Page last updated: 2024-08-07 16:17:09
Alpha-1D adrenergic receptor
An alpha-1D adrenergic receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P25100]
Synonyms
Alpha-1A adrenergic receptor;
Alpha-1D adrenoreceptor;
Alpha-1D adrenoceptor;
Alpha-adrenergic receptor 1a
Research
Bioassay Publications (125)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 10 (8.00) | 18.7374 |
| 1990's | 22 (17.60) | 18.2507 |
| 2000's | 49 (39.20) | 29.6817 |
| 2010's | 38 (30.40) | 24.3611 |
| 2020's | 6 (4.80) | 2.80 |
Compounds (160)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| quinacrine | Homo sapiens (human) | IC50 | 2.0650 | 1 | 0 |
| quinacrine | Homo sapiens (human) | Ki | 1.0150 | 1 | 0 |
| 8-hydroxy-2-(di-n-propylamino)tetralin | Homo sapiens (human) | Ki | 1.0000 | 9 | 9 |
| alfuzosin | Homo sapiens (human) | IC50 | 0.0230 | 1 | 1 |
| alfuzosin | Homo sapiens (human) | Ki | 0.0034 | 2 | 2 |
| amitriptyline | Homo sapiens (human) | IC50 | 0.1050 | 1 | 0 |
| amitriptyline | Homo sapiens (human) | Ki | 0.0520 | 1 | 0 |
| amlodipine | Homo sapiens (human) | Ki | 5.3700 | 1 | 1 |
| amoxapine | Homo sapiens (human) | IC50 | 0.3060 | 1 | 0 |
| amoxapine | Homo sapiens (human) | Ki | 0.1500 | 1 | 0 |
| apraclonidine | Homo sapiens (human) | Ki | 0.1800 | 1 | 1 |
| astemizole | Homo sapiens (human) | IC50 | 0.7690 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 0.3780 | 1 | 0 |
| atenolol | Homo sapiens (human) | IC50 | 0.2300 | 1 | 1 |
| bmy 7378 | Homo sapiens (human) | Ki | 0.0016 | 15 | 16 |
| brimonidine | Homo sapiens (human) | IC50 | 1.7200 | 1 | 0 |
| brimonidine | Homo sapiens (human) | Ki | 0.8460 | 1 | 0 |
| bunazosin | Homo sapiens (human) | IC50 | 0.0012 | 1 | 1 |
| buspirone | Homo sapiens (human) | IC50 | 1.0770 | 1 | 0 |
| buspirone | Homo sapiens (human) | Ki | 0.5290 | 1 | 0 |
| carvedilol | Homo sapiens (human) | IC50 | 0.0018 | 1 | 0 |
| carvedilol | Homo sapiens (human) | Ki | 0.0009 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | IC50 | 0.0040 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | Ki | 0.0020 | 1 | 0 |
| cisapride | Homo sapiens (human) | IC50 | 0.0830 | 3 | 2 |
| cisapride | Homo sapiens (human) | Ki | 0.0930 | 1 | 0 |
| citalopram | Homo sapiens (human) | IC50 | 3.2890 | 1 | 0 |
| citalopram | Homo sapiens (human) | Ki | 1.6170 | 1 | 0 |
| clomipramine | Homo sapiens (human) | IC50 | 0.1800 | 1 | 0 |
| clomipramine | Homo sapiens (human) | Ki | 0.0880 | 1 | 0 |
| clonidine | Homo sapiens (human) | IC50 | 1.2100 | 1 | 0 |
| clonidine | Homo sapiens (human) | Ki | 0.4058 | 4 | 3 |
| clotrimazole | Homo sapiens (human) | IC50 | 15.0120 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 7.3790 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | IC50 | 0.1070 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | Ki | 0.0530 | 1 | 0 |
| domperidone | Homo sapiens (human) | IC50 | 1.0650 | 1 | 0 |
| domperidone | Homo sapiens (human) | Ki | 0.5240 | 1 | 0 |
| doxazosin | Homo sapiens (human) | IC50 | 0.0034 | 1 | 0 |
| doxazosin | Homo sapiens (human) | Ki | 0.0015 | 6 | 5 |
| doxepin | Homo sapiens (human) | IC50 | 0.1180 | 1 | 0 |
| doxepin | Homo sapiens (human) | Ki | 0.0580 | 1 | 0 |
| droperidol | Homo sapiens (human) | IC50 | 0.0830 | 1 | 0 |
| droperidol | Homo sapiens (human) | Ki | 0.0410 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 0.9771 | 2 | 1 |
