sapiens (human) | Ki | 0.2130 | 1 | 1 |
| n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamide | Homo sapiens (human) | IC50 | 0.0055 | 4 | 4 |
| n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamide | Homo sapiens (human) | Ki | 0.0008 | 14 | 14 |
| wb 4101 | Homo sapiens (human) | Ki | 0.0021 | 5 | 5 |
| zotepine | Homo sapiens (human) | Ki | 0.3300 | 1 | 1 |
| lysergic acid diethylamide | Homo sapiens (human) | Ki | 0.0012 | 3 | 3 |
| apomorphine | Homo sapiens (human) | Ki | 0.2512 | 4 | 4 |
| chlorpromazine hydrochloride | Homo sapiens (human) | Ki | 0.6730 | 1 | 2 |
| indopan | Homo sapiens (human) | Ki | 3.1996 | 1 | 2 |
| dibenzepin | Homo sapiens (human) | Ki | 2.5000 | 1 | 1 |
| azaperone | Homo sapiens (human) | Ki | 0.0078 | 2 | 4 |
| n-methyllaurotetanine | Homo sapiens (human) | Ki | 0.1995 | 2 | 2 |
| glaucine | Homo sapiens (human) | Ki | 0.1710 | 1 | 1 |
| canadine, (s)-isomer | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| metergoline | Homo sapiens (human) | IC50 | 0.0041 | 1 | 1 |
| metergoline | Homo sapiens (human) | Ki | 0.0076 | 2 | 2 |
| lisuride | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| lofexidine | Homo sapiens (human) | Ki | 0.1259 | 1 | 1 |
| bromocriptine | Homo sapiens (human) | Ki | 0.0240 | 1 | 1 |
| penfluridol | Homo sapiens (human) | Ki | 0.3560 | 1 | 1 |
| 5-methoxy-alpha-methyltryptamine | Homo sapiens (human) | IC50 | 0.0864 | 1 | 1 |
| 5-methoxy-alpha-methyltryptamine | Homo sapiens (human) | Ki | 0.0046 | 1 | 1 |
| pergolide | Homo sapiens (human) | Ki | 0.0040 | 1 | 1 |
| colforsin | Homo sapiens (human) | IC50 | 0.0410 | 1 | 1 |
| gepirone | Homo sapiens (human) | IC50 | 0.1140 | 1 | 1 |
| gepirone | Homo sapiens (human) | Ki | 0.0224 | 2 | 2 |
| ipsapirone | Homo sapiens (human) | Ki | 0.0160 | 4 | 4 |
| sertindole | Homo sapiens (human) | Ki | 0.0330 | 1 | 1 |
| aripiprazole | Homo sapiens (human) | Ki | 0.0093 | 15 | 16 |
| ziprasidone | Homo sapiens (human) | Ki | 0.0094 | 5 | 5 |
| zolmitriptan | Homo sapiens (human) | Ki | 0.1013 | 2 | 2 |
| tasosartan | Homo sapiens (human) | IC50 | 0.0320 | 1 | 1 |
| mezilamine | Homo sapiens (human) | Ki | 0.4300 | 1 | 1 |
| tetrahydropalmatine | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| frovatriptan | Homo sapiens (human) | Ki | 0.0620 | 1 | 1 |
| tandospirone | Homo sapiens (human) | Ki | 0.0189 | 2 | 2 |
| way 100635 | Homo sapiens (human) | IC50 | 0.0108 | 6 | 6 |
| way 100635 | Homo sapiens (human) | Ki | 0.0006 | 7 | 8 |
| gr 127935 | Homo sapiens (human) | Ki | 0.0750 | 2 | 2 |
| pramipexole | Homo sapiens (human) | Ki | 6.5140 | 1 | 1 |
| uh 301 | Homo sapiens (human) | Ki | 0.0870 | 1 | 1 |
| 2-chloro-n(6)cyclopentyladenosine | Homo sapiens (human) | Ki | 0.7960 | 1 | 1 |
| ly 206130 | Homo sapiens (human) | Ki | 0.0067 | 2 | 2 |
| 11-hydroxy-n-(n-propyl)noraporphine | Homo sapiens (human) | Ki | 0.0660 | 1 | 1 |
| gr 55562 | Homo sapiens (human) | Ki | 0.8420 | 1 | 1 |
| tamsulosin | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
| l 694247 | Homo sapiens (human) | IC50 | 0.0032 | 1 | 1 |
| cyclazosin | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| 4-(benzodioxan-5-yl)-1-(indan-2-yl)piperazine | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
| u 93385 | Homo sapiens (human) | Ki | 0.0150 | 1 | 2 |
| u-91356 | Homo sapiens (human) | Ki | 0.0580 | 1 | 1 |
| sonepiprazole | Homo sapiens (human) | Ki | 1.6000 | 1 | 1 |
| sk&f 83959 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| l 741626 | Homo sapiens (human) | Ki | 6.3000 | 1 | 1 |
| rec 15-2739 | Homo sapiens (human) | Ki | 0.0059 | 1 | 1 |
| Serotonin hydrochloride | Homo sapiens (human) | Ki | 0.0100 | 1 | 1 |
| harmalan | Homo sapiens (human) | Ki | 1.6700 | 1 | 1 |
| corydalmine | Homo sapiens (human) | Ki | 0.1490 | 1 | 1 |
| 8-gingerol | Homo sapiens (human) | Ki | 11.7100 | 1 | 1 |
| 10-gingerol | Homo sapiens (human) | Ki | 3.7400 | 1 | 1 |
| n-demethyllysergic acid diethylamide | Homo sapiens (human) | IC50 | 0.0030 | 1 | 1 |
| 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) | IC50 | 0.0012 | 1 | 1 |
| 8-(di-n-propylamino)-6,7,8,9-tetrahydro-3h-benz(e)indole-1-carbaldehyde | Homo sapiens (human) | Ki | 0.0012 | 1 | 1 |
| sunepitron | Homo sapiens (human) | Ki | 0.0920 | 1 | 1 |
| ngd 94-1 | Homo sapiens (human) | Ki | 0.1805 | 2 | 2 |
| latrepirdine | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
