Page last updated: 2024-08-07 16:40:26
Alpha-1A adrenergic receptor
An alpha-1A adrenergic receptor that is encoded in the genome of rat. [OMA:P43140, PRO:DNx]
Synonyms
Alpha-1A adrenoreceptor;
Alpha-1A adrenoceptor;
Alpha-1C adrenergic receptor
Research
Bioassay Publications (188)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 41 (21.81) | 18.7374 |
| 1990's | 68 (36.17) | 18.2507 |
| 2000's | 42 (22.34) | 29.6817 |
| 2010's | 34 (18.09) | 24.3611 |
| 2020's | 3 (1.60) | 2.80 |
Compounds (278)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| melatonin | Rattus norvegicus (Norway rat) | IC50 | 0.0005 | 1 | 1 |
| 8-hydroxy-2-(di-n-propylamino)tetralin | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 5 |
| 8-hydroxy-2-(di-n-propylamino)tetralin | Rattus norvegicus (Norway rat) | Ki | 1.5410 | 2 | 2 |
| 1-(2-methoxyphenyl)piperazine | Rattus norvegicus (Norway rat) | Ki | 2.7585 | 2 | 4 |
| 1-(3-chlorophenyl)piperazine | Rattus norvegicus (Norway rat) | Ki | 0.2360 | 1 | 1 |
| 3-methylcholanthrene | Rattus norvegicus (Norway rat) | IC50 | 5.5440 | 1 | 0 |
| 3-methylcholanthrene | Rattus norvegicus (Norway rat) | Ki | 3.1340 | 1 | 0 |
| 4-nonylphenol | Rattus norvegicus (Norway rat) | IC50 | 1.9150 | 1 | 0 |
| 4-nonylphenol | Rattus norvegicus (Norway rat) | Ki | 1.0820 | 1 | 0 |
| 6-fluoronorepinephrine | Rattus norvegicus (Norway rat) | Ki | 0.9250 | 2 | 2 |
| amiodarone | Rattus norvegicus (Norway rat) | IC50 | 17.5470 | 1 | 0 |
| amiodarone | Rattus norvegicus (Norway rat) | Ki | 9.9180 | 1 | 0 |
| dan 2163 | Rattus norvegicus (Norway rat) | Ki | 0.0126 | 1 | 1 |
| amitriptyline | Rattus norvegicus (Norway rat) | IC50 | 0.0000 | 1 | 1 |
| astemizole | Rattus norvegicus (Norway rat) | IC50 | 29.1200 | 1 | 0 |
| astemizole | Rattus norvegicus (Norway rat) | Ki | 16.4610 | 1 | 0 |
| azelastine | Rattus norvegicus (Norway rat) | Ki | 0.0501 | 1 | 1 |
| benextramine | Rattus norvegicus (Norway rat) | IC50 | 4.0200 | 1 | 1 |
| benzbromarone | Rattus norvegicus (Norway rat) | IC50 | 5.2220 | 1 | 0 |
| benzbromarone | Rattus norvegicus (Norway rat) | Ki | 2.9520 | 1 | 0 |
| bithionol | Rattus norvegicus (Norway rat) | IC50 | 0.8290 | 1 | 0 |
| bithionol | Rattus norvegicus (Norway rat) | Ki | 0.4680 | 1 | 0 |
| bmy 7378 | Rattus norvegicus (Norway rat) | Ki | 0.3544 | 5 | 7 |
| brimonidine | Rattus norvegicus (Norway rat) | Ki | 0.7400 | 1 | 1 |
| buspirone | Rattus norvegicus (Norway rat) | IC50 | 7.0200 | 3 | 8 |
| buspirone | Rattus norvegicus (Norway rat) | Ki | 0.2520 | 2 | 3 |
| candesartan | Rattus norvegicus (Norway rat) | IC50 | 1.2199 | 1 | 0 |
| candesartan | Rattus norvegicus (Norway rat) | Ki | 0.6895 | 1 | 0 |
| celecoxib | Rattus norvegicus (Norway rat) | IC50 | 24.6220 | 1 | 0 |
| celecoxib | Rattus norvegicus (Norway rat) | Ki | 13.9170 | 1 | 0 |
| chlorpromazine | Rattus norvegicus (Norway rat) | IC50 | 0.0310 | 2 | 2 |
| chlorpromazine | Rattus norvegicus (Norway rat) | Ki | 0.0100 | 1 | 1 |
| ciglitazone | Rattus norvegicus (Norway rat) | IC50 | 3.0470 | 1 | 0 |
| ciglitazone | Rattus norvegicus (Norway rat) | Ki | 1.7220 | 1 | 0 |
| cisapride | Rattus norvegicus (Norway rat) | IC50 | 2.2900 | 2 | 2 |
| clomipramine | Rattus norvegicus (Norway rat) | IC50 | 0.0000 | 1 | 1 |
| clomipramine | Rattus norvegicus (Norway rat) | Ki | 0.0750 | 1 | 1 |
| clonidine | Rattus norvegicus (Norway rat) | Ki | 0.3757 | 6 | 7 |
| clotrimazole | Rattus norvegicus (Norway rat) | IC50 | 4.7520 | 1 | 0 |
| clotrimazole | Rattus norvegicus (Norway rat) | Ki | 2.6860 | 1 | 0 |
| desipramine | Rattus norvegicus (Norway rat) | IC50 | 0.0002 | 1 | 1 |
| disulfiram | Rattus norvegicus (Norway rat) | IC50 | 0.3560 | 1 | 0 |
| disulfiram | Rattus norvegicus (Norway rat) | Ki | 0.2010 | 1 | 0 |
| doxazosin | Rattus norvegicus (Norway rat) | IC50 | 0.0007 | 1 | 1 |
| doxazosin | Rattus norvegicus (Norway rat) | Ki | 0.0020 | 1 | 3 |
| doxepin | Rattus norvegicus (Norway rat) | IC50 | 0.0000 | 1 | 1 |
| ebastine | Rattus norvegicus (Norway rat) | IC50 | 1.1871 | 2 | 2 |
| ebastine | Rattus norvegicus (Norway rat) | Ki | 1.8061 | 1 | 0 |
| econazole | Rattus norvegicus (Norway rat) | IC50 | 3.2490 | 1 | 0 |
| econazole | Rattus norvegicus (Norway rat) | Ki | 1.8360 | 1 | 0 |
| felodipine | Rattus norvegicus (Norway rat) | IC50 | 1.0570 | 1 | 0 |
| felodipine | Rattus norvegicus (Norway rat) | Ki | 0.5970 | 1 | 0 |
| fenofibrate | Rattus norvegicus (Norway rat) | IC50 | 5.7010 | 1 | 0 |
| fenofibrate | Rattus norvegicus (Norway rat) | Ki | 3.2220 | 1 | 0 |
| fluphenazine | Rattus norvegicus (Norway rat) | IC50 | 11.9350 | 1 | 0 |
| fluphenazine | Rattus norvegicus (Norway rat) | Ki | 6.7460 | 1 | 0 |
| fluoxetine | Rattus norvegicus (Norway rat) | IC50 | 0.1000 | 1 | 1 |
| fluoxetine | Rattus norvegicus (Norway rat) | Ki | 3.2820 | 3 | 3 |
| haloperidol | Rattus norvegicus (Norway rat) | IC50 | 0.0852 | 4 | 5 |
| haloperidol | Rattus norvegicus (Norway rat) | Ki | 0.0142 | 10 | 12 |
| haloprogin | Rattus norvegicus (Norway rat) | IC50 | 0.2230 | 1 | 0 |
| haloprogin | Rattus norvegicus (Norway rat) | Ki | 0.1260 | 1 | 0 |
| hexachlorophene | Rattus norvegicus (Norway rat) | IC50 | 0.6389 | 1 | 0 |
| hexachlorophene | Rattus norvegicus (Norway rat) | Ki | 0.3611 | 1 | 0 |
| hydroxyzine | Rattus norvegicus (Norway rat) | Ki | 0.1750 | 2 | 2 |
| ifenprodil | Rattus norvegicus (Norway rat) | IC50 | 0.1050 | 2 | 2 |
| imipramine | Rattus norvegicus (Norway rat) | IC50 | 0.1600 | 1 | 1 |
| imipramine | Rattus norvegicus (Norway rat) | Ki | 0.2200 | 1 | 1 |
| iodoquinol | Rattus norvegicus (Norway rat) | IC50 | 0.9330 | 1 | 0 |
| iodoquinol | Rattus norvegicus (Norway rat) | Ki | 0.5270 | 1 | 0 |
| isoproterenol | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| isoproterenol | Rattus norvegicus (Norway rat) | Ki | 35.5000 | 1 | 1 |
| jl 18 | Rattus norvegicus (Norway rat) | Ki | 0.1080 | 1 | 1 |
| nsc 664704 | Rattus norvegicus (Norway rat) | IC50 | 0.0640 | 1 | 1 |
| ketanserin | Rattus norvegicus (Norway rat) | IC50 | 0.0150 | 1 | 1 |
| ketanserin | Rattus norvegicus (Norway rat) | Ki | 0.0100 | 1 | 1 |
| kojic acid | Rattus norvegicus (Norway rat) | IC50 | 2.0000 | 1 | 1 |
| loxapine | Rattus norvegicus (Norway rat) | IC50 | 0.0180 | 1 | 1 |
| methiothepin | Rattus norvegicus (Norway rat) | Ki | 0.0046 | 1 | 1 |
