Page last updated: 2024-08-07 16:34:37
D(3) dopamine receptor
A D(3) dopamine receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P35462]
Synonyms
Dopamine D3 receptor
Research
Bioassay Publications (272)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 4 (1.47) | 18.7374 |
| 1990's | 44 (16.18) | 18.2507 |
| 2000's | 104 (38.24) | 29.6817 |
| 2010's | 99 (36.40) | 24.3611 |
| 2020's | 21 (7.72) | 2.80 |
Compounds (248)
Drugs with Potency Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| l 741626 | Homo sapiens (human) | Potency | 0.0646 | 1 | 0 |
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| quinacrine | Homo sapiens (human) | IC50 | 1.3180 | 1 | 0 |
| quinacrine | Homo sapiens (human) | Ki | 0.4480 | 1 | 0 |
| 7-hydroxy-2-n,n-dipropylaminotetralin | Homo sapiens (human) | Ki | 0.2403 | 7 | 7 |
| 2-(n-phenethyl-n-propyl)amino-5-hydroxytetralin | Homo sapiens (human) | Ki | 0.0034 | 1 | 1 |
| 1-(2-methoxyphenyl)piperazine | Homo sapiens (human) | Ki | 2.2620 | 1 | 1 |
| 3-[(4-chlorophenyl)-phenylmethoxy]-8-methyl-8-azabicyclo[3.2.1]octane | Homo sapiens (human) | Ki | 5.3800 | 1 | 1 |
| amifostine anhydrous | Homo sapiens (human) | IC50 | 1.9290 | 1 | 0 |
| amifostine anhydrous | Homo sapiens (human) | Ki | 0.6550 | 1 | 0 |
| amiodarone | Homo sapiens (human) | IC50 | 1.2080 | 1 | 0 |
| amiodarone | Homo sapiens (human) | Ki | 0.4100 | 1 | 0 |
| dan 2163 | Homo sapiens (human) | Ki | 0.0037 | 2 | 2 |
| amitriptyline | Homo sapiens (human) | IC50 | 0.1820 | 1 | 0 |
| amitriptyline | Homo sapiens (human) | Ki | 0.1340 | 2 | 1 |
| amoxapine | Homo sapiens (human) | IC50 | 0.1340 | 1 | 0 |
| amoxapine | Homo sapiens (human) | Ki | 0.0460 | 1 | 0 |
| astemizole | Homo sapiens (human) | IC50 | 0.4360 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 0.1480 | 1 | 0 |
| bithionol | Homo sapiens (human) | IC50 | 4.2180 | 1 | 0 |
| bithionol | Homo sapiens (human) | Ki | 1.4330 | 1 | 0 |
| buspirone | Homo sapiens (human) | IC50 | 0.0440 | 1 | 0 |
| buspirone | Homo sapiens (human) | Ki | 0.0150 | 1 | 0 |
| verapamil | Homo sapiens (human) | IC50 | 0.1860 | 1 | 0 |
| verapamil | Homo sapiens (human) | Ki | 0.0630 | 1 | 0 |
| carvedilol | Homo sapiens (human) | IC50 | 0.5770 | 1 | 0 |
| carvedilol | Homo sapiens (human) | Ki | 0.1960 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | IC50 | 0.0120 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | Ki | 0.0059 | 8 | 9 |
| ciglitazone | Homo sapiens (human) | IC50 | 26.7040 | 1 | 0 |
| ciglitazone | Homo sapiens (human) | Ki | 9.0690 | 1 | 0 |
| cisapride | Homo sapiens (human) | IC50 | 0.1440 | 1 | 0 |
| cisapride | Homo sapiens (human) | Ki | 0.0490 | 1 | 0 |
| clebopride | Homo sapiens (human) | Ki | 0.0902 | 2 | 2 |
| clomipramine | Homo sapiens (human) | IC50 | 0.1390 | 1 | 0 |
| clomipramine | Homo sapiens (human) | Ki | 0.0470 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | IC50 | 2.6470 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 0.8990 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | IC50 | 0.0480 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | Ki | 0.0160 | 1 | 0 |
| dicyclomine | Homo sapiens (human) | IC50 | 1.2100 | 1 | 0 |
| dicyclomine | Homo sapiens (human) | Ki | 0.4110 | 1 | 0 |
| diphenidol | Homo sapiens (human) | IC50 | 2.3110 | 1 | 0 |
| diphenidol | Homo sapiens (human) | Ki | 0.7850 | 1 | 0 |
| disulfiram | Homo sapiens (human) | IC50 | 1.0840 | 1 | 0 |
| disulfiram | Homo sapiens (human) | Ki | 0.3680 | 1 | 0 |
| domperidone | Homo sapiens (human) | IC50 | 0.0180 | 1 | 0 |
| domperidone | Homo sapiens (human) | Ki | 0.0049 | 2 | 1 |
| doxepin | Homo sapiens (human) | IC50 | 1.3930 | 1 | 0 |
| doxepin | Homo sapiens (human) | Ki | 0.4730 | 1 | 0 |
| droperidol | Homo sapiens (human) | IC50 | 0.0028 | 1 | 0 |
| droperidol | Homo sapiens (human) | Ki | 0.0009 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 0.1216 | 1 | 0 |
| ebastine | Homo sapiens (human) | Ki | 0.0413 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 4.7560 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 1.6150 | 1 | 0 |
| fenofibrate | Homo sapiens (human) | IC50 | 137.5330 | 1 | 0 |
| fenofibrate | Homo sapiens (human) | Ki | 46.7090 | 1 | 0 |
| fentanyl | Homo sapiens (human) | Ki | 26.2000 | 1 | 1 |
| fluphenazine | Homo sapiens (human) | IC50 | 0.0006 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 0.0017 | 2 | 1 |
| formoterol fumarate | Homo sapiens (human) | Ki | 1.6260 | 1 | 1 |
| haloperidol | Homo sapiens (human) | IC50 | 0.0065 | 6 | 5 |
| haloperidol | Homo sapiens (human) | Ki | 0.0099 | 48 | 49 |
| haloprogin | Homo sapiens (human) | IC50 | 0.4880 | 1 | 0 |
| haloprogin | Homo sapiens (human) | Ki | 0.1660 | 1 | 0 |
| hypericin | Homo sapiens (human) | Ki | 0.0345 | 1 | 1 |
| isoproterenol | Homo sapiens (human) | Ki | 4.7000 | 1 | 1 |
| ketotifen | Homo sapiens (human) | IC50 | 1.9630 | 1 | 0 |
| ketotifen | Homo sapiens (human) | Ki | 0.6670 | 1 | 0 |
| loperamide | Homo sapiens (human) | IC50 | 1.3370 | 1 | 0 |
| loperamide | Homo sapiens (human) | Ki | 1.1970 | 2 | 1 |
| loxapine | Homo sapiens (human) | IC50 | 0.0220 | 1 | 1 |
| maprotiline | Homo sapiens (human) | IC50 | 0.6450 | 1 | 0 |
| maprotiline | Homo sapiens (human) | Ki | 0.3615 | 2 | 1 |
| methadone | Homo sapiens (human) | Ki | 2.1100 | 1 | 1 |
| metoclopramide | Homo sapiens (human) | IC50 | 0.2000 | 1 | 0 |
| metoclopramide | Homo sapiens (human) | Ki | 0.0475 | 2 | 1 |
| mianserin | Homo sapiens (human) | IC50 | 3.8904 | 2 | 2 |
| mianserin | Homo sapiens (human) | Ki | 2.8410 | 1 | 1 |
| miconazole | Homo sapiens (human) | IC50 | 3.1990 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 1.0860 | 1 | 0 |
| mirtazapine | Homo sapiens (human) | Ki | 2.8715 | 2 | 2 |
| modafinil | Homo sapiens (human) | Ki | 39.0000 | 1 | 1 |
| nemonapride | Homo sapiens (human) | Ki | 0.0010 | 2 | 2 |
| nortriptyline | Homo sapiens (human) | IC50 | 0.1790 | 1 | 0 |
| nortriptyline | Homo sapiens (human) | Ki | 0.0610 | 1 | 0 |
| oxatomide | Homo sapiens (human) | Ki | 0.0627 | 1 | 1 |
| oxybutynin | Homo sapiens (human) | IC50 | 0.4288 | 1 | 0 |
| oxybutynin | Homo sapiens (human) | Ki | 0.1456 | 1 | 0 |
| pentamidine | Homo sapiens (human) | IC50 | 3.9980 | 1 | 0 |
| pentamidine | Homo sapiens (human) | Ki | 1.3580 | 1 | 0 |
| prazosin | Homo sapiens (human) | Ki | 7.1000 | 1 | 1 |
| prochlorperazine | Homo sapiens (human) | IC50 | 0.0130 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | Ki | 0.0045 | 1 | 0 |
| promazine | Homo sapiens (human) | IC50 | 0.2050 | 1 | 0 |
| promazine | Homo sapiens (human) | Ki | 0.0690 | 1 | 0 |
| promethazine | Homo sapiens (human) | IC50 | 0.5590 | 1 | 0 |
| promethazine | Homo sapiens (human) | Ki | 0.1900 | 1 | 0 |
| quetiapine | Homo sapiens (human) | IC50 | 1.1632 | 1 | 0 |
| quetiapine | Homo sapiens (human) | Ki | 0.3913 | 5 | 4 |
| 7-chloro-3-methyl-1-phenyl-1,2,4,5-tetrahydro-3-benzazepin-8-ol | Homo sapiens (human) | Ki | 0.0017 | 1 | 1 |
| rabeprazole | Homo sapiens (human) | IC50 | 2.3260 | 1 | 0 |
| rabeprazole | Homo sapiens (human) | Ki | 0.7900 | 1 | 0 |
| raloxifene | Homo sapiens (human) | IC50 | 1.5650 | 1 | 0 |
| raloxifene | Homo sapiens (human) | Ki | 0.5310 | 1 | 0 |