| ebastine | Homo sapiens (human) | Ki | 0.8706 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 8.8970 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 4.3730 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | IC50 | 0.0330 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 0.0160 | 1 | 0 |
| haloperidol | Homo sapiens (human) | IC50 | 0.0840 | 1 | 0 |
| haloperidol | Homo sapiens (human) | Ki | 0.0219 | 3 | 2 |
| hydroxychloroquine | Homo sapiens (human) | IC50 | 4.7720 | 1 | 0 |
| hydroxychloroquine | Homo sapiens (human) | Ki | 2.3460 | 1 | 0 |
| ketotifen | Homo sapiens (human) | IC50 | 3.7270 | 1 | 0 |
| ketotifen | Homo sapiens (human) | Ki | 1.8320 | 1 | 0 |
| labetalol | Homo sapiens (human) | IC50 | 0.5210 | 1 | 0 |
| labetalol | Homo sapiens (human) | Ki | 0.2560 | 1 | 0 |
| maprotiline | Homo sapiens (human) | IC50 | 0.3970 | 1 | 0 |
| maprotiline | Homo sapiens (human) | Ki | 0.1950 | 1 | 0 |
| mianserin | Homo sapiens (human) | IC50 | 0.0830 | 1 | 0 |
| mianserin | Homo sapiens (human) | Ki | 0.0410 | 1 | 0 |
| miconazole | Homo sapiens (human) | IC50 | 3.0460 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 1.4970 | 1 | 0 |
| naftopidil | Homo sapiens (human) | IC50 | 0.0552 | 2 | 2 |
| naftopidil | Homo sapiens (human) | Ki | 0.0012 | 1 | 1 |
| nan 190 | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| nortriptyline | Homo sapiens (human) | IC50 | 0.2730 | 1 | 0 |
| nortriptyline | Homo sapiens (human) | Ki | 0.1340 | 1 | 0 |
| oxymetazoline | Homo sapiens (human) | IC50 | 2.8440 | 1 | 0 |
| oxymetazoline | Homo sapiens (human) | Ki | 0.9297 | 3 | 2 |
| moxonidine | Homo sapiens (human) | Ki | 15.5000 | 2 | 2 |
| prazosin | Homo sapiens (human) | IC50 | 0.0007 | 6 | 5 |
| prazosin | Homo sapiens (human) | Ki | 0.0016 | 17 | 17 |
| prochlorperazine | Homo sapiens (human) | IC50 | 0.0340 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | Ki | 0.0160 | 1 | 0 |
| promazine | Homo sapiens (human) | IC50 | 0.0130 | 1 | 0 |
| promazine | Homo sapiens (human) | Ki | 0.0062 | 1 | 0 |
| promethazine | Homo sapiens (human) | IC50 | 0.1830 | 1 | 0 |
| promethazine | Homo sapiens (human) | Ki | 0.0900 | 1 | 0 |
| quetiapine | Homo sapiens (human) | IC50 | 0.0966 | 1 | 0 |
| quetiapine | Homo sapiens (human) | Ki | 0.0292 | 4 | 3 |
| raloxifene | Homo sapiens (human) | IC50 | 0.9730 | 1 | 0 |
| raloxifene | Homo sapiens (human) | Ki | 0.4780 | 1 | 0 |
| risperidone | Homo sapiens (human) | IC50 | 0.0100 | 1 | 0 |
| risperidone | Homo sapiens (human) | Ki | 0.0053 | 6 | 5 |
| terazosin | Homo sapiens (human) | IC50 | 0.0110 | 2 | 1 |
| terazosin | Homo sapiens (human) | Ki | 0.0492 | 11 | 12 |
| terfenadine | Homo sapiens (human) | IC50 | 2.3400 | 1 | 1 |
| thioridazine | Homo sapiens (human) | IC50 | 0.0059 | 1 | 0 |
| thioridazine | Homo sapiens (human) | Ki | 0.0029 | 1 | 0 |
| trazodone | Homo sapiens (human) | IC50 | 0.2650 | 1 | 0 |
| trazodone | Homo sapiens (human) | Ki | 0.1300 | 1 | 0 |
| 5-methylurapidil | Homo sapiens (human) | Ki | 0.0155 | 2 | 2 |
| n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamide | Homo sapiens (human) | Ki | 0.0046 | 3 | 3 |
| wb 4101 | Homo sapiens (human) | Ki | 0.0005 | 9 | 10 |
| xylometazoline | Homo sapiens (human) | Ki | 0.0910 | 1 | 1 |