| metoclopramide | Rattus norvegicus (Norway rat) | IC50 | 20.3000 | 2 | 2 |
| mianserin | Rattus norvegicus (Norway rat) | IC50 | 0.1900 | 2 | 2 |
| mianserin | Rattus norvegicus (Norway rat) | Ki | 0.0750 | 3 | 4 |
| miconazole | Rattus norvegicus (Norway rat) | IC50 | 2.8110 | 1 | 0 |
| miconazole | Rattus norvegicus (Norway rat) | Ki | 1.5890 | 1 | 0 |
| mirtazapine | Rattus norvegicus (Norway rat) | IC50 | 0.2239 | 1 | 1 |
| mirtazapine | Rattus norvegicus (Norway rat) | Ki | 0.8290 | 2 | 2 |
| mitotane | Rattus norvegicus (Norway rat) | IC50 | 7.4450 | 1 | 0 |
| mitotane | Rattus norvegicus (Norway rat) | Ki | 4.2080 | 1 | 0 |
| 1-(3-trifluoromethylphenyl)piperazine | Rattus norvegicus (Norway rat) | Ki | 0.3370 | 1 | 1 |
| nan 190 | Rattus norvegicus (Norway rat) | Ki | 0.0008 | 3 | 6 |
| nifedipine | Rattus norvegicus (Norway rat) | IC50 | 7.2140 | 1 | 0 |
| nifedipine | Rattus norvegicus (Norway rat) | Ki | 4.0780 | 1 | 0 |
| nisoldipine | Rattus norvegicus (Norway rat) | IC50 | 7.1200 | 1 | 0 |
| nisoldipine | Rattus norvegicus (Norway rat) | Ki | 4.0240 | 1 | 0 |
| nortriptyline | Rattus norvegicus (Norway rat) | IC50 | 0.0000 | 1 | 1 |
| ondansetron | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| oxymetazoline | Rattus norvegicus (Norway rat) | Ki | 0.3311 | 1 | 1 |
| phenoxybenzamine | Rattus norvegicus (Norway rat) | Ki | 0.0018 | 1 | 1 |
| phenylpropanolamine | Rattus norvegicus (Norway rat) | Ki | 9.7724 | 1 | 1 |
| szl 49 | Rattus norvegicus (Norway rat) | IC50 | 0.0076 | 1 | 2 |
| prazosin | Rattus norvegicus (Norway rat) | IC50 | 0.0008 | 7 | 11 |
| prazosin | Rattus norvegicus (Norway rat) | Ki | 0.0003 | 12 | 13 |
| propranolol | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| quetiapine | Rattus norvegicus (Norway rat) | Ki | 0.8300 | 1 | 1 |
| rabeprazole | Rattus norvegicus (Norway rat) | IC50 | 3.2190 | 1 | 0 |
| rabeprazole | Rattus norvegicus (Norway rat) | Ki | 1.8200 | 1 | 0 |
| risperidone | Rattus norvegicus (Norway rat) | Ki | 0.0175 | 9 | 10 |
| ritanserin | Rattus norvegicus (Norway rat) | IC50 | 0.0470 | 3 | 3 |
| ritanserin | Rattus norvegicus (Norway rat) | Ki | 0.0290 | 1 | 2 |
| saccharin | Rattus norvegicus (Norway rat) | Ki | 10.0600 | 1 | 1 |
| sb 206553 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| spiperone | Rattus norvegicus (Norway rat) | IC50 | 0.0970 | 1 | 1 |
| spiperone | Rattus norvegicus (Norway rat) | Ki | 0.0072 | 1 | 2 |
| spiroxatrine | Rattus norvegicus (Norway rat) | Ki | 0.5995 | 1 | 4 |
| vorinostat | Rattus norvegicus (Norway rat) | IC50 | 2.8000 | 1 | 1 |
| sulconazole | Rattus norvegicus (Norway rat) | IC50 | 2.6280 | 1 | 0 |
| sulconazole | Rattus norvegicus (Norway rat) | Ki | 1.4850 | 1 | 0 |
| sumatriptan | Rattus norvegicus (Norway rat) | IC50 | 0.6400 | 1 | 1 |
| terazosin | Rattus norvegicus (Norway rat) | Ki | 0.0726 | 3 | 3 |
| terfenadine | Rattus norvegicus (Norway rat) | IC50 | 2.3400 | 1 | 2 |
| tetrahydropapaverine | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 2 |
| thioridazine | Rattus norvegicus (Norway rat) | IC50 | 0.0650 | 2 | 2 |
| tolazoline | Rattus norvegicus (Norway rat) | IC50 | 2.1000 | 1 | 1 |
| trazodone | Rattus norvegicus (Norway rat) | IC50 | 0.2810 | 1 | 1 |
| trifluoperazine | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| troglitazone | Rattus norvegicus (Norway rat) | IC50 | 5.2080 | 1 | 0 |
| troglitazone | Rattus norvegicus (Norway rat) | Ki | 2.9430 | 1 | 0 |
| urapidil | Rattus norvegicus (Norway rat) | Ki | 0.1279 | 1 | 1 |
| 5-methylurapidil | Rattus norvegicus (Norway rat) | Ki | 0.0007 | 1 | 2 |
| n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamide | Rattus norvegicus (Norway rat) | Ki | 0.0890 | 1 | 1 |
| wb 4101 | Rattus norvegicus (Norway rat) | Ki | 0.0022 | 3 | 5 |
| ici 204,219 | Rattus norvegicus (Norway rat) | IC50 | 1.3630 | 1 | 0 |
| ici 204,219 | Rattus norvegicus (Norway rat) | Ki | 0.7700 | 1 | 0 |
| zotepine | Rattus norvegicus (Norway rat) | Ki | 0.3300 | 1 | 1 |
| phentolamine | Rattus norvegicus (Norway rat) | IC50 | 0.0316 | 6 | 7 |
| phentolamine | Rattus norvegicus (Norway rat) | Ki | 0.0154 | 4 | 4 |
| physostigmine | Rattus norvegicus (Norway rat) | IC50 | 0.8570 | 1 | 1 |
| ethinyl estradiol | Rattus norvegicus (Norway rat) | IC50 | 32.9250 | 1 | 0 |
| ethinyl estradiol | Rattus norvegicus (Norway rat) | Ki | 18.6100 | 1 | 0 |
| apomorphine | Rattus norvegicus (Norway rat) | IC50 | 7.7500 | 1 | 1 |
| piperoxan | Rattus norvegicus (Norway rat) | IC50 | 0.7200 | 1 | 1 |
| phenylephrine | Rattus norvegicus (Norway rat) | Ki | 3.1311 | 2 | 2 |
| methylene blue | Rattus norvegicus (Norway rat) | IC50 | 0.5000 | 1 | 1 |
| 17-alpha-hydroxyprogesterone | Rattus norvegicus (Norway rat) | IC50 | 4.7300 | 1 | 0 |
| 17-alpha-hydroxyprogesterone | Rattus norvegicus (Norway rat) | Ki | 2.6740 | 1 | 0 |
| phenylpiperazine | Rattus norvegicus (Norway rat) | Ki | 0.7940 | 1 | 1 |
| phenothiazine | Rattus norvegicus (Norway rat) | IC50 | 25.6400 | 1 | 0 |
| phenothiazine | Rattus norvegicus (Norway rat) | Ki | 14.4920 | 1 | 0 |
| dibenzothiazyl disulfide | Rattus norvegicus (Norway rat) | IC50 | 0.3470 | 1 | 0 |
| dibenzothiazyl disulfide | Rattus norvegicus (Norway rat) | Ki | 0.1960 | 1 | 0 |
| sterogenol | Rattus norvegicus (Norway rat) | IC50 | 4.7580 | 1 | 0 |
| sterogenol | Rattus norvegicus (Norway rat) | Ki | 2.6890 | 1 | 0 |
| azapetine | Rattus norvegicus (Norway rat) | IC50 | 0.2050 | 1 | 1 |
| yohimbine | Rattus norvegicus (Norway rat) | IC50 | 1.3000 | 1 | 1 |
| yohimbine | Rattus norvegicus (Norway rat) | Ki | 0.3886 | 3 | 4 |
| n-phenethylpiperidine | Rattus norvegicus (Norway rat) | Ki | 7.5000 | 1 | 2 |
| phenylpropanolamine | Rattus norvegicus (Norway rat) | Ki | 9.8000 | 1 | 1 |
| gentian violet | Rattus norvegicus (Norway rat) | IC50 | 4.1660 | 1 | 0 |
| gentian violet | Rattus norvegicus (Norway rat) | Ki | 2.3550 | 1 | 0 |
| 1-naphthylisothiocyanate | Rattus norvegicus (Norway rat) | IC50 | 6.1000 | 1 | 0 |
| 1-naphthylisothiocyanate | Rattus norvegicus (Norway rat) | Ki | 3.4480 | 1 | 0 |
| vancomycin | Rattus norvegicus (Norway rat) | Ki | 1.0000 | 1 | 1 |
| fluanisone | Rattus norvegicus (Norway rat) | Ki | 0.0009 | 2 | 3 |
| 4-octylphenol | Rattus norvegicus (Norway rat) | IC50 | 6.0140 | 1 | 0 |
| 4-octylphenol | Rattus norvegicus (Norway rat) | Ki | 3.3990 | 1 | 0 |