| eptapirone | Homo sapiens (human) | Ki | 0.1750 | 1 | 1 |
| bifeprunox | Homo sapiens (human) | Ki | 0.0086 | 3 | 3 |
| bmy 7378 | Homo sapiens (human) | Ki | 0.0017 | 2 | 2 |
| lurasidone | Homo sapiens (human) | Ki | 0.0067 | 1 | 1 |
| sorafenib | Homo sapiens (human) | Ki | 1.1810 | 1 | 1 |
| regadenoson | Homo sapiens (human) | Ki | 1,269.0000 | 1 | 1 |
| roxindole | Homo sapiens (human) | IC50 | 0.0008 | 1 | 1 |
| sorbinil | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| 1-methyl-6-methoxy-dihydro-beta-carboline | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 5-hydroxytryptophan | Homo sapiens (human) | Ki | 0.0014 | 2 | 2 |
| gingerol | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| sb 243213 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| tropisetron | Homo sapiens (human) | Ki | 0.0053 | 1 | 1 |
| n(6)-cyclopentyladenosine | Homo sapiens (human) | Ki | 0.6150 | 1 | 1 |
| (S)-(-)-pindolol | Homo sapiens (human) | Ki | 0.1100 | 1 | 1 |
| 3,4,5-trimethoxycinnamic acid | Homo sapiens (human) | IC50 | 7.6000 | 2 | 2 |
| altanserin | Homo sapiens (human) | Ki | 1.5700 | 1 | 1 |
| mitragynine | Homo sapiens (human) | Ki | 5.8800 | 1 | 1 |
| 2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide | Homo sapiens (human) | Ki | 0.0600 | 1 | 1 |
| paynantheine | Homo sapiens (human) | Ki | 0.0519 | 2 | 2 |
| bp 897 | Homo sapiens (human) | Ki | 0.1120 | 3 | 3 |
| sb-224289 | Homo sapiens (human) | Ki | 3.1623 | 1 | 1 |
| mm 77 | Homo sapiens (human) | Ki | 0.0064 | 1 | 1 |
| abt724 | Homo sapiens (human) | Ki | 1,395.0000 | 1 | 2 |
| harmine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| methysergide maleate | Homo sapiens (human) | Ki | 0.0170 | 1 | 1 |
| shogaol | Homo sapiens (human) | Ki | 18.0200 | 1 | 1 |
| ly 344864 | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
| l 745870 | Homo sapiens (human) | Ki | 7.2104 | 2 | 2 |
| ly 334370 | Homo sapiens (human) | Ki | 0.0220 | 3 | 3 |
| mdl 100907 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| sb 258719 | Homo sapiens (human) | Ki | 6.2954 | 3 | 3 |
| sb 271046 | Homo sapiens (human) | Ki | 0.3691 | 2 | 2 |
| gr 46611 | Homo sapiens (human) | Ki | 0.0013 | 1 | 1 |
| (8)-shogaol | Homo sapiens (human) | Ki | 13.0500 | 1 | 1 |
| (10)-shogaol | Homo sapiens (human) | Ki | 5.8400 | 1 | 1 |
| kf 17837 | Homo sapiens (human) | Ki | 0.4300 | 1 | 1 |
| 8-hydroxy-2-(di-n-propylamino)tetralin, (r)-isomer | Homo sapiens (human) | Ki | 0.0042 | 2 | 2 |
| sb 269970 | Homo sapiens (human) | Ki | 8.2077 | 10 | 10 |
| stepholidine | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| flibanserin | Homo sapiens (human) | Ki | 0.0118 | 1 | 1 |
| vilazodone | Homo sapiens (human) | IC50 | 0.0002 | 2 | 2 |
| vilazodone | Homo sapiens (human) | Ki | 0.0096 | 4 | 4 |
| sarizotan | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
| 2-ethyl-5-methoxy-n,n-dimethyltryptamine | Homo sapiens (human) | Ki | 0.1700 | 1 | 1 |
| 5-methoxy-2-phenyl-n,n-dimethyltryptamine | Homo sapiens (human) | Ki | 1.4700 | 1 | 1 |
| ms-245 | Homo sapiens (human) | Ki | 0.9010 | 2 | 2 |
| n-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide | Homo sapiens (human) | Ki | 6.3096 | 1 | 1 |
| pnu-95666 | Homo sapiens (human) | Ki | 0.0730 | 1 | 1 |
| cp 293019 | Homo sapiens (human) | Ki | 0.1800 | 1 | 1 |
| n-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide | Homo sapiens (human) | Ki | 0.0234 | 1 | 1 |
| 4-iodo-2,5-dimethoxyphenylisopropylamine, (r)-isomer | Homo sapiens (human) | IC50 | 3.8430 | 1 | 1 |
| 4-iodo-2,5-dimethoxyphenylisopropylamine, (r)-isomer | Homo sapiens (human) | Ki | 0.0006 | 1 | 1 |
| l 772405 | Homo sapiens (human) | IC50 | 0.0660 | 1 | 1 |
| s 21007 | Homo sapiens (human) | IC50 | 0.3981 | 2 | 2 |
| sb258741 | Homo sapiens (human) | Ki | 1.0000 | 2 | 2 |
| f 13640 | Homo sapiens (human) | Ki | 0.0010 | 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 | 0.0070 | 2 | 2 |
| vn2222 | Homo sapiens (human) | Ki | 0.0200 | 2 | 2 |
| slv 313 | Homo sapiens (human) | Ki | 0.0047 | 2 | 2 |
| fauc 346 | Homo sapiens (human) | Ki | 0.0410 | 1 | 1 |
| ngb 2904 | Homo sapiens (human) | Ki | 2.0400 | 1 | 1 |
| 4-(3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl)-1-(4-fluorophenyl)butan-1-one | Homo sapiens (human) | Ki | 0.7895 | 2 | 4 |
| pnu 109291 | Homo sapiens (human) | Ki | 1.0920 | 2 | 2 |
| pnu 96415e | Homo sapiens (human) | Ki | 0.1340 | 1 | 1 |