| rbi 257 | Homo sapiens (human) | Ki | 0.1450 | 1 | 1 |
| risperidone | Homo sapiens (human) | IC50 | 0.0240 | 1 | 0 |
| risperidone | Homo sapiens (human) | Ki | 0.0132 | 11 | 10 |
| ropinirole | Homo sapiens (human) | Ki | 0.0388 | 3 | 3 |
| 3-(3-cyanophenyl)-n-n-propylpiperidine | Homo sapiens (human) | Ki | 0.6410 | 2 | 3 |
| salmeterol xinafoate | Homo sapiens (human) | Ki | 1.0490 | 1 | 1 |
| sb 206553 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| spiperone | Homo sapiens (human) | IC50 | 0.0635 | 3 | 3 |
| spiperone | Homo sapiens (human) | Ki | 0.0005 | 9 | 10 |
| sulconazole | Homo sapiens (human) | IC50 | 3.1040 | 1 | 0 |
| sulconazole | Homo sapiens (human) | Ki | 1.0540 | 1 | 0 |
| sulpiride | Homo sapiens (human) | IC50 | 0.2651 | 3 | 2 |
| sulpiride | Homo sapiens (human) | Ki | 0.0617 | 3 | 2 |
| terfenadine | Homo sapiens (human) | IC50 | 1.5030 | 1 | 0 |
| terfenadine | Homo sapiens (human) | Ki | 0.5110 | 1 | 0 |
| thioridazine | Homo sapiens (human) | IC50 | 0.0099 | 1 | 0 |
| thioridazine | Homo sapiens (human) | Ki | 0.0034 | 1 | 0 |
| tiapride | Homo sapiens (human) | IC50 | 1.1490 | 1 | 0 |
| tiapride | Homo sapiens (human) | Ki | 0.3900 | 1 | 0 |
| trazodone | Homo sapiens (human) | IC50 | 3.7430 | 1 | 0 |
| trazodone | Homo sapiens (human) | Ki | 1.2710 | 1 | 0 |
| zotepine | Homo sapiens (human) | Ki | 0.0112 | 2 | 2 |
| lysergic acid diethylamide | Homo sapiens (human) | Ki | 0.0270 | 1 | 1 |
| apomorphine | Homo sapiens (human) | IC50 | 0.0250 | 1 | 1 |
| apomorphine | Homo sapiens (human) | Ki | 0.0094 | 4 | 4 |
| mepazine | Homo sapiens (human) | IC50 | 2.0060 | 1 | 0 |
| mepazine | Homo sapiens (human) | Ki | 0.6810 | 1 | 0 |
| cyclizine | Homo sapiens (human) | IC50 | 2.9920 | 1 | 0 |
| cyclizine | Homo sapiens (human) | Ki | 1.0160 | 1 | 0 |
| phenyltoloxamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| ergotamine | Homo sapiens (human) | IC50 | 0.0043 | 1 | 0 |
| ergotamine | Homo sapiens (human) | Ki | 0.0015 | 1 | 0 |
| methylergonovine | Homo sapiens (human) | IC50 | 0.1670 | 1 | 0 |
| methylergonovine | Homo sapiens (human) | Ki | 0.0570 | 1 | 0 |
| dibenzothiazyl disulfide | Homo sapiens (human) | IC50 | 0.8510 | 1 | 0 |
| dibenzothiazyl disulfide | Homo sapiens (human) | Ki | 0.2890 | 1 | 0 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| methysergide | Homo sapiens (human) | IC50 | 0.1720 | 1 | 0 |
| methysergide | Homo sapiens (human) | Ki | 0.0590 | 1 | 0 |
| normethadone | Homo sapiens (human) | Ki | 4.2700 | 1 | 1 |
| dihydroergotamine | Homo sapiens (human) | IC50 | 0.0053 | 1 | 0 |
| dihydroergotamine | Homo sapiens (human) | Ki | 0.0018 | 1 | 0 |
| gentian violet | Homo sapiens (human) | IC50 | 0.8310 | 1 | 0 |
| gentian violet | Homo sapiens (human) | Ki | 0.2820 | 1 | 0 |
| acetabutone | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| azaperone | Homo sapiens (human) | Ki | 0.0768 | 3 | 5 |
| 2-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine | Homo sapiens (human) | IC50 | 0.1200 | 1 | 1 |
| benperidol | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| n-methyllaurotetanine | Homo sapiens (human) | Ki | 0.9500 | 1 | 1 |
| canadine, (s)-isomer | Homo sapiens (human) | Ki | 0.4330 | 1 | 1 |
| clemastine | Homo sapiens (human) | IC50 | 0.0073 | 1 | 0 |
| clemastine | Homo sapiens (human) | Ki | 0.0025 | 1 | 0 |
| danazol | Homo sapiens (human) | IC50 | 28.8600 | 1 | 0 |
| danazol | Homo sapiens (human) | Ki | 9.8000 | 1 | 0 |
| metergoline | Homo sapiens (human) | IC50 | 0.0077 | 1 | 0 |
| metergoline | Homo sapiens (human) | Ki | 0.0026 | 1 | 0 |
| lisuride | Homo sapiens (human) | IC50 | 0.0002 | 1 | 0 |
| lisuride | Homo sapiens (human) | Ki | 0.0006 | 3 | 2 |
| norapomorphine | Homo sapiens (human) | Ki | 0.0589 | 1 | 1 |
| bromocriptine | Homo sapiens (human) | IC50 | 0.0006 | 1 | 0 |
| bromocriptine | Homo sapiens (human) | Ki | 0.0436 | 2 | 1 |
| penfluridol | Homo sapiens (human) | Ki | 0.1360 | 1 | 1 |
| dobutamine | Homo sapiens (human) | IC50 | 4.9850 | 1 | 0 |
| dobutamine | Homo sapiens (human) | Ki | 1.6930 | 1 | 0 |
| butaclamol | Homo sapiens (human) | IC50 | 0.0112 | 3 | 3 |
| butaclamol | Homo sapiens (human) | Ki | 0.0000 | 2 | 2 |
| butaclamol | Homo sapiens (human) | IC50 | 0.0139 | 5 | 5 |
| butaclamol | Homo sapiens (human) | Ki | 0.0027 | 3 | 3 |
| pergolide | Homo sapiens (human) | IC50 | 0.0054 | 1 | 0 |
| pergolide | Homo sapiens (human) | Ki | 0.0022 | 3 | 2 |
| haloperidol decanoate | Homo sapiens (human) | Ki | 0.0035 | 1 | 1 |
| rimcazole | Homo sapiens (human) | Ki | 8.0000 | 1 | 1 |
| quinpirole | Homo sapiens (human) | Ki | 0.0844 | 20 | 20 |
| preclamol | Homo sapiens (human) | Ki | 0.1603 | 2 | 3 |
| ipsapirone | Homo sapiens (human) | IC50 | 1.2000 | 1 | 1 |
| quinelorane | Homo sapiens (human) | Ki | 0.0009 | 1 | 1 |
| eticlopride | Homo sapiens (human) | Ki | 0.0001 | 4 | 4 |
| mk 458 | Homo sapiens (human) | Ki | 0.0010 | 1 | 2 |
| naxagolide | Homo sapiens (human) | Ki | 0.0002 | 2 | 2 |
| n 0437, (-)-isomer | Homo sapiens (human) | Ki | 0.0040 | 2 | 2 |
| sertindole | Homo sapiens (human) | Ki | 0.0054 | 2 | 2 |
| aripiprazole | Homo sapiens (human) | Ki | 0.0054 | 19 | 20 |
| ziprasidone | Homo sapiens (human) | Ki | 0.0076 | 5 | 5 |
| dopamine hydrochloride | Homo sapiens (human) | Ki | 0.0187 | 1 | 2 |
| centbutindole | Homo sapiens (human) | Ki | 0.0110 | 1 | 1 |
| tetrahydropalmatine | Homo sapiens (human) | Ki | 1.3710 | 1 | 1 |
| ergocornine | Homo sapiens (human) | IC50 | 0.0029 | 1 | 0 |
| ergocornine | Homo sapiens (human) | Ki | 0.0010 | 1 | 0 |
| salsolinol | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
| gr 127935 | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
| 3-iodo-2-hydroxy-6-methoxy-n-((1-ethyl-2-pyrrolidinyl)methyl)benzamide | Homo sapiens (human) | Ki | 0.0042 | 1 | 1 |
| s 14297 | Homo sapiens (human) | Ki | 0.0130 | 1 | 1 |
| pd 128907 | Homo sapiens (human) | Ki | 7.8100 | 2 | 2 |
| 3-n-methylspiperone | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| pramipexole | Homo sapiens (human) | Ki | 0.0082 | 17 | 17 |
| sb 204070a | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| aj 76 | Homo sapiens (human) | Ki | 0.0480 | 2 | 2 |
| desloratadine | Homo sapiens (human) | IC50 | 1.9060 | 1 | 0 |
| desloratadine | Homo sapiens (human) | Ki | 0.6470 | 1 | 0 |
| 1,2,3,6-tetrahydro-4-phenyl-1-((3-phenyl-3-cyclohexen-1-yl)methyl)pyridine | Homo sapiens (human) | Ki | 0.0166 | 3 | 3 |
| n 0734 | Homo sapiens (human) | Ki | 0.0018 | 1 | 1 |
| tamsulosin | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| 2-methoxy-n-n-propylnorapomorphine | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| 5-(dipropylamino)-5,6-dihydro-4h-imidazo-(5,1ij)quinolin-2(1h)-one | Homo sapiens (human) | Ki | 0.0271 | 1 | 1 |
| dc 015 | Homo sapiens (human) | Ki | 0.9850 | 1 | 1 |
| u-91356 | Homo sapiens (human) | Ki | 0.1572 | 3 | 3 |
| l 741742 | Homo sapiens (human) | Ki | 0.6975 | 4 | 4 |
| sonepiprazole | Homo sapiens (human) | Ki | 2.7780 | 1 | 1 |
| l 741626 | Homo sapiens (human) | IC50 | 0.0904 | 1 | 1 |
| l 741626 | Homo sapiens (human) | Ki | 0.1037 | 7 | 7 |