| 2-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine | Rattus norvegicus (Norway rat) | IC50 | 0.0640 | 1 | 1 |
| tetrahydropapaveroline | Rattus norvegicus (Norway rat) | Ki | 40.0000 | 1 | 2 |
| stanozolol | Rattus norvegicus (Norway rat) | IC50 | 8.3250 | 1 | 0 |
| stanozolol | Rattus norvegicus (Norway rat) | Ki | 4.7050 | 1 | 0 |
| danazol | Rattus norvegicus (Norway rat) | IC50 | 11.1600 | 1 | 0 |
| danazol | Rattus norvegicus (Norway rat) | Ki | 6.3090 | 1 | 0 |
| 1-deoxynojirimycin | Rattus norvegicus (Norway rat) | IC50 | 1.3000 | 1 | 1 |
| canadine | Rattus norvegicus (Norway rat) | Ki | 1.1220 | 1 | 1 |
| closantel | Rattus norvegicus (Norway rat) | IC50 | 0.0960 | 1 | 0 |
| closantel | Rattus norvegicus (Norway rat) | Ki | 0.0540 | 1 | 0 |
| st 1059 | Rattus norvegicus (Norway rat) | Ki | 1.9984 | 2 | 3 |
| idazoxan | Rattus norvegicus (Norway rat) | IC50 | 0.0195 | 1 | 1 |
| idazoxan | Rattus norvegicus (Norway rat) | Ki | 0.6787 | 3 | 4 |
| tiospirone | Rattus norvegicus (Norway rat) | Ki | 0.0015 | 1 | 1 |
| sertindole | Rattus norvegicus (Norway rat) | IC50 | 0.0034 | 2 | 2 |
| besipirdine | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 2 |
| eliprodil | Rattus norvegicus (Norway rat) | IC50 | 3.3000 | 1 | 4 |
| delequamine | Rattus norvegicus (Norway rat) | Ki | 10.2329 | 1 | 2 |
| fananserin | Rattus norvegicus (Norway rat) | Ki | 0.0280 | 4 | 5 |
| aripiprazole | Rattus norvegicus (Norway rat) | Ki | 0.0132 | 3 | 3 |
| ziprasidone | Rattus norvegicus (Norway rat) | Ki | 0.0151 | 4 | 4 |
| nelfinavir | Rattus norvegicus (Norway rat) | IC50 | 17.3480 | 2 | 1 |
| nelfinavir | Rattus norvegicus (Norway rat) | Ki | 8.3630 | 1 | 0 |
| norharman | Rattus norvegicus (Norway rat) | IC50 | 15.0000 | 1 | 1 |
| amprenavir | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| irindalone | Rattus norvegicus (Norway rat) | IC50 | 0.3480 | 1 | 2 |
| prazosin hydrochloride | Rattus norvegicus (Norway rat) | Ki | 0.0035 | 1 | 1 |
| mianserin hydrochloride | Rattus norvegicus (Norway rat) | IC50 | 1.2000 | 1 | 1 |
| medetomidine | Rattus norvegicus (Norway rat) | Ki | 1.1100 | 1 | 1 |
| setoperone | Rattus norvegicus (Norway rat) | Ki | 0.0120 | 1 | 1 |
| mezilamine | Rattus norvegicus (Norway rat) | Ki | 0.0910 | 1 | 1 |
| etisulergine | Rattus norvegicus (Norway rat) | IC50 | 3.3000 | 1 | 1 |
| mesulergine | Rattus norvegicus (Norway rat) | Ki | 0.0019 | 2 | 2 |
| tefludazine | Rattus norvegicus (Norway rat) | IC50 | 0.0170 | 1 | 1 |
| atipamezole | Rattus norvegicus (Norway rat) | Ki | 1.9953 | 1 | 1 |
| lopinavir | Rattus norvegicus (Norway rat) | IC50 | 10.3000 | 1 | 1 |
| cp-55,940 | Rattus norvegicus (Norway rat) | Ki | 0.0130 | 1 | 1 |
| gr 127935 | Rattus norvegicus (Norway rat) | Ki | 1.0000 | 1 | 1 |
| 6-chloro-2-(1-piperazinyl)pyrazine | Rattus norvegicus (Norway rat) | Ki | 0.9130 | 1 | 1 |
| alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol | Rattus norvegicus (Norway rat) | IC50 | 0.8267 | 3 | 3 |
| st 587 | Rattus norvegicus (Norway rat) | Ki | 65.8000 | 1 | 2 |
| way 100135 | Rattus norvegicus (Norway rat) | IC50 | 1.4910 | 1 | 2 |
| 3-n-methylspiperone | Rattus norvegicus (Norway rat) | IC50 | 0.0101 | 1 | 1 |
| mosapride | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 2 | 2 |
| uh 301 | Rattus norvegicus (Norway rat) | Ki | 6.0800 | 1 | 1 |
| 5-fluorodopamine | Rattus norvegicus (Norway rat) | Ki | 6.0000 | 1 | 1 |
| a 68930 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| l 687384 | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 1 |
| mcn 5707 | Rattus norvegicus (Norway rat) | Ki | 0.3110 | 1 | 3 |
| 5,6-dihydroxy-1-(2-imidazolinyl)tetralin | Rattus norvegicus (Norway rat) | Ki | 0.4000 | 1 | 2 |
| tamsulosin | Rattus norvegicus (Norway rat) | Ki | 0.0001 | 3 | 3 |
| 4-(benzodioxan-5-yl)-1-(indan-2-yl)piperazine | Rattus norvegicus (Norway rat) | Ki | 0.1399 | 2 | 4 |
| dc 015 | Rattus norvegicus (Norway rat) | Ki | 0.0002 | 2 | 2 |
| sonepiprazole | Rattus norvegicus (Norway rat) | Ki | 4.9000 | 1 | 3 |
| ciladopa | Rattus norvegicus (Norway rat) | IC50 | 1.0900 | 1 | 2 |
| atazanavir | Rattus norvegicus (Norway rat) | IC50 | 67.8000 | 1 | 1 |
| homonojirimycin | Rattus norvegicus (Norway rat) | IC50 | 0.7000 | 1 | 1 |
| n,n-di-n-propylserotonin | Rattus norvegicus (Norway rat) | IC50 | 0.8200 | 1 | 1 |
| 3-fluoronorepinephrine | Rattus norvegicus (Norway rat) | Ki | 32.6667 | 3 | 3 |
| cilengitide | Rattus norvegicus (Norway rat) | IC50 | 0.0005 | 1 | 1 |
| f 1394 | Rattus norvegicus (Norway rat) | IC50 | 0.0320 | 1 | 1 |
| 2-fluorodopamine | Rattus norvegicus (Norway rat) | Ki | 16.0000 | 1 | 1 |
| bmy 7378 | Rattus norvegicus (Norway rat) | Ki | 0.0017 | 1 | 1 |
| darunavir | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| cp 101,606 | Rattus norvegicus (Norway rat) | IC50 | 12.6100 | 1 | 2 |
| estradiol 3-benzoate | Rattus norvegicus (Norway rat) | IC50 | 21.7800 | 1 | 0 |
| estradiol 3-benzoate | Rattus norvegicus (Norway rat) | Ki | 12.3120 | 1 | 0 |
| epitrate | Rattus norvegicus (Norway rat) | Ki | 20.0000 | 1 | 1 |
| paullone | Rattus norvegicus (Norway rat) | IC50 | 0.8100 | 1 | 1 |
| ritonavir | Rattus norvegicus (Norway rat) | IC50 | 39.6000 | 1 | 1 |
| (R)-norlaudanosoline | Rattus norvegicus (Norway rat) | Ki | 25.0000 | 1 | 2 |
| saquinavir | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| tretinoin | Rattus norvegicus (Norway rat) | IC50 | 5.2750 | 1 | 0 |
| tretinoin | Rattus norvegicus (Norway rat) | Ki | 0.7458 | 2 | 3 |
| diethylstilbestrol | Rattus norvegicus (Norway rat) | IC50 | 2.2080 | 1 | 0 |
| diethylstilbestrol | Rattus norvegicus (Norway rat) | Ki | 1.2480 | 1 | 0 |
| 2-(1-piperazinyl)-4-amino-6,7-dimethoxyquinazoline | Rattus norvegicus (Norway rat) | IC50 | 0.3400 | 1 | 1 |
| rauwolscine | Rattus norvegicus (Norway rat) | Ki | 0.3162 | 1 | 2 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Rattus norvegicus (Norway rat) | IC50 | 3.7058 | 1 | 0 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Rattus norvegicus (Norway rat) | Ki | 2.0946 | 1 | 0 |
| levosulpiride | Rattus norvegicus (Norway rat) | Ki | 15.0000 | 1 | 1 |
| flunarizine | Rattus norvegicus (Norway rat) | IC50 | 5.1980 | 1 | 0 |
| flunarizine | Rattus norvegicus (Norway rat) | Ki | 2.9380 | 1 | 0 |
| curcumin | Rattus norvegicus (Norway rat) | IC50 | 5.4000 | 1 | 1 |