| n-(4-((4-(dimethylamino)quinazolin-2-yl)amino)cyclohexyl)-3,4-difluorobenzamide hydrochloride | Homo sapiens (human) | IC50 | 0.0169 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 0.2800 | 1 | 1 |
| vortioxetine | Homo sapiens (human) | Ki | 0.0106 | 5 | 5 |
| sb-656104-a | Homo sapiens (human) | Ki | 0.4062 | 2 | 2 |
| lecozotan | Homo sapiens (human) | IC50 | 0.0335 | 2 | 2 |
| lecozotan | Homo sapiens (human) | Ki | 0.0016 | 1 | 1 |
| vuf 8504 | Homo sapiens (human) | Ki | 17.0000 | 1 | 1 |
| fauc 365 | Homo sapiens (human) | Ki | 0.3195 | 4 | 4 |
| sb-649915 | Homo sapiens (human) | Ki | 0.0015 | 9 | 9 |
| 11-hydroxy-n-(n-propyl)noraporphine hydrochloride, (r)-isomer | Homo sapiens (human) | Ki | 0.0450 | 1 | 1 |
| fauc 113 | Homo sapiens (human) | Ki | 1.4000 | 1 | 1 |
| meridianin a | Homo sapiens (human) | Ki | 0.6840 | 1 | 1 |
| cariprazine | Homo sapiens (human) | Ki | 0.0032 | 5 | 6 |
| barettin | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| naphyrone | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sb 742457 | Homo sapiens (human) | Ki | 1.5887 | 3 | 3 |
| naluzotan | Homo sapiens (human) | Ki | 0.0051 | 1 | 1 |
| pg 01037 | Homo sapiens (human) | Ki | 0.0854 | 1 | 1 |
| col-144 | Homo sapiens (human) | Ki | 0.5900 | 1 | 1 |
| brexpiprazole | Homo sapiens (human) | Ki | 0.0001 | 2 | 2 |
| 4-(4-chlorophenyl)sulfonyl-5-(3,4-dihydro-1H-isoquinolin-2-yl)-2-ethylsulfonylthiazole | Homo sapiens (human) | Ki | 12.2000 | 1 | 1 |
| mitragynine | Homo sapiens (human) | Ki | 0.0670 | 2 | 2 |
| a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| lu ae58054 | Homo sapiens (human) | Ki | 3.9360 | 1 | 1 |
| lu aa33810 | Homo sapiens (human) | Ki | 0.4780 | 1 | 1 |
| e-55888 | Homo sapiens (human) | Ki | 0.7000 | 2 | 2 |
| 2-(1-(2-allylphenoxy)ethyl)-4,5-dihydro-1h-imidazole | Homo sapiens (human) | Ki | 0.0282 | 2 | 2 |
| n-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide | Homo sapiens (human) | Ki | 0.2699 | 7 | 7 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 2.0775 | 2 | 5 |
| clozapine | Homo sapiens (human) | IC50 | 0.1500 | 1 | 1 |
| clozapine | Homo sapiens (human) | Ki | 0.1657 | 15 | 18 |
| olanzapine | Homo sapiens (human) | Ki | 3.0734 | 7 | 7 |
| aplysinopsin | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Activity of Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
[no title available]Bioorganic & medicinal chemistry letters, , 08-15, Volume: 30, Issue:16, 2020
Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HTBioorganic & medicinal chemistry, , 08-01, Volume: 28, Issue:15, 2020
[no title available]Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Identification of C10 nitrogen-containing aporphines with dopamine DBioorganic & medicinal chemistry letters, , 04-15, Volume: 30, Issue:8, 2020
[no title available]European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
[1]Benzothieno[3,2-d]pyrimidine derivatives as ligands for the serotonergic 5-HTEuropean journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
[no title available]Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
[no title available]European journal of medicinal chemistry, , Aug-15, Volume: 176, 2019
Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 29, Issue:21, 2019
New N- and O-arylpiperazinylalkyl pyrimidines and 2-methylquinazolines derivatives as 5-HTBioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Design and synthesis of new homo and hetero bis-piperazinyl-1-propanone derivatives as 5-HT7R selective ligands over 5-HT1AR.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 26, Issue:16, 2016
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
Synthesis and binding properties of new long-chain 4-substituted piperazine derivatives as 5-HT₁A and 5-HT₇ receptor ligands.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 25, Issue:7, 2015
Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment of β-arrestin-2.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.Journal of natural products, , Apr-24, Volume: 78, Issue:4, 2015
Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.ACS medicinal chemistry letters, , Sep-12, Volume: 4, Issue:9, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition.Journal of medicinal chemistry, , Jan-24, Volume: 56, Issue:2, 2013
Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT₁A/5-HT₂A/5-HT₇ and dopamine D₂/D₃ receptors.European journal of medicinal chemistry, , Volume: 60, 2013