| zotepine | Homo sapiens (human) | Ki | 0.0034 | 1 | 1 |
| phentolamine | Homo sapiens (human) | IC50 | 0.0173 | 2 | 1 |
| phentolamine | Homo sapiens (human) | Ki | 0.0127 | 3 | 2 |
| mepazine | Homo sapiens (human) | IC50 | 0.1370 | 1 | 0 |
| mepazine | Homo sapiens (human) | Ki | 0.0670 | 1 | 0 |
| cyclizine | Homo sapiens (human) | IC50 | 1.2150 | 1 | 0 |
| cyclizine | Homo sapiens (human) | Ki | 0.5970 | 1 | 0 |
| ergotamine | Homo sapiens (human) | IC50 | 0.0490 | 1 | 0 |
| ergotamine | Homo sapiens (human) | Ki | 0.0240 | 1 | 0 |
| yohimbine | Homo sapiens (human) | IC50 | 1.0130 | 1 | 0 |
| yohimbine | Homo sapiens (human) | Ki | 0.2629 | 3 | 2 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| dihydroergotamine | Homo sapiens (human) | IC50 | 0.0290 | 1 | 0 |
| dihydroergotamine | Homo sapiens (human) | Ki | 0.0140 | 1 | 0 |
| dimenhydrinate | Homo sapiens (human) | IC50 | 2.8940 | 1 | 0 |
| dimenhydrinate | Homo sapiens (human) | Ki | 1.4230 | 1 | 0 |
| gentian violet | Homo sapiens (human) | IC50 | 1.9800 | 1 | 0 |
| gentian violet | Homo sapiens (human) | Ki | 0.9730 | 1 | 0 |
| clemastine | Homo sapiens (human) | IC50 | 0.0320 | 1 | 0 |
| clemastine | Homo sapiens (human) | Ki | 0.0150 | 1 | 0 |
| pizotyline | Homo sapiens (human) | Ki | 0.0750 | 1 | 1 |
| metergoline | Homo sapiens (human) | IC50 | 0.1360 | 1 | 0 |
| metergoline | Homo sapiens (human) | Ki | 0.0670 | 1 | 0 |
| lisuride | Homo sapiens (human) | IC50 | 0.0410 | 1 | 0 |
| lisuride | Homo sapiens (human) | Ki | 0.0200 | 1 | 0 |
| bromocriptine | Homo sapiens (human) | IC50 | 0.0300 | 1 | 0 |
| bromocriptine | Homo sapiens (human) | Ki | 0.0150 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | IC50 | 33.7210 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | Ki | 16.5750 | 1 | 0 |
| indoramin | Homo sapiens (human) | Ki | 0.1342 | 2 | 2 |
| penfluridol | Homo sapiens (human) | Ki | 0.6020 | 1 | 1 |
| dobutamine | Homo sapiens (human) | IC50 | 0.1140 | 1 | 0 |
| dobutamine | Homo sapiens (human) | Ki | 0.0560 | 1 | 0 |
| pergolide | Homo sapiens (human) | IC50 | 1.5130 | 1 | 0 |
| pergolide | Homo sapiens (human) | Ki | 0.7440 | 1 | 0 |
| ipsapirone | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| ipsapirone | Homo sapiens (human) | Ki | 0.1375 | 2 | 2 |
| imiquimod | Homo sapiens (human) | IC50 | 2.6210 | 1 | 0 |
| imiquimod | Homo sapiens (human) | Ki | 1.2880 | 1 | 0 |
| sertindole | Homo sapiens (human) | Ki | 0.0018 | 1 | 1 |
| niguldipine | Homo sapiens (human) | Ki | 0.2070 | 3 | 3 |
| aripiprazole | Homo sapiens (human) | Ki | 0.0570 | 1 | 1 |
| ziprasidone | Homo sapiens (human) | IC50 | 0.0110 | 1 | 1 |
| ziprasidone | Homo sapiens (human) | Ki | 0.0090 | 4 | 4 |
| ergocornine | Homo sapiens (human) | IC50 | 0.0180 | 1 | 0 |
| ergocornine | Homo sapiens (human) | Ki | 0.0087 | 1 | 0 |
| corynanthine | Homo sapiens (human) | Ki | 0.2530 | 1 | 1 |
| way 100635 | Homo sapiens (human) | Ki | 0.0050 | 1 | 1 |
| gr 127935 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| roemerine | Homo sapiens (human) | Ki | 0.6310 | 1 | 1 |
| sk&f 104078 | Homo sapiens (human) | Ki | 0.0330 | 1 | 1 |
| sk&f 86466 | Homo sapiens (human) | Ki | 0.1260 | 1 | 1 |
| sk&f 104856 | Homo sapiens (human) | Ki | 0.0021 | 3 | 3 |
| tamsulosin | Homo sapiens (human) | IC50 | 0.