| enclomiphene | Rattus norvegicus (Norway rat) | IC50 | 5.3500 | 1 | 0 |
| enclomiphene | Rattus norvegicus (Norway rat) | Ki | 3.0240 | 1 | 0 |
| thioguanine anhydrous | Rattus norvegicus (Norway rat) | IC50 | 21.6870 | 1 | 0 |
| thioguanine anhydrous | Rattus norvegicus (Norway rat) | Ki | 12.2580 | 1 | 0 |
| tamoxifen | Rattus norvegicus (Norway rat) | IC50 | 3.7010 | 1 | 0 |
| tamoxifen | Rattus norvegicus (Norway rat) | Ki | 2.0920 | 1 | 0 |
| altanserin | Rattus norvegicus (Norway rat) | Ki | 0.0050 | 1 | 1 |
| mcn 5652 | Rattus norvegicus (Norway rat) | Ki | 0.2670 | 1 | 3 |
| bp 897 | Rattus norvegicus (Norway rat) | Ki | 0.0600 | 1 | 1 |
| vx-745 | Rattus norvegicus (Norway rat) | IC50 | 8.5470 | 1 | 0 |
| vx-745 | Rattus norvegicus (Norway rat) | Ki | 4.8310 | 1 | 0 |
| quinagolide | Rattus norvegicus (Norway rat) | IC50 | 7.9333 | 1 | 3 |
| n-(1-methyl-5-indolyl)-n'-(3-methyl-5-isothiazolyl)urea | Rattus norvegicus (Norway rat) | Ki | 3.1623 | 1 | 1 |
| sb-224289 | Rattus norvegicus (Norway rat) | Ki | 1.0000 | 1 | 1 |
| n-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3-methoxybenzamide | Rattus norvegicus (Norway rat) | Ki | 0.2450 | 1 | 1 |
| rs 102221 | Rattus norvegicus (Norway rat) | IC50 | 0.0015 | 1 | 1 |
| mm 77 | Rattus norvegicus (Norway rat) | Ki | 0.0119 | 1 | 1 |
| 3-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione | Rattus norvegicus (Norway rat) | Ki | 0.0002 | 4 | 4 |
| a 61603 | Rattus norvegicus (Norway rat) | Ki | 0.3462 | 3 | 4 |
| 2-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-6,7,8,8a-tetrahydro-5H-imidazo[1,5-a]pyridine-1,3-dione | Rattus norvegicus (Norway rat) | Ki | 0.1310 | 1 | 2 |
| 5-methoxycarbonylamino-n-acetyltryptamine | Rattus norvegicus (Norway rat) | IC50 | 4.0000 | 1 | 1 |
| montelukast | Rattus norvegicus (Norway rat) | IC50 | 0.4340 | 1 | 0 |
| montelukast | Rattus norvegicus (Norway rat) | Ki | 0.2450 | 1 | 0 |
| anandamide | Rattus norvegicus (Norway rat) | Ki | 0.0720 | 1 | 1 |
| isotretinoin | Rattus norvegicus (Norway rat) | IC50 | 4.1690 | 1 | 0 |
| isotretinoin | Rattus norvegicus (Norway rat) | Ki | 2.3570 | 1 | 0 |
| cyclosporine | Rattus norvegicus (Norway rat) | IC50 | 9.3400 | 1 | 1 |
| fenretinide | Rattus norvegicus (Norway rat) | Ki | 2.2000 | 1 | 3 |
| dexmedetomidine | Rattus norvegicus (Norway rat) | Ki | 0.0050 | 1 | 1 |
| lacidipine | Rattus norvegicus (Norway rat) | IC50 | 4.0360 | 1 | 0 |
| lacidipine | Rattus norvegicus (Norway rat) | Ki | 2.2810 | 1 | 0 |
| mdl 100907 | Rattus norvegicus (Norway rat) | Ki | 0.4200 | 1 | 2 |
| (3r)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone | Rattus norvegicus (Norway rat) | Ki | 0.0210 | 1 | 1 |
| silodosin | Rattus norvegicus (Norway rat) | IC50 | 0.0008 | 1 | 1 |
| sulindac sulfide | Rattus norvegicus (Norway rat) | IC50 | 7.2310 | 1 | 0 |
| sulindac sulfide | Rattus norvegicus (Norway rat) | Ki | 4.0870 | 1 | 0 |
| oxiconazole | Rattus norvegicus (Norway rat) | IC50 | 0.6345 | 1 | 0 |
| oxiconazole | Rattus norvegicus (Norway rat) | Ki | 0.3586 | 1 | 0 |
| indinavir sulfate | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| cp 135807 | Rattus norvegicus (Norway rat) | IC50 | 0.0330 | 1 | 1 |
| brecanavir | Rattus norvegicus (Norway rat) | IC50 | 24.1000 | 1 | 1 |
| gw 1929 | Rattus norvegicus (Norway rat) | IC50 | 14.3180 | 1 | 0 |
| gw 1929 | Rattus norvegicus (Norway rat) | Ki | 8.0930 | 1 | 0 |
| am 404 | Rattus norvegicus (Norway rat) | Ki | 1.7600 | 1 | 1 |
| stepholidine | Rattus norvegicus (Norway rat) | Ki | 2.2387 | 1 | 1 |
| cilansetron | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| pd 174494 | Rattus norvegicus (Norway rat) | IC50 | 27.0000 | 1 | 4 |
| rwj 52353 | Rattus norvegicus (Norway rat) | Ki | 0.4430 | 2 | 2 |
| lu 28-179 | Rattus norvegicus (Norway rat) | IC50 | 0.3300 | 1 | 1 |
| abt 866 | Rattus norvegicus (Norway rat) | Ki | 0.1375 | 2 | 2 |
| vn2222 | Rattus norvegicus (Norway rat) | Ki | 0.0350 | 1 | 1 |
| slv 313 | Rattus norvegicus (Norway rat) | Ki | 0.0040 | 1 | 1 |
| ngb 2904 | Rattus norvegicus (Norway rat) | Ki | 0.6420 | 1 | 1 |
| kni 10006 | Rattus norvegicus (Norway rat) | Ki | 0.0005 | 1 | 1 |
| pnu 96415e | Rattus norvegicus (Norway rat) | Ki | 0.0380 | 1 | 3 |
| mk 936 | Rattus norvegicus (Norway rat) | IC50 | 0.8700 | 1 | 0 |
| mk 936 | Rattus norvegicus (Norway rat) | Ki | 0.4920 | 1 | 0 |
| st 1936 | Rattus norvegicus (Norway rat) | Ki | 0.3000 | 1 | 1 |
| ps1145 | Rattus norvegicus (Norway rat) | IC50 | 0.1000 | 1 | 1 |
| n,n-dipropyl-2-(4-methoxy-3-(2-phenylethoxy)phenyl)ethylamine monohydrochloride | Rattus norvegicus (Norway rat) | IC50 | 10.8000 | 1 | 1 |
| 4-(6-iodo-2-imidazo[1,2-a]pyridinyl)-N,N-dimethylaniline | Rattus norvegicus (Norway rat) | Ki | 0.0150 | 1 | 1 |
| PB28 | Rattus norvegicus (Norway rat) | Ki | 7.5000 | 1 | 2 |
| 1-(2,4-difluorophenethyl)-4-(4-fluorophenylsulfonyl)piperidine | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 1 | 2 |
| cariprazine | Rattus norvegicus (Norway rat) | Ki | 0.1550 | 1 | 1 |
| n-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide | Rattus norvegicus (Norway rat) | Ki | 0.0116 | 2 | 2 |
| tetracycline | Rattus norvegicus (Norway rat) | IC50 | 180.0000 | 1 | 1 |
| clozapine | Rattus norvegicus (Norway rat) | IC50 | 0.0567 | 7 | 8 |
| clozapine | Rattus norvegicus (Norway rat) | Ki | 0.0865 | 9 | 11 |
| olanzapine | Rattus norvegicus (Norway rat) | Ki | 2.4026 | 3 | 3 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| norepinephrine, (+,-)-isomer | Rattus norvegicus (Norway rat) | EC50 | 1.9000 | 2 | 2 |
| methylbufotenin | Rattus norvegicus (Norway rat) | Kd | 0.0794 | 1 | 1 |
| bmy 7378 | Rattus norvegicus (Norway rat) | Kd | 0.1148 | 1 | 1 |
| buspirone | Rattus norvegicus (Norway rat) | EC50 | 0.0800 | 1 | 1 |
| chloroxine | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| clioquinol | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| clonidine | Rattus norvegicus (Norway rat) | Kd | 0.2570 | 1 | 1 |
| doxazosin | Rattus norvegicus (Norway rat) | Kd | 0.0020 | 1 | 1 |
| ketanserin | Rattus norvegicus (Norway rat) | Kd | 0.0158 | 1 | 2 |
| mianserin | Rattus norvegicus (Norway rat) | Kd | 1.9740 | 2 | 2 |
| naftopidil | Rattus norvegicus (Norway rat) | Kd | 0.0331 | 1 | 1 |
| prazosin | Rattus norvegicus (Norway rat) | Kd | 0.0018 | 9 | 13 |