Synthesis, docking and pharmacological evaluation of novel homo- and hetero-bis 3-piperazinylpropylindole derivatives at SERT and 5-HT1A receptor.Bioorganic & medicinal chemistry, , Dec-15, Volume: 21, Issue:24, 2013
New serotonin 5-HT1A receptor agonists endowed with antinociceptive activity in vivo.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.ACS medicinal chemistry letters, , Jul-12, Volume: 3, Issue:7, 2012
Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors.Journal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
Novel benzo[b]thiophene derivatives as new potential antidepressants with rapid onset of action.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Discovery of a new series of 5-HT1A receptor agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 20, Issue:6, 2010
Synthesis of dihydrofuroaporphine derivatives: identification of a potent and selective serotonin 5-HT 1A receptor agonist.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
N-[omega-[4-(2-methoxyphenyl)-1-piperazinyl]alkyl]-2-quinolinamines as high-affinity fluorescent 5-HT1A receptor ligands.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.Journal of medicinal chemistry, , May-22, Volume: 51, Issue:10, 2008
2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties.Journal of medicinal chemistry, , Dec-11, Volume: 51, Issue:23, 2008
Advances toward new antidepressants with dual serotonin transporter and 5-HT1A receptor affinity within a class of 3-aminochroman derivatives. Part 2.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
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Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.Journal of medicinal chemistry, , Oct-04, Volume: 50, Issue:20, 2007
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor.Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.Journal of medicinal chemistry, , Dec-06, Volume: 44, Issue:25, 2001
Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists.Journal of medicinal chemistry, , Jul-19, Volume: 44, Issue:15, 2001
A novel fluorinated tryptamine with highly potent serotonin 5-HT1A receptor agonist properties.Bioorganic & medicinal chemistry letters, , Mar-26, Volume: 11, Issue:6, 2001
Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines.Journal of medicinal chemistry, , Nov-30, Volume: 43, Issue:24, 2000
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 8, Issue:11, 1998
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability.Journal of medicinal chemistry, , Jul-23, Volume: 36, Issue:15, 1993
Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
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
[no title available]European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Physical binding pocket induction for affinity prediction.Journal of medicinal chemistry, , Oct-08, Volume: 52, Issue:19, 2009
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A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
Synthesis and serotonergic pharmacology of the enantiomers of 3-[(N-methylpyrrolidin-2-yl)methyl]-5-methoxy-1H-indole: discovery of stereogenic differentiation in the aminoethyl side chain of the neurotransmitter serotonin.Journal of medicinal chemistry, , Nov-13, Volume: 35, Issue:23, 1992
Serotonin receptor binding affinities of several hallucinogenic phenylalkylamine and N,N-dimethyltryptamine analogues.Journal of medicinal chemistry, , Volume: 21, Issue:8, 1978
[no title available]European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
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Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors.Journal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
Discovery of a new series of 5-HT1A receptor agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 20, Issue:6, 2010
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
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1,2,4-Benzothiadiazine derivatives as alpha1 and 5-HT1A receptor ligands.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor.Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
Structure-activity relationships in 1,4-benzodioxan-related compounds. 7. Selectivity of 4-phenylchroman analogues for alpha(1)-adrenoreceptor subtypes.Journal of medicinal chemistry, , Apr-11, Volume: 45, Issue:8, 2002