| alpha-ergocryptine | Homo sapiens (human) | IC50 | 0.0006 | 1 | 0 |
| alpha-ergocryptine | Homo sapiens (human) | Ki | 0.0002 | 1 | 0 |
| chloroethylnorapomorphine | Homo sapiens (human) | IC50 | 8.0000 | 1 | 1 |
| harmalan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| corydalmine | Homo sapiens (human) | Ki | 1.7130 | 1 | 1 |
| n-n-propylnorapomorphine | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| n-demethyllysergic acid diethylamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 5-hydroxy-2-n,n-dipropylaminotetralin | Homo sapiens (human) | Ki | 0.0011 | 3 | 3 |
| piboserod | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 0.3090 | 1 | 1 |
| ngd 94-1 | Homo sapiens (human) | Ki | 8.0000 | 1 | 1 |
| maduramicin | Homo sapiens (human) | IC50 | 0.0270 | 1 | 0 |
| maduramicin | Homo sapiens (human) | Ki | 0.0093 | 1 | 0 |
| roxindole | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| 1-methyl-6-methoxy-dihydro-beta-carboline | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| tetrahydrocolumbamine | Homo sapiens (human) | Ki | 0.0373 | 1 | 1 |
| saquinavir | Homo sapiens (human) | IC50 | 15.3660 | 1 | 0 |
| saquinavir | Homo sapiens (human) | Ki | 5.2190 | 1 | 0 |
| terconazole | Homo sapiens (human) | IC50 | 4.7120 | 1 | 0 |
| terconazole | Homo sapiens (human) | Ki | 1.6000 | 1 | 0 |
| sb 243213 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| ergonovine | Homo sapiens (human) | IC50 | 0.5670 | 1 | 0 |
| ergonovine | Homo sapiens (human) | Ki | 0.1930 | 1 | 0 |
| dihydroergocristine monomesylate | Homo sapiens (human) | IC50 | 0.0023 | 1 | 0 |
| dihydroergocristine monomesylate | Homo sapiens (human) | Ki | 0.0008 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 8.7960 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 2.9870 | 1 | 0 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | IC50 | 2.1039 | 1 | 0 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | Ki | 0.7145 | 1 | 0 |
| chlorprothixene | Homo sapiens (human) | Ki | 0.0046 | 1 | 1 |
| levosulpiride | Homo sapiens (human) | IC50 | 0.1230 | 1 | 0 |
| levosulpiride | Homo sapiens (human) | Ki | 0.0727 | 3 | 2 |
| 4,4-dicarboxy-5-pyridoxylproline | Homo sapiens (human) | Ki | 0.1974 | 1 | 1 |
| flunarizine | Homo sapiens (human) | IC50 | 0.0970 | 1 | 0 |
| flunarizine | Homo sapiens (human) | Ki | 0.0330 | 1 | 0 |
| benztropine | Homo sapiens (human) | IC50 | 0.6540 | 1 | 0 |
| benztropine | Homo sapiens (human) | Ki | 0.2220 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | IC50 | 0.2520 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | Ki | 0.0860 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | IC50 | 1.3190 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | Ki | 0.4480 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | IC50 | 1.0720 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 0.3640 | 1 | 0 |
| raclopride | Homo sapiens (human) | Ki | 0.0114 | 4 | 4 |
| bp 897 | Homo sapiens (human) | IC50 | 0.0203 | 2 | 3 |
| bp 897 | Homo sapiens (human) | Ki | 0.0021 | 12 | 12 |
| n-(1-methyl-5-indolyl)-n'-(3-methyl-5-isothiazolyl)urea | Homo sapiens (human) | Ki | 31.6228 | 1 | 1 |
| sb-224289 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| nafadotride | Homo sapiens (human) | Ki | 0.0005 | 2 | 2 |
| pd 168,077 | Homo sapiens (human) | Ki | 3.7550 | 2 | 2 |
| 3-[bis(4-fluorophenyl)methoxy]-8-methyl-8-azabicyclo[3.2.1]octane | Homo sapiens (human) | Ki | 0.1450 | 1 | 1 |
| gr 103691 | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| le 300 | Homo sapiens (human) | Ki | 0.0331 | 2 | 2 |
| harmine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| montelukast | Homo sapiens (human) | IC50 | 7.7470 | 1 | 0 |
| montelukast | Homo sapiens (human) | Ki | 2.6310 | 1 | 0 |
| amentoflavone | Homo sapiens (human) | Ki | 1.2410 | 1 | 1 |
| sb 277011 | Homo sapiens (human) | Ki | 0.7202 | 14 | 14 |
| preclamol | Homo sapiens (human) | Ki | 0.0785 | 4 | 4 |
| l 745870 | Homo sapiens (human) | Ki | 14.2256 | 13 | 13 |
| lacidipine | Homo sapiens (human) | IC50 | 6.1700 | 1 | 0 |
| lacidipine | Homo sapiens (human) | Ki | 2.0960 | 1 | 0 |
| pd 128907 | Homo sapiens (human) | Ki | 0.0143 | 5 | 6 |
| sb 258719 | Homo sapiens (human) | Ki | 3.9811 | 1 | 1 |
| sb 271046 | Homo sapiens (human) | Ki | 0.9156 | 2 | 2 |
| bay 11-7085 | Homo sapiens (human) | IC50 | 3.4600 | 1 | 0 |
| bay 11-7085 | Homo sapiens (human) | Ki | 1.1750 | 1 | 0 |
| oxiconazole | Homo sapiens (human) | IC50 | 1.9937 | 1 | 0 |
| oxiconazole | Homo sapiens (human) | Ki | 0.6771 | 1 | 0 |
| 7-hydroxy-2-(n-n-propyl-n-(3-iodo-2'-propenyl)-amino)tetralin | Homo sapiens (human) | Ki | 0.0018 | 1 | 1 |
| 8-hydroxy-2-(di-n-propylamino)tetralin, (r)-isomer | Homo sapiens (human) | Ki | 0.1790 | 1 | 1 |
| 7-hydroxy-2-n,n-dipropylaminotetralin, (r)-isomer | Homo sapiens (human) | Ki | 0.0032 | 7 | 8 |
| l 750667 | Homo sapiens (human) | Ki | 4.5000 | 1 | 1 |
| uh 232 | Homo sapiens (human) | Ki | 0.0040 | 1 | 1 |
| sb 269970 | Homo sapiens (human) | Ki | 2.5119 | 1 | 1 |
| stepholidine | Homo sapiens (human) | Ki | 0.0500 | 3 | 3 |
| sarizotan | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
| ms-245 | Homo sapiens (human) | Ki | 0.0800 | 1 | 1 |
| n-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide | Homo sapiens (human) | Ki | 5.0119 | 1 | 1 |
| indacaterol | Homo sapiens (human) | Ki | 1.0480 | 1 | 1 |
| armodafinil | Homo sapiens (human) | Ki | 39.0000 | 1 | 1 |
| osu 6162 | Homo sapiens (human) | Ki | 1.3050 | 1 | 1 |
| pnu-95666 | Homo sapiens (human) | Ki | 2.4455 | 4 | 4 |
| cp 293019 | Homo sapiens (human) | Ki | 2.0000 | 2 | 2 |
| n-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide | Homo sapiens (human) | IC50 | 0.0063 | 1 | 1 |
| n-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide | Homo sapiens (human) | Ki | 0.0009 | 4 | 4 |
| sb258741 | Homo sapiens (human) | Ki | 1.2589 | 1 | 1 |
| f 13640 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| s 33084 | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| slv 313 | Homo sapiens (human) | Ki | 0.0040 | 1 | 1 |
| fauc 346 | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
| fauc 346 | Homo sapiens (human) | Ki | 0.0002 | 5 | 5 |
| ngb 2904 | Homo sapiens (human) | IC50 | 0.0113 | 3 | 3 |
| ngb 2904 | Homo sapiens (human) | Ki | 0.0017 | 9 | 9 |
| 4-(3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl)-1-(4-fluorophenyl)butan-1-one | Homo sapiens (human) | Ki | 0.8153 | 2 | 3 |
| flb 457 | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| pnu 96415e | Homo sapiens (human) | Ki | 0.2400 | 1 | 1 |
| sb 269,652 | Homo sapiens (human) | Ki | 0.0039 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| n-((1-allyl-2-pyrrolidinyl)methyl)-5-(3-fluoropropyl)-2,3-dimethoxybenzamide | Homo sapiens (human) | Ki | 0.0016 | 1 | 1 |
| 77-lh-28-1 | Homo sapiens (human) | Ki | 0.6166 | 2 | 2 |
| fauc 365 | Homo sapiens (human) | IC50 | 0.0049 | 2 | 2 |
| fauc 365 | Homo sapiens (human) | Ki | 0.0008 | 12 | 12 |
| sb-649915 | Homo sapiens (human) | Ki | 0.6310 | 1 | 1 |
| 11-hydroxy-n-(n-propyl)noraporphine hydrochloride, (r)-isomer | Homo sapiens (human) | Ki | 0.8506 | 2 | 2 |
| fauc 213 | Homo sapiens (human) | Ki | 4.7813 | 16 | 16 |