| propranolol | Rattus norvegicus (Norway rat) | Kd | 0.0148 | 1 | 1 |
| ritanserin | Rattus norvegicus (Norway rat) | Kd | 0.0316 | 1 | 2 |
| terazosin | Rattus norvegicus (Norway rat) | Kd | 0.0109 | 2 | 2 |
| tolazoline | Rattus norvegicus (Norway rat) | Kd | 2.1878 | 1 | 1 |
| wb 4101 | Rattus norvegicus (Norway rat) | Kd | 0.0005 | 2 | 3 |
| phentolamine | Rattus norvegicus (Norway rat) | EC50 | 1.0000 | 1 | 1 |
| phentolamine | Rattus norvegicus (Norway rat) | Kd | 0.0267 | 5 | 6 |
| piperoxan | Rattus norvegicus (Norway rat) | Kd | 1.0977 | 2 | 2 |
| 1-(2-pyridylazo)-2-naphthol | Rattus norvegicus (Norway rat) | EC50 | 25.7000 | 1 | 0 |
| azapetine | Rattus norvegicus (Norway rat) | Kd | 0.8128 | 1 | 1 |
| yohimbine | Rattus norvegicus (Norway rat) | Kd | 0.5543 | 5 | 8 |
| dihydroergotamine | Rattus norvegicus (Norway rat) | Kd | 0.2089 | 1 | 1 |
| idazoxan | Rattus norvegicus (Norway rat) | Kd | 0.7808 | 5 | 9 |
| gepirone | Rattus norvegicus (Norway rat) | EC50 | 0.2880 | 1 | 1 |
| medetomidine | Rattus norvegicus (Norway rat) | EC50 | 0.2810 | 1 | 1 |
| labetalol hydrochloride | Rattus norvegicus (Norway rat) | Kd | 0.0316 | 1 | 1 |
| 8-(4-tolylsulfonylamino)quinoline | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| corynanthine | Rattus norvegicus (Norway rat) | Kd | 0.5623 | 1 | 1 |
| 1-(2-pyridinyl)piperazine | Rattus norvegicus (Norway rat) | Kd | 1.9953 | 1 | 1 |
| rx 821002 | Rattus norvegicus (Norway rat) | Kd | 0.0589 | 1 | 2 |
| cyclazosin | Rattus norvegicus (Norway rat) | Kd | 0.0091 | 2 | 2 |
| idazoxan hydrochloride | Rattus norvegicus (Norway rat) | Kd | 1.0430 | 2 | 2 |
| corbadrine | Rattus norvegicus (Norway rat) | EC50 | 0.7760 | 1 | 1 |
| 2,3-dichloro-5,8-dimethoxy-1,4-naphthoquinone | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| rauwolscine | Rattus norvegicus (Norway rat) | Kd | 4.2929 | 2 | 2 |
| 5H-quinolino[8,7-c][1,2]benzothiazine 6,6-dioxide | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| 6-[2-(2-methoxyphenyl)imino-3-(2-oxolanylmethyl)-4-thiazolyl]-4H-1,4-benzoxazin-3-one | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| N-[2,2,2-trichloro-1-[[(2,6-dichloroanilino)-sulfanylidenemethyl]amino]ethyl]carbamic acid (phenylmethyl) ester | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| 4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| 2-[(5-methyl-4-phenyl-2-thiazolyl)methyl]-4-thiazolol | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| 2,5-dichloro-N-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]-3-thiophenecarboxamide | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| 7-hydroxyflavone | Rattus norvegicus (Norway rat) | Kd | 0.2460 | 1 | 1 |
| nalmefene | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| naloxone hydrochloride | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| naltrexone hydrochloride | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 0 |
| sodium selenate | Rattus norvegicus (Norway rat) | EC50 | 0.0013 | 1 | 1 |
| naluzotan | Rattus norvegicus (Norway rat) | EC50 | 0.0200 | 1 | 1 |
| 6-fluoronorepinephrine monohydrochloride, (+-)-isomer | Rattus norvegicus (Norway rat) | EC50 | 51.5000 | 2 | 2 |
| efaroxan hydrochloride | Rattus norvegicus (Norway rat) | Kd | 1.2303 | 1 | 1 |
| clozapine | Rattus norvegicus (Norway rat) | Kd | 0.5129 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| snap 6201 | Rattus norvegicus (Norway rat) | Kb | 0.7501 | 2 | 4 |
| l 701324 | Rattus norvegicus (Norway rat) | Kb | 0.0280 | 1 | 1 |
| mdl 104653 | Rattus norvegicus (Norway rat) | Kb | 0.8800 | 1 | 1 |
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor.Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4.Journal of medicinal chemistry, , Dec-06, Volume: 39, Issue:25, 1996
Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity.Journal of medicinal chemistry, , Nov-26, Volume: 36, Issue:24, 1993
Conformationally defined adrenergic agents. 1. Design and synthesis of novel alpha 2 selective adrenergic agents: electrostatic repulsion based conformational prototypes.Journal of medicinal chemistry, , Volume: 28, Issue:10, 1985
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor.Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Design, synthesis, and biological activity of prazosin-related antagonists. Role of the piperazine and furan units of prazosin on the selectivity for alpha1-adrenoreceptor subtypes.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.Journal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT(7) receptor ligands among phenylpiperazine hydantoin derivatives.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.Journal of medicinal chemistry, , Jun-01, Volume: 49, Issue:11, 2006
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Synthesis and structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist.Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
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(S)-N-tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
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
The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.Journal of medicinal chemistry, , Volume: 29, Issue:3, 1986
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Conformationally defined adrenergic agents. 5. Resolution, absolute configuration, and pharmacological characterization of the enantiomers of 2-(5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthyl)imidazoline: a potent agonist at alpha-adrenoceptors.Journal of medicinal chemistry, , Volume: 30, Issue:6, 1987
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Conformationally defined adrenergic agents. 1. Design and synthesis of novel alpha 2 selective adrenergic agents: electrostatic repulsion based conformational prototypes.Journal of medicinal chemistry, , Volume: 28, Issue:10, 1985
1-(alkylamino)isochromans: hypotensives with peripheral and central activities.Journal of medicinal chemistry, , Volume: 25, Issue:1, 1982
Design and synthesis of small molecule agonists of EphA2 receptor.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
2,4-diamino-6,7-dimethoxyquinazolines. 1. 2-[4-(1,4-benzodioxan-2-ylcarbonyl)piperazin-1-yl] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.Journal of medicinal chemistry, , Jul-15, Volume: 47, Issue:15, 2004