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Design, synthesis, and biological activity of prazosin-related antagonists. Role of the piperazine and furan units of prazosin on the selectivity for alpha1-adrenoreceptor subtypes.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
Design, synthesis, and behavioral evaluation of dual-acting compounds as phosphodiesterase type 10A (PDE10A) inhibitors and serotonin ligands targeting neuropsychiatric symptoms in dementia.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
Synthesis of novel 5-substituted-2-aminotetralin analogs: 5-HTBioorganic & medicinal chemistry, , 02-01, Volume: 28, Issue:3, 2020
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
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Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HTEuropean journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
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2-Aminoimidazole-based antagonists of the 5-HTEuropean journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 29, Issue:21, 2019
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[no title available]European journal of medicinal chemistry, , May-15, Volume: 170, 2019
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
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Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HTEuropean journal of medicinal chemistry, , Mar-10, Volume: 147, 2018
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Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation.European journal of medicinal chemistry, , Apr-13, Volume: 112, 2016
Synthesis and evaluation of antidepressant-like activity of some 4-substituted 1-(2-methoxyphenyl)piperazine derivatives.Chemical biology & drug design, , Volume: 85, Issue:3, 2015
SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT(7) receptor ligands among phenylpiperazine hydantoin derivatives.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Synthesis of dihydrofuroaporphine derivatives: identification of a potent and selective serotonin 5-HT 1A receptor agonist.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Physical binding pocket induction for affinity prediction.Journal of medicinal chemistry, , Oct-08, Volume: 52, Issue:19, 2009
Synthesis and pharmacological evaluation of aminopyrimidine series of 5-HT1A partial agonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 19, Issue:4, 2009
Arylpiperazines with N-acylated amino acids as 5-HT1A receptor ligands.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.Journal of medicinal chemistry, , Jun-01, Volume: 49, Issue:11, 2006
The design and preparation of metabolically protected new arylpiperazine 5-HT1A ligands.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
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New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.Bioorganic & medicinal chemistry letters, , Sep-03, Volume: 11, Issue:17, 2001
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
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Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HTEuropean journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
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[no title available]Bioorganic & medicinal chemistry letters, , 11-01, Volume: 26, Issue:21, 2016
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
Physical binding pocket induction for affinity prediction.Journal of medicinal chemistry, , Oct-08, Volume: 52, Issue:19, 2009
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
Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 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 1.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
Design, synthesis and evaluation of activity and pharmacokinetic profile of new derivatives of xanthone and piperazine in the central nervous system.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 29, Issue:21, 2019
Physical binding pocket induction for affinity prediction.Journal of medicinal chemistry, , Oct-08, Volume: 52, Issue:19, 2009
Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
[no title available]European journal of medicinal chemistry, , Sep-01, Volume: 201, 2020
Privileged scaffold-based design to identify a novel drug-like 5-HTEuropean journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability.Bioorganic & medicinal chemistry, , 09-15, Volume: 27, Issue:18, 2019