| way-208466 | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| fauc 113 | Homo sapiens (human) | Ki | 4.8390 | 10 | 10 |
| desmethoxyfallypride | Homo sapiens (human) | Ki | 0.0330 | 1 | 1 |
| 2-(3',4',5',6'-tetrahydro-2'h-(2,4') bipyridinyl-1'-yl)-n-m-tolyl-acetamide | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 2-(3',4',5',6'-tetrahydro-2'h-(2,4') bipyridinyl-1'-yl)-n-m-tolyl-acetamide | Homo sapiens (human) | Ki | 0.9235 | 2 | 2 |
| cariprazine | Homo sapiens (human) | Ki | 0.0002 | 6 | 7 |
| naphyrone | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 5-hydroxy-2-n,n-dipropylaminotetralin, (s)-isomer | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
| naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| pg 01037 | Homo sapiens (human) | IC50 | 0.0030 | 2 | 2 |
| pg 01037 | Homo sapiens (human) | Ki | 0.0009 | 6 | 6 |
| le 404 | Homo sapiens (human) | Ki | 0.0473 | 3 | 3 |
| gsk598809 | Homo sapiens (human) | Ki | 0.0032 | 1 | 1 |
| 7-hydroxy-2-n,n-dipropylaminotetralin hydrobromide | Homo sapiens (human) | Ki | 0.0069 | 1 | 1 |
| ncq 298 | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| LSM-2536 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 3.6616 | 2 | 3 |
| 3-(2-((cyclobutylmethyl)(phenethyl)amino)ethyl)phenol | Homo sapiens (human) | IC50 | 0.9530 | 1 | 1 |
| 3-(2-((cyclobutylmethyl)(phenethyl)amino)ethyl)phenol | Homo sapiens (human) | Ki | 0.2820 | 1 | 1 |
| clozapine | Homo sapiens (human) | IC50 | 0.3540 | 2 | 1 |
| clozapine | Homo sapiens (human) | Ki | 0.4831 | 34 | 33 |
| olanzapine | Homo sapiens (human) | IC50 | 0.0780 | 1 | 0 |
| olanzapine | Homo sapiens (human) | Ki | 0.0400 | 10 | 9 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 7-hydroxy-2-n,n-dipropylaminotetralin | Homo sapiens (human) | EC50 | 0.0005 | 1 | 1 |
| haloperidol | Homo sapiens (human) | Kd | 0.3162 | 1 | 1 |
| ropinirole | Homo sapiens (human) | EC50 | 0.0406 | 5 | 6 |
| sulpiride | Homo sapiens (human) | Kd | 0.0398 | 1 | 1 |
| apomorphine | Homo sapiens (human) | EC50 | 0.0070 | 1 | 1 |
| dronabinol | Homo sapiens (human) | EC50 | 0.0102 | 1 | 1 |
| quinpirole | Homo sapiens (human) | EC50 | 0.0113 | 27 | 30 |
| quinelorane | Homo sapiens (human) | EC50 | 0.0010 | 1 | 1 |
| aripiprazole | Homo sapiens (human) | EC50 | 0.0198 | 2 | 4 |
| pramipexole | Homo sapiens (human) | EC50 | 0.0020 | 6 | 6 |
| pramipexole | Homo sapiens (human) | Kd | 0.0000 | 1 | 1 |
| 5-(dipropylamino)-5,6-dihydro-4h-imidazo-(5,1ij)quinolin-2(1h)-one | Homo sapiens (human) | EC50 | 0.0218 | 1 | 1 |
| u-91356 | Homo sapiens (human) | EC50 | 0.0096 | 2 | 2 |
| l 741626 | Homo sapiens (human) | EC50 | 0.0904 | 1 | 1 |
| sk&f 89124 | Homo sapiens (human) | EC50 | 0.0018 | 1 | 2 |
| 5-hydroxy-2-n,n-dipropylaminotetralin | Homo sapiens (human) | EC50 | 0.0007 | 2 | 2 |
| bp 897 | Homo sapiens (human) | EC50 | 0.0022 | 3 | 3 |
| bp 897 | Homo sapiens (human) | Kd | 0.0158 | 1 | 1 |
| preclamol | Homo sapiens (human) | EC50 | 0.0308 | 2 | 2 |
| pnu-95666 | Homo sapiens (human) | EC50 | 0.4275 | 2 | 2 |
| n-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide | Homo sapiens (human) | EC50 | 0.0063 | 2 | 2 |
| fauc 346 | Homo sapiens (human) | EC50 | 0.0004 | 1 | 1 |
| ngb 2904 | Homo sapiens (human) | Kd | 0.0020 | 1 | 1 |
| 2-(3',4',5',6'-tetrahydro-2'h-(2,4') bipyridinyl-1'-yl)-n-m-tolyl-acetamide | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
| cariprazine | Homo sapiens (human) | EC50 | 0.0058 | 1 | 2 |
| 5-hydroxy-2-n,n-dipropylaminotetralin, (s)-isomer | Homo sapiens (human) | EC50 | 0.0006 | 1 | 1 |
| 7-hydroxy-2-n,n-dipropylaminotetralin hydrobromide | Homo sapiens (human) | EC50 | 0.0010 | 1 | 1 |
| 3-(2-((cyclobutylmethyl)(phenethyl)amino)ethyl)phenol | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
Drugs with Other Measurements
Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Discovery of 4-(4-(2-((5-Hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)(propyl)amino)ethyl)piperazin-1-yl)quinolin-8-ol and its analogues as highly potent dopamine D2/D3 agonists and as iron chelator: in vivo activity indicates potential application in symptoJournal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.Journal of medicinal chemistry, , May-22, Volume: 51, Issue:10, 2008
Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
Iodinated 2-aminotetralins and 3-amino-1-benzopyrans: ligands for dopamine D2 and D3 receptors.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
[no title available]Bioorganic & medicinal chemistry letters, , 06-01, Volume: 28, Issue:10, 2018
Tetrahydroprotoberberine alkaloids with dopamine and σ receptor affinity.Bioorganic & medicinal chemistry, , May-01, Volume: 24, Issue:9, 2016
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Identification of a 2-phenyl-substituted octahydrobenzo[f]quinoline as a dopamine D₃ receptor-selective full agonist ligand.Bioorganic & medicinal chemistry, , Nov-01, Volume: 20, Issue:21, 2012
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 19, Issue:2, 2009
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
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists.Journal of medicinal chemistry, , Volume: 24, Issue:6, 1981
[no title available],
Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 13, Issue:19, 2003
18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography.Journal of medicinal chemistry, , Nov-12, Volume: 36, Issue:23, 1993
[no title available]Bioorganic & medicinal chemistry letters, , 03-01, Volume: 59, 2022
2-Phenylcyclopropylmethylamine Derivatives as Dopamine DJournal of medicinal chemistry, , 12-09, Volume: 64, Issue:23, 2021
Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the HEuropean journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
[no title available]Journal of natural products, , 01-24, Volume: 83, Issue:1, 2020
[no title available]Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Potent haloperidol derivatives covalently binding to the dopamine D2 receptor.Bioorganic & medicinal chemistry, , 10-01, Volume: 25, Issue:19, 2017
Multicomponent Synthesis and Biological Evaluation of a Piperazine-Based Dopamine Receptor Ligand Library.ACS medicinal chemistry letters, , Aug-13, Volume: 6, Issue:8, 2015
Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
Design, synthesis, and structure-activity relationship studies of a series of [4-(4-carboxamidobutyl)]-1-arylpiperazines: insights into structural features contributing to dopamine D3 versus D2 receptor subtype selectivity.Journal of medicinal chemistry, , Aug-28, Volume: 57, Issue:16, 2014
Further evaluation of the tropane analogs of haloperidol.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles.Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.Bioorganic & medicinal chemistry, , Feb-01, Volume: 20, Issue:3, 2012
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Development of a bivalent dopamine D₂ receptor agonist.Journal of medicinal chemistry, , Nov-24, Volume: 54, Issue:22, 2011
Bivalent dopamine D2 receptor ligands: synthesis and binding properties.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626.Bioorganic & medicinal chemistry, , Jul-15, Volume: 18, Issue:14, 2010