Potential antidepressants displayed combined alpha(2)-adrenoceptor antagonist and monoamine uptake inhibitor properties.Journal of medicinal chemistry, , Mar-01, Volume: 44, Issue:5, 2001
New indole derivatives as potent and selective serotonin uptake inhibitors.Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.Journal of medicinal chemistry, , Volume: 30, Issue:8, 1987
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
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
A rapid computational method for lead evolution: description and application to alpha(1)-adrenergic antagonists.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.Bioorganic & medicinal chemistry letters, , Apr-21, Volume: 8, Issue:8, 1998
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Novel potent sigma 1 ligands: N-[omega-(tetralin-1-yl)alkyl]piperidine derivatives.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
N-aryl-N'-benzylpiperazines as potential antipsychotic agents.Journal of medicinal chemistry, , Oct-13, Volume: 38, Issue:21, 1995
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.Journal of medicinal chemistry, , Nov-27, Volume: 35, Issue:24, 1992
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.Journal of medicinal chemistry, , Volume: 30, Issue:8, 1987
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Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Syntheses and 5-HT2 antagonist activity of bicyclic 1,2,4-triazol-3(2H)-one and 1,3,5-triazine-2,4(3H)-dione derivatives.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity.Journal of medicinal chemistry, , Volume: 31, Issue:12, 1988
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
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.Journal of medicinal chemistry, , Volume: 30, Issue:8, 1987
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.Journal of medicinal chemistry, , Volume: 27, Issue:4, 1984
Pyridinylpiperazines, a new class of selective alpha 2-adrenoceptor antagonists.Journal of medicinal chemistry, , Volume: 26, Issue:12, 1983
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
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 10, Issue:1, 2000
Synthesis, biological evaluation, and pharmacophore generation of new pyridazinone derivatives with affinity toward alpha(1)- and alpha(2)-adrenoceptors.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
Synthesis and structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist.Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, synthesis and biological evaluation of new arylpiperazine derivatives bearing a flavone moiety as α1-adrenoceptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 21, Issue:3, 2011
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Pharmacophore-based design, synthesis, biological evaluation, and 3D-QSAR studies of aryl-piperazines as alpha(1)-adrenoceptor antagonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 15, Issue:13, 2005
Alpha1-adrenoceptor antagonists. 6. Structural optimization of pyridazinone-arylpiperazines. Study of the influence on affinity and selectivity of cyclic substituents at the pyridazinone ring and alkoxy groups at the arylpiperazine moiety.Journal of medicinal chemistry, , Jul-31, Volume: 46, Issue:16, 2003
Synthesis, biological evaluation, and pharmacophore generation of new pyridazinone derivatives with affinity toward alpha(1)- and alpha(2)-adrenoceptors.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
A rapid computational method for lead evolution: description and application to alpha(1)-adrenergic antagonists.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
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
Design, synthesis, and biological activity of prazosin-related antagonists. Role of the piperazine and furan units of prazosin on the selectivity for alpha1-adrenoreceptor subtypes.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.Journal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4.Journal of medicinal chemistry, , Dec-06, Volume: 39, Issue:25, 1996
The furoxan system as a useful tool for balancing "hybrids" with mixed alpha 1-antagonist and NO-like vasodilator activities.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2.Journal of medicinal chemistry, , Mar-17, Volume: 38, Issue:6, 1995
Discovery of nanomolar ligands for 7-transmembrane G-protein-coupled receptors from a diverse N-(substituted)glycine peptoid library.Journal of medicinal chemistry, , Aug-19, Volume: 37, Issue:17, 1994
Alkylating prazosin analogue: irreversible label for alpha 1-adrenoceptors.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
Heteroaromatic analogues of the alpha 2-adrenoreceptor partial agonist clonidine.Journal of medicinal chemistry, , Volume: 32, Issue:7, 1989
Structure-activity relationships in prazosin-related compounds. Effect of replacing a piperazine ring with an alkanediamine moiety on alpha 1-adrenoreceptor blocking activity.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
1,3-Diamino-6,7-dimethoxyisoquinoline derivatives as potential alpha 1-adrenoceptor antagonists.Journal of medicinal chemistry, , Volume: 31, Issue:5, 1988
Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity.Journal of medicinal chemistry, , Volume: 31, Issue:12, 1988
2,4-Diamino-6,7-dimethoxyquinazolines. 2. 2-(4-Carbamoylpiperidino) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.Journal of medicinal chemistry, , Volume: 30, Issue:6, 1987
2,4-diamino-6,7-dimethoxyquinazolines. 1. 2-[4-(1,4-benzodioxan-2-ylcarbonyl)piperazin-1-yl] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.Journal of medicinal chemistry, , Volume: 27, Issue:4, 1984
alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.Journal of medicinal chemistry, , Volume: 26, Issue:6, 1983
1-(alkylamino)isochromans: hypotensives with peripheral and central activities.Journal of medicinal chemistry, , Volume: 25, Issue:1, 1982
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.Journal of medicinal chemistry, , Volume: 24, Issue:11, 1981
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 207, 2020
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
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
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
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.Bioorganic & medicinal chemistry letters, , Apr-21, Volume: 8, Issue:8, 1998