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Synthesis of a new series of aryl/heteroarylpiperazinyl derivatives of 8-acetyl-7-hydroxy-4-methylcoumarin with low nanomolar 5-HTEuropean journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
Structure-activity relationships and molecular modeling studies of novel arylpiperazinylalkyl 2-benzoxazolones and 2-benzothiazolones as 5-HT(7) and 5-HT(1A) receptor ligands.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Synthesis and characterization of environment-sensitive fluorescent ligands for human 5-HT1A receptors with 1-arylpiperazine structure.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Novel DEuropean journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
Physical binding pocket induction for affinity prediction.Journal of medicinal chemistry, , Oct-08, Volume: 52, Issue:19, 2009
Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 2007
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 1999
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists.Journal of medicinal chemistry, , Jul-19, Volume: 44, Issue:15, 2001
Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 8, Issue:11, 1998
Design, synthesis, and biological activity of prazosin-related antagonists. Role of the piperazine and furan units of prazosin on the selectivity for alpha1-adrenoreceptor subtypes.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile.Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Physical binding pocket induction for affinity prediction.Journal of medicinal chemistry, , Oct-08, Volume: 52, Issue:19, 2009
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 30, Issue:20, 2020
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.Bioorganic & medicinal chemistry, , 09-01, Volume: 25, Issue:17, 2017
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Physical binding pocket induction for affinity prediction.Journal of medicinal chemistry, , Oct-08, Volume: 52, Issue:19, 2009
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.Bioorganic & medicinal chemistry letters, , Sep-03, Volume: 11, Issue:17, 2001
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.Journal of medicinal chemistry, , Feb-11, Volume: 42, Issue:3, 1999
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
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Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
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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
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
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
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Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 17, Issue:18, 2007
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 2005
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
[no title available]European journal of medicinal chemistry, , May-05, Volume: 235, 2022
2-Phenylcyclopropylmethylamine Derivatives as Dopamine DJournal of medicinal chemistry, , 12-09, Volume: 64, Issue:23, 2021
[no title available]Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.Journal of medicinal chemistry, , Oct-04, Volume: 50, Issue:20, 2007
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.Journal of medicinal chemistry, , Jun-01, Volume: 49, Issue:11, 2006
Activity of Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.ACS medicinal chemistry letters, , Sep-12, Volume: 4, Issue:9, 2013
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.ACS medicinal chemistry letters, , Jul-12, Volume: 3, Issue:7, 2012
Search for a 5-CT alternative. MedChemComm, , Nov-01, Volume: 9, Issue:11, 2018
Structural modifications of the serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-biphenyl)-1-piperazinehexanamide (LP-211) to improve in vitro microsomal stability: A case study.European journal of medicinal chemistry, , Sep-14, Volume: 120, 2016
Design, synthesis, radiolabeling and in vivo evaluation of potential positron emission tomography (PET) radioligands for brain imaging of the 5-HT₇ receptor.Bioorganic & medicinal chemistry, , Mar-01, Volume: 22, Issue:5, 2014
Solid-supported synthesis, molecular modeling, and biological activity of long-chain arylpiperazine derivatives with cyclic amino acid amide fragments as 5-HT(7) and 5-HT(1A) receptor ligands.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
Novel highly potent serotonin 5-HT7 receptor ligands: structural modifications to improve pharmacokinetic properties.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 23, Issue:22, 2013