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.Bioorganic & medicinal chemistry, , Feb-15, Volume: 17, Issue:4, 2009
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.Journal of medicinal chemistry, , Jan-08, Volume: 52, Issue:1, 2009
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 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
Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors.European journal of medicinal chemistry, , Volume: 42, Issue:7, 2007
4-[omega-[4-arylpiperazin-1-yl]alkoxy]phenyl)imidazo[1,2-a]pyridine derivatives: fluorescent high-affinity dopamine D3 receptor ligands as potential probes for receptor visualization.Journal of medicinal chemistry, , Oct-04, Volume: 50, Issue:20, 2007
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
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
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.Journal of medicinal chemistry, , Dec-15, Volume: 48, Issue:25, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
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
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands.Bioorganic & medicinal chemistry letters, , May-20, Volume: 12, Issue:10, 2002
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.Journal of medicinal chemistry, , Jul-18, Volume: 40, Issue:15, 1997
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists.Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.Journal of medicinal chemistry, , Oct-14, Volume: 37, Issue:21, 1994
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.Journal of medicinal chemistry, , Nov-26, Volume: 36, Issue:24, 1993
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.Journal of medicinal chemistry, , Oct-15, Volume: 36, Issue:21, 1993
Aporphines. 58. N-(2-chloroethyl) [8,9-2H]norapomorphine, an irreversible ligand for dopamine receptors: synthesis and application.Journal of medicinal chemistry, , Volume: 27, Issue:6, 1984
Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists.Journal of medicinal chemistry, , Volume: 24, Issue:6, 1981
[no title available],
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
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 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
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
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
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
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
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
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 new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.Journal of medicinal chemistry, , Jan-08, Volume: 52, Issue:1, 2009
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 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
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).Journal of medicinal chemistry, , Dec-31, Volume: 41, Issue:27, 1998
[no title available],
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[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
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Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 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
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Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
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Exception That Proves the Rule: Investigation of Privileged Stereochemistry in Designing Dopamine DACS medicinal chemistry letters, , Oct-08, Volume: 11, Issue:10, 2020
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Tranylcypromine substituted cis-hydroxycyclobutylnaphthamides as potent and selective dopamine D₃ receptor antagonists.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Synthesis and binding affinity of new 1,4-disubstituted triazoles as potential dopamine D(3) receptor ligands.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 23, Issue:20, 2013
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 17, Issue:24, 2007
Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists.Journal of medicinal chemistry, , Sep-08, Volume: 48, Issue:18, 2005
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
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Thiazoloindans and thiazolobenzopyrans: a novel class of orally active central dopamine (partial) agonists.Journal of medicinal chemistry, , Sep-21, Volume: 43, Issue:19, 2000
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.Journal of medicinal chemistry, , Oct-15, Volume: 36, Issue:21, 1993
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Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 17, Issue:3, 2007
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
[no title available],
Discovery of 4-(4-(2-((5-Hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)(propyl)amino)ethyl)piperazin-1-yl)quinolin-8-ol and its analogues as highly potent dopamine D2/D3 agonists and as iron chelator: in vivo activity indicates potential application in symptoJournal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Development of (S)-N6-(2-(4-(isoquinolin-1-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]-thiazole-2,6-diamine and its analogue as a D3 receptor preferring agonist: potent in vivo activity in Parkinson's disease animal models.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Investigation of various N-heterocyclic substituted piperazine versions of 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol: effect on affinity and selectivity for dopamine D3 receptor.Bioorganic & medicinal chemistry, , Jun-01, Volume: 17, Issue:11, 2009
Synthesis and dopaminergic activity of pyridine analogs of 5-hydroxy-2-(di-n-propylamino)tetralin.Journal of medicinal chemistry, , Aug-04, Volume: 38, Issue:16, 1995
Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles.Bioorganic & medicinal chemistry letters, , Sep-04, Volume: 10, Issue:17, 2000
Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid.Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 9, Issue:6, 1999
[no title available],
Highly Selective Dopamine D3 Receptor (D3R) Antagonists and Partial Agonists Based on Eticlopride and the D3R Crystal Structure: New Leads for Opioid Dependence Treatment.Journal of medicinal chemistry, , 08-25, Volume: 59, Issue:16, 2016
Tranylcypromine substituted cis-hydroxycyclobutylnaphthamides as potent and selective dopamine D₃ receptor antagonists.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.Bioorganic & medicinal chemistry, , Nov-01, Volume: 15, Issue:21, 2007
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
Design, synthesis and preliminary bioactivity evaluation of bitopic benzopyranomorpholine analogues as selective dopamine D3 receptor ligands as anti-drug addiction therapeutic agents.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 48, 2021
Improving selectivity of dopamine D3 receptor ligands.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 26, Issue:3, 2016
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.Journal of medicinal chemistry, , May-26, Volume: 54, Issue:10, 2011
Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II.Bioorganic & medicinal chemistry, , Jan-15, Volume: 17, Issue:2, 2009