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Selective, centrally acting serotonin 5-HT2 antagonists. 2. Substituted 3-(4-fluorophenyl)-1H-indoles.Journal of medicinal chemistry, , Dec-25, Volume: 35, Issue:26, 1992
Syntheses and 5-HT2 antagonist activity of bicyclic 1,2,4-triazol-3(2H)-one and 1,3,5-triazine-2,4(3H)-dione derivatives.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.Journal of medicinal chemistry, , Dec-25, Volume: 35, Issue:26, 1992
Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists.Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity.Journal of medicinal chemistry, , Volume: 31, Issue:12, 1988
5-Methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2,3-f]indole: a novel 5-HT2C/5-HT2B receptor antagonist with improved affinity, selectivity, and oral activity.Journal of medicinal chemistry, , Jul-07, Volume: 38, Issue:14, 1995
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
[no title available]Bioorganic & medicinal chemistry letters, , 02-15, Volume: 28, Issue:4, 2018
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).Journal of medicinal chemistry, , Apr-20, Volume: 43, Issue:8, 2000
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.Journal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.Journal of medicinal chemistry, , Nov-27, Volume: 35, Issue:24, 1992
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.Journal of medicinal chemistry, , Volume: 29, Issue:3, 1986
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Structure-activity relationships in 1,4-benzodioxan-related compounds. 7. Selectivity of 4-phenylchroman analogues for alpha(1)-adrenoreceptor subtypes.Journal of medicinal chemistry, , Apr-11, Volume: 45, Issue:8, 2002
A rapid computational method for lead evolution: description and application to alpha(1)-adrenergic antagonists.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Structure-activity relationships in 1,4-benzodioxan-related compounds. 4. Effect of aryl and alkyl substituents at position 3 on alpha-adrenoreceptor blocking activity.Journal of medicinal chemistry, , May-28, Volume: 36, Issue:11, 1993
Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HTEuropean journal of medicinal chemistry, , Mar-10, Volume: 147, 2018
Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.Journal of medicinal chemistry, , Dec-06, Volume: 44, Issue:25, 2001
1-aryl-4-[(5-methoxy-1,2,3, 4-tetrahydronaphthalen-1-yl)alkyl]piperazines and their analogues: influence of the stereochemistry of the tetrahydronaphthalen-1-yl nucleus on 5-HT1A receptor affinity and selectivity versus alpha1 and D2 receptors. 5.Journal of medicinal chemistry, , Feb-11, Volume: 42, Issue:3, 1999
Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
[[(Arylpiperazinyl)alkyl]thio]thieno[2,3-d]pyrimidinone derivatives as high-affinity, selective 5-HT1A receptor ligands.Journal of medicinal chemistry, , Feb-14, Volume: 40, Issue:4, 1997
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.Journal of medicinal chemistry, , Volume: 27, Issue:4, 1984
alpha-Adrenergic activities of some substituted 2-(aminomethyl)imidazolines.Journal of medicinal chemistry, , Volume: 26, Issue:12, 1983
alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.Journal of medicinal chemistry, , Volume: 26, Issue:6, 1983
Syntheses and adrenergic agonist properties of ring-fluorinated isoproterenols.Journal of medicinal chemistry, , Volume: 25, Issue:6, 1982
1-(alkylamino)isochromans: hypotensives with peripheral and central activities.Journal of medicinal chemistry, , Volume: 25, Issue:1, 1982
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.Journal of medicinal chemistry, , Volume: 25, Issue:6, 1982
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.Journal of medicinal chemistry, , Volume: 24, Issue:11, 1981
Conformationally restricted tricyclic antidepressants. 1. Octahydrodibenzazepinonaphthyridines as rigid imipramine analogues.Journal of medicinal chemistry, , Volume: 23, Issue:8, 1980
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.Journal of medicinal chemistry, , Volume: 28, Issue:10, 1985
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity.Journal of medicinal chemistry, , Nov-26, Volume: 36, Issue:24, 1993
Structure-affinity relationships of 12-sulfonyl derivatives of 5,8,8a,9,10,11,12,12a,13,13a-decahydro-6H-isoquino[2,1-g][1 ,6] naphthyridines at alpha-adrenoceptors.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
(8a alpha,12a alpha,13a alpha)-5,8,8a,9,10,11,12,12a,13,13a-decahydro- 3-methoxy-12-(methylsulfonyl)-6H-isoquino[2,1-g][1,6]naphthyridi ne, a potent and highly selective alpha 2-adrenoceptor antagonist.Journal of medicinal chemistry, , Volume: 32, Issue:9, 1989
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.Journal of medicinal chemistry, , Volume: 29, Issue:8, 1986
Alpha-adrenoreceptor reagents. 2. Effects of modification of the 1,4-benzodioxan ring system on alpha-adrenoreceptor activity.Journal of medicinal chemistry, , Volume: 27, Issue:5, 1984
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.Journal of medicinal chemistry, , Volume: 27, Issue:4, 1984
Pyridinylpiperazines, a new class of selective alpha 2-adrenoceptor antagonists.Journal of medicinal chemistry, , Volume: 26, Issue:12, 1983
alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.Journal of medicinal chemistry, , Volume: 26, Issue:6, 1983
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.Journal of medicinal chemistry, , Volume: 24, Issue:11, 1981
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 10, Issue:1, 2000
Structure-activity relationships in 1,4-benzodioxan-related compounds. 4. Effect of aryl and alkyl substituents at position 3 on alpha-adrenoreceptor blocking activity.Journal of medicinal chemistry, , May-28, Volume: 36, Issue:11, 1993
Structure-affinity relationships of 12-sulfonyl derivatives of 5,8,8a,9,10,11,12,12a,13,13a-decahydro-6H-isoquino[2,1-g][1 ,6] naphthyridines at alpha-adrenoceptors.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
(8a alpha,12a alpha,13a alpha)-5,8,8a,9,10,11,12,12a,13,13a-decahydro- 3-methoxy-12-(methylsulfonyl)-6H-isoquino[2,1-g][1,6]naphthyridi ne, a potent and highly selective alpha 2-adrenoceptor antagonist.Journal of medicinal chemistry, , Volume: 32, Issue:9, 1989