The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists.European journal of medicinal chemistry, , Volume: 56, 2012
Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
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
Novel DEuropean journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile.Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
Synthesis and evaluation of antidepressant-like activity of some 4-substituted 1-(2-methoxyphenyl)piperazine derivatives.Chemical biology & drug design, , Volume: 85, Issue:3, 2015
Solid-Supported Synthesis and 5-HT7 /5-HT1A Receptor Affinity of Arylpiperazinylbutyl Derivatives of 4,5-dihydro-1,2,4-triazine-6-(1H)-one.Chemical biology & drug design, , Volume: 86, Issue:4, 2015
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists.European journal of medicinal chemistry, , Volume: 56, 2012
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.Bioorganic & medicinal chemistry letters, , Sep-03, Volume: 11, Issue:17, 2001
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Further evaluation of the tropane analogs of haloperidol.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists.European journal of medicinal chemistry, , Volume: 56, 2012
Physical binding pocket induction for affinity prediction.Journal of medicinal chemistry, , Oct-08, Volume: 52, Issue:19, 2009
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Enables
This protein enables 5 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] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| receptor-receptor interaction | molecular function | The aggregation, arrangement and bonding together of two or more different receptor complexes that individually undergo combination with a hormone, neurotransmitter, drug or intracellular messenger to form a higher level receptor complex. The formation of the higher level complex initiates a change in cell function. [GOC:dox, GOC:pad, GOC:PARL, PMID:22035699, PMID:24157794] |
| neurotransmitter receptor activity | molecular function | Combining with a neurotransmitter and transmitting the signal to initiate a change in cell activity. [GOC:jl, GOC:signaling] |
| serotonin binding | molecular function | Binding to serotonin (5-hydroxytryptamine), a monoamine neurotransmitter occurring in the peripheral and central nervous systems, also having hormonal properties. [GOC:ai] |
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 15 target(s):
| Target | Category | Definition |
|---|
| behavioral fear response | biological process | An acute behavioral change resulting from a perceived external threat. [GOC:dph, PMID:9920659] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| 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] |
| serotonin receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a serotonin receptor binding to one of its physiological ligands. [GOC:mah] |
| gamma-aminobutyric acid signaling pathway | biological process | The series of molecular signals generated by the binding of gamma-aminobutyric acid (GABA, 4-aminobutyrate), an amino acid which acts as a neurotransmitter in some organisms, to its receptor on the surface of a target cell. [GOC:mah] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| regulation of serotonin secretion | biological process | Any process that modulates the frequency, rate or extent of the regulated release of serotonin. [GOC:ef] |
| regulation of vasoconstriction | biological process | Any process that modulates the frequency, rate or extent of reductions in the diameter of blood vessels. [GOC:jl] |
| exploration behavior | biological process | The specific behavior of an organism in response to a novel environment or stimulus. [GOC:BHF, GOC:pr, PMID:11682103, PMID:9767169] |
| regulation of dopamine metabolic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways involving dopamine. [GOC:go_curators] |
| serotonin metabolic process | biological process | The chemical reactions and pathways involving serotonin (5-hydroxytryptamine), a monoamine neurotransmitter occurring in the peripheral and central nervous systems, also having hormonal properties. [GOC:jl, ISBN:0198506732] |
| regulation of hormone secretion | biological process | Any process that modulates the frequency, rate or extent of the regulated release of a hormone from a cell. [GOC:ai] |
| 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] |