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
Hybrid approach for the design of highly affine and selective dopamine D(3) receptor ligands using privileged scaffolds of biogenic amine GPCR ligands.Bioorganic & medicinal chemistry, , Dec-01, Volume: 15, Issue:23, 2007
Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.Journal of medicinal chemistry, , Dec-15, Volume: 48, Issue:25, 2005
N-(omega-(4-(2-methoxyphenyl)piperazin-1-yl)alkyl)carboxamides as dopamine D2 and D3 receptor ligands.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.Journal of medicinal chemistry, , Oct-10, Volume: 45, Issue:21, 2002
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
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
[no title available]Journal of medicinal chemistry, , 11-14, Volume: 62, Issue:21, 2019
Substituted [(4-phenylpiperazinyl)-methyl]benzamides: selective dopamine D4 agonists.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
Dopamine/serotonin receptor ligands. Part 15: Oxygenation of the benz-indolo-azecine LE 300 leads to novel subnanomolar dopamine D1/D5 antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Dopamine/serotonin receptor ligands. 13: Homologization of a benzindoloazecine-type dopamine receptor antagonist modulates the affinities for dopamine D(1)-D(5) receptors.Journal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
[no title available]Journal of medicinal chemistry, , 02-23, Volume: 60, Issue:4, 2017
1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists.Journal of medicinal chemistry, , 09-22, Volume: 59, Issue:18, 2016
1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 26, Issue:4, 2016
1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Dopamine D3 receptor antagonists: the quest for a potentially selective PET ligand. Part one: lead identification.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Dopamine D3 receptor antagonists: the quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part 2: [g]-fused and hetero-fused systems.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
Novel 2,3,4,5-tetrahydro-1H-3-benzazepines with high affinity and selectivity for the dopamine D3 receptor.Bioorganic & medicinal chemistry letters, , Nov-20, Volume: 10, Issue:22, 2000
[no title available]Bioorganic & medicinal chemistry letters, , 06-01, Volume: 28, Issue:10, 2018
Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the TreatJournal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725.Bioorganic & medicinal chemistry letters, , Sep-02, Volume: 12, Issue:17, 2002
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.Journal of medicinal chemistry, , Aug-19, Volume: 37, Issue:17, 1994
[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
[no title available]Journal of medicinal chemistry, , 11-14, Volume: 62, Issue:21, 2019
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine DJournal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
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Identification of a new selective dopamine D4 receptor ligand.Bioorganic & medicinal chemistry, , Jun-15, Volume: 22, Issue:12, 2014
Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases.Bioorganic & medicinal chemistry, , Jul-01, Volume: 17, Issue:13, 2009
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
Synthesis and sar of 2- and 3-substituted 7-azaindoles as potential dopamine D4 ligands.Bioorganic & medicinal chemistry letters, , Feb-22, Volume: 9, Issue:4, 1999
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.Journal of medicinal chemistry, , Dec-16, Volume: 42, Issue:25, 1999
Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.Bioorganic & medicinal chemistry letters, , Jan-04, Volume: 9, Issue:1, 1999
Isoindolinone enantiomers having affinity for the dopamine D4 receptor.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 8, Issue:12, 1998
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Design, synthesis and preliminary bioactivity evaluation of bitopic benzopyranomorpholine analogues as selective dopamine D3 receptor ligands as anti-drug addiction therapeutic agents.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 48, 2021
Exception That Proves the Rule: Investigation of Privileged Stereochemistry in Designing Dopamine DACS medicinal chemistry letters, , Oct-08, Volume: 11, Issue:10, 2020
The Significance of Chirality in Drug Design and Synthesis of Bitopic Ligands as DJournal of medicinal chemistry, , 07-11, Volume: 62, Issue:13, 2019
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907).Journal of medicinal chemistry, , Jul-27, Volume: 43, Issue:15, 2000
Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.Bioorganic & medicinal chemistry letters, , May-20, Volume: 12, Issue:10, 2002
Development of (S)-N6-(2-(4-(isoquinolin-1-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]-thiazole-2,6-diamine and its analogue as a D3 receptor preferring agonist: potent in vivo activity in Parkinson's disease animal models.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Further structure-activity relationships study of hybrid 7-{[2-(4-phenylpiperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol analogues: identification of a high-affinity D3-preferring agonist with potent in vivo activity with long duration Journal of medicinal chemistry, , Jan-10, Volume: 51, Issue:1, 2008
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
Further characterization of structural requirements for ligands at the dopamine D(2) and D(3) receptor: exploring the thiophene moiety.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Dopaminergic 7-aminotetrahydroindolizines: ex-chiral pool synthesis and preferential D3 receptor binding.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
Affinity for dopamine D2, D3, and D4 receptors of 2-aminotetralins. Relevance of D2 agonist binding for determination of receptor subtype selectivity.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Synthesis and evaluation of C9 alkoxy analogues of (-)-stepholidine as dopamine receptor ligands.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Tetrahydroprotoberberine alkaloids with dopamine and σ receptor affinity.Bioorganic & medicinal chemistry, , May-01, Volume: 24, Issue:9, 2016
Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles.Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
[no title available]Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
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Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists.Bioorganic & medicinal chemistry letters, , Jul-07, Volume: 13, Issue:13, 2003
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
Novel benzopyrano[3,4-c]pyrrole derivatives as potent and selective dopamine D3 receptor antagonist.Bioorganic & medicinal chemistry letters, , Jul-19, Volume: 9, Issue:14, 1999
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II.Bioorganic & medicinal chemistry, , Jan-15, Volume: 17, Issue:2, 2009
N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.Journal of medicinal chemistry, , Oct-10, Volume: 45, Issue:21, 2002
Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Evaluation of N-phenyl homopiperazine analogs as potential dopamine D3 receptor selective ligands.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.Journal of medicinal chemistry, , May-26, Volume: 54, Issue:10, 2011
Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.Journal of medicinal chemistry, , Dec-15, Volume: 48, Issue:25, 2005
NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.Bioorganic & medicinal chemistry, , Feb-15, Volume: 17, Issue:4, 2009
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 16, Issue:12, 2006
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
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[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine DJournal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
Evaluation of N-phenyl homopiperazine analogs as potential dopamine D3 receptor selective ligands.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Aromatic ring functionalization of benzolactam derivatives: new potent dopamine D3 receptor ligands.Bioorganic & medicinal chemistry letters, , May-01, Volume: 21, Issue:9, 2011
N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype.Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 14, Issue:15, 2004
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.Journal of medicinal chemistry, , Oct-10, Volume: 45, Issue:21, 2002
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Discovery of highly potent and selective D4 ligands by interactive SAR study.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 23, Issue:18, 2013
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
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Identification of a new selective dopamine D4 receptor ligand.Bioorganic & medicinal chemistry, , Jun-15, Volume: 22, Issue:12, 2014
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.Bioorganic & medicinal chemistry letters, , Aug-05, Volume: 12, Issue:15, 2002
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.Bioorganic & medicinal chemistry letters, , Jan-04, Volume: 9, Issue:1, 1999
Dopamine DJournal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
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
Development of molecular tools based on the dopamine DBioorganic & medicinal chemistry, , 07-01, Volume: 25, Issue:13, 2017
Synthetic Approaches to the New Drugs Approved During 2015.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 2017
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
Functionally selective dopamine D₂, D₃ receptor partial agonists.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Novel bivalent ligands for D2/D3 dopamine receptors: Significant co-operative gain in D2 affinity and potency.ACS medicinal chemistry letters, , Oct-26, Volume: 3, Issue:12, 2012
Affinity for dopamine D2, D3, and D4 receptors of 2-aminotetralins. Relevance of D2 agonist binding for determination of receptor subtype selectivity.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.Journal of medicinal chemistry, , May-26, Volume: 54, Issue:10, 2011
Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities?Bioorganic & medicinal chemistry, , Oct-01, Volume: 17, Issue:19, 2009
Dopamine/serotonin receptor ligands. Part 15: Oxygenation of the benz-indolo-azecine LE 300 leads to novel subnanomolar dopamine D1/D5 antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Dopamine/serotonin receptor ligands. 12(1): SAR studies on hexahydro-dibenz[d,g]azecines lead to 4-chloro-7-methyl-5,6,7,8,9,14-hexahydrodibenz[d,g]azecin-3-ol, the first picomolar D5-selective dopamine-receptor antagonist.Journal of medicinal chemistry, , Mar-23, Volume: 49, Issue:6, 2006
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
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
Lessons learned from herbal medicinal products: the example of St. John's Wort (perpendicular).Journal of natural products, , May-28, Volume: 73, Issue:5, 2010
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.Journal of medicinal chemistry, , Jan-08, Volume: 52, Issue:1, 2009
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 19, Issue:2, 2009
Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases.Bioorganic & medicinal chemistry, , Jul-01, Volume: 17, Issue:13, 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
2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.Bioorganic & medicinal chemistry letters, , Aug-05, Volume: 12, Issue:15, 2002
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles.Bioorganic & medicinal chemistry letters, , Sep-04, Volume: 10, Issue:17, 2000
Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments.Journal of medicinal chemistry, , Nov-16, Volume: 43, Issue:23, 2000
2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands.Bioorganic & medicinal chemistry letters, , Jul-19, Volume: 9, Issue:14, 1999
1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels.Journal of medicinal chemistry, , Jul-15, Volume: 42, Issue:14, 1999
Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 9, Issue:21, 1999
Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.Bioorganic & medicinal chemistry letters, , Jan-04, Volume: 9, Issue:1, 1999
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.Bioorganic & medicinal chemistry letters, , May-03, Volume: 9, Issue:9, 1999
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).Journal of medicinal chemistry, , Dec-31, Volume: 41, Issue:27, 1998
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.Journal of medicinal chemistry, , Jul-18, Volume: 40, Issue:15, 1997
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
2-Phenyl-4(5)-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]imidazole. A highly selective antagonist at cloned human D4 receptors.Journal of medicinal chemistry, , Jan-03, Volume: 40, Issue:1, 1997
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists.Journal of medicinal chemistry, , Volume: 24, Issue:6, 1981
[no title available],
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 new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.Journal of medicinal chemistry, , Jan-08, Volume: 52, Issue:1, 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
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| dopamine neurotransmitter receptor activity, coupled via Gi/Go | molecular function | Combining with the neurotransmitter dopamine and activating adenylate cyclase via coupling to Gi/Go to initiate a change in cell activity. [GOC:mah, ISBN:0953351033, IUPHAR_RECEPTOR:2254, IUPHAR_RECEPTOR:2256, IUPHAR_RECEPTOR:2258] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
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 1 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] |
Involved In
This protein is involved in 39 target(s):
| Target | Category | Definition |
|---|
| synaptic transmission, dopaminergic | biological process | The vesicular release of dopamine. from a presynapse, across a chemical synapse, the subsequent activation of dopamine 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:dos, GOC:dph] |
| G protein-coupled receptor internalization | biological process | The process that results in the uptake of a G protein-coupled receptor into an endocytic vesicle. [PMID:8396717] |
| intracellular calcium ion homeostasis | biological process | A homeostatic process involved in the maintenance of a steady state level of calcium ions within a cell. [GOC:ceb, GOC:mah] |
| 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-activating dopamine receptor signaling pathway | biological process | An adenylate cyclase-activating G protein-coupled receptor signaling pathway initiated by dopamine binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:mah, GOC:signaling] |
| adenylate cyclase-inhibiting dopamine receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by dopamine binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| learning or memory | biological process | The acquisition and processing of information and/or the storage and retrieval of this information over time. [GOC:jid, PMID:8938125] |
| learning | biological process | Any process in an organism in which a relatively long-lasting adaptive behavioral change occurs as the result of experience. [ISBN:0582227089, ISBN:0721662544] |
| locomotory behavior | biological process | The specific movement from place to place of an organism in response to external or internal stimuli. Locomotion of a whole organism in a manner dependent upon some combination of that organism's internal state and external conditions. [GOC:dph] |
| visual learning | biological process | Any process in an organism in which a change in behavior of an individual occurs in response to repeated exposure to a visual cue. [GOC:jid, ISBN:0582227089] |
| response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
| regulation of dopamine secretion | biological process | Any process that modulates the frequency, rate or extent of the regulated release of dopamine. [GOC:ef] |
| positive regulation of cytokinesis | biological process | Any process that activates or increases the frequency, rate or extent of the division of the cytoplasm of a cell, and its separation into two daughter cells. [GOC:mah] |
| circadian regulation of gene expression | biological process | Any process that modulates the frequency, rate or extent of gene expression such that an expression pattern recurs with a regularity of approximately 24 hours. [GOC:mah] |
| response to histamine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a histamine stimulus. Histamine, the biogenic amine 2-(1H-imidazol-4-yl)ethanamine, is involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter. [GOC:BHF, GOC:mah, GOC:vk] |
| social behavior | biological process | Behavior directed towards society, or taking place between members of the same species. Occurs predominantly, or only, in individuals that are part of a group. [GOC:jh2, PMID:12848939, Wikipedia:Social_behavior] |
| response to cocaine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cocaine stimulus. Cocaine is a crystalline alkaloid obtained from the leaves of the coca plant. [GOC:ef, GOC:jl] |
| dopamine metabolic process | biological process | The chemical reactions and pathways involving dopamine, a catecholamine neurotransmitter and a metabolic precursor of noradrenaline and adrenaline. [GOC:jl, ISBN:0198506732] |
| response to morphine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a morphine stimulus. Morphine is an opioid alkaloid, isolated from opium, with a complex ring structure. [GOC:ef, GOC:jl] |
| negative regulation of blood pressure | biological process | Any process in which the force of blood traveling through the circulatory system is decreased. [GOC:go_curators, GOC:mtg_cardio] |
| positive regulation of mitotic nuclear division | biological process | Any process that activates or increases the frequency, rate or extent of mitosis. [GOC:go_curators] |
| acid secretion | biological process | The controlled release of acid by a cell or a tissue. [GOC:ai] |
| behavioral response to cocaine | biological process | Any process that results in a change in the behavior of an organism as a result of a cocaine stimulus. [GOC:jid] |
| negative regulation of oligodendrocyte differentiation | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of oligodendrocyte differentiation. [GOC:vp, PMID:15139015] |
| arachidonic acid secretion | biological process | The controlled release of arachidonic acid from a cell or a tissue. [GOC:ai] |
| negative regulation of protein secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the controlled release of a protein from a cell. [GOC:ai] |
| musculoskeletal movement, spinal reflex action | biological process | Involuntary movement caused by the application of a stimulus to an organism and a subsequent movement. The signal processing of this movement takes place in the spinal cord. [GOC:dph] |
| regulation of dopamine uptake involved in synaptic transmission | biological process | Any process that modulates the frequency, rate or extent of the directed movement of the catecholamine neurotransmitter dopamine into a cell. [GOC:ai] |
| negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| prepulse inhibition | biological process | The process in which a startle magnitude is reduced when the startling stimulus is preceded by a low-intensity prepulse. [GOC:dph, PMID:10341260] |
| positive regulation of dopamine receptor signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of the dopamine receptor protein signaling pathway. A dopamine receptor signaling pathway is the series of molecular signals generated as a consequence of a dopamine receptor binding to one of its physiological ligands. [GOC:dph] |
| negative regulation of adenylate cyclase activity | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of adenylate cyclase activity. [GOC:go_curators] |
| adenylate cyclase-activating adrenergic receptor signaling pathway | biological process | An adenylate cyclase-activating G protein-coupled receptor signaling pathway initiated by a ligand binding to an adrenergic receptor on the surface of the target cell, and ending with the regulation of a downstream cellular process. [GOC:BHF, GOC:mah, GOC:signaling] |
| negative regulation of voltage-gated calcium channel activity | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of voltage-gated calcium channel activity. [GOC:BHF, GOC:TermGenie] |
| regulation of potassium ion transport | biological process | Any process that modulates the frequency, rate or extent of the directed movement of potassium ions (K+) into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:jl] |
| phospholipase C-activating dopamine receptor signaling pathway | biological process | A phospholipase C-activating receptor G protein-coupled receptor signaling pathway initiated by dopamine binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:dph, GOC:signaling, GOC:tb, PMID:12675914] |
| positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
| negative regulation of cytosolic calcium ion concentration | biological process | Any process that decreases the concentration of calcium ions in the cytosol. [GOC:ai] |
| negative regulation of synaptic transmission, glutamatergic | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of glutamatergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter glutamate. [GOC:ai] |