Synthesis and alpha 2-adrenoceptor antagonist activity of some disulfonamidobenzoquinolizines.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.Journal of medicinal chemistry, , Volume: 30, Issue:9, 1987
Alpha-adrenoreceptor reagents. 3. Synthesis of some 2-substituted 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists.Journal of medicinal chemistry, , Volume: 28, Issue:8, 1985
Pyridinylpiperazines, a new class of selective alpha 2-adrenoceptor antagonists.Journal of medicinal chemistry, , Volume: 26, Issue:12, 1983
alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.Journal of medicinal chemistry, , Volume: 26, Issue:6, 1983
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.Journal of medicinal chemistry, , Dec-25, Volume: 35, Issue:26, 1992
Selective, centrally acting serotonin 5-HT2 antagonists. 2. Substituted 3-(4-fluorophenyl)-1H-indoles.Journal of medicinal chemistry, , Dec-25, Volume: 35, Issue:26, 1992
Structure-affinity relationships of 12-sulfonyl derivatives of 5,8,8a,9,10,11,12,12a,13,13a-decahydro-6H-isoquino[2,1-g][1 ,6] naphthyridines at alpha-adrenoceptors.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists.Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 207, 2020
Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT₁A/5-HT₂A/5-HT₇ and dopamine D₂/D₃ receptors.European journal of medicinal chemistry, , Volume: 60, 2013
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
1-Aminoindanes as novel motif with potential atypical antipsychotic properties.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket".Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 1996
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.Journal of medicinal chemistry, , Volume: 28, Issue:10, 1985
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.Journal of medicinal chemistry, , Nov-27, Volume: 35, Issue:24, 1992
Design, synthesis, and structure-activity relationships of a new series of alpha-adrenergic agonists: spiro[(1,3-diazacyclopent-1-ene)-5,2'-(1',2',3',4'- tetrahydronaphthalene)].Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
Conformationally defined adrenergic agents. 5. Resolution, absolute configuration, and pharmacological characterization of the enantiomers of 2-(5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthyl)imidazoline: a potent agonist at alpha-adrenoceptors.Journal of medicinal chemistry, , Volume: 30, Issue:6, 1987
Discovery of LASSBio-772, a 1,3-benzodioxole N-phenylpiperazine derivative with potent alpha 1A/D-adrenergic receptor blocking properties.European journal of medicinal chemistry, , Volume: 46, Issue:7, 2011
Synthesis and α1-adrenoceptor antagonist activity of tamsulosin analogues.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).Journal of medicinal chemistry, , Apr-20, Volume: 43, Issue:8, 2000
[no title available]Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.Journal of medicinal chemistry, , Aug-13, Volume: 41, Issue:17, 1998
Syntheses of (R)- and (S)-2- and 6-fluoronorepinephrine and (R)- and (S)-2- and 6-fluoroepinephrine: effect of stereochemistry on fluorine-induced adrenergic selectivities.Journal of medicinal chemistry, , Apr-20, Volume: 43, Issue:8, 2000
Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity.Journal of medicinal chemistry, , Nov-26, Volume: 36, Issue:24, 1993
Conformationally defined adrenergic agents. 1. Design and synthesis of novel alpha 2 selective adrenergic agents: electrostatic repulsion based conformational prototypes.Journal of medicinal chemistry, , Volume: 28, Issue:10, 1985
Structure-affinity relationships of 12-sulfonyl derivatives of 5,8,8a,9,10,11,12,12a,13,13a-decahydro-6H-isoquino[2,1-g][1 ,6] naphthyridines at alpha-adrenoceptors.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.Journal of medicinal chemistry, , Volume: 27, Issue:4, 1984
Pyridinylpiperazines, a new class of selective alpha 2-adrenoceptor antagonists.Journal of medicinal chemistry, , Volume: 26, Issue:12, 1983
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.Journal of medicinal chemistry, , Volume: 28, Issue:10, 1985
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
Synthesis and molecular modeling of 1H-pyrrolopyrimidine-2,4-dione derivatives as ligands for the α1-adrenoceptors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 19, Issue:17, 2011
Synthesis of 3-arylpiperazinylalkylpyrrolo[3,2-d]pyrimidine-2,4-dione derivatives as novel, potent, and selective alpha1-adrenoceptor ligands.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Synthesis, biological evaluation, and pharmacophore generation of new pyridazinone derivatives with affinity toward alpha(1)- and alpha(2)-adrenoceptors.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands.Journal of medicinal chemistry, , Volume: 34, Issue:6, 1991
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Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
Design, synthesis, radiolabeling and in vivo evaluation of potential positron emission tomography (PET) radioligands for brain imaging of the 5-HT₇ receptor.Bioorganic & medicinal chemistry, , Mar-01, Volume: 22, Issue:5, 2014
Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
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
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
A rapid computational method for lead evolution: description and application to alpha(1)-adrenergic antagonists.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 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
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
N-aryl-N'-benzylpiperazines as potential antipsychotic agents.Journal of medicinal chemistry, , Oct-13, Volume: 38, Issue:21, 1995
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.Journal of medicinal chemistry, , Nov-27, Volume: 35, Issue:24, 1992
The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Atypical antipsychotic agents: patterns of activity in a series of 3-substituted 2-pyridinyl-1-piperazine derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:3, 1988
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.Journal of medicinal chemistry, , Volume: 29, Issue:3, 1986
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.Journal of medicinal chemistry, , Volume: 27, Issue:4, 1984
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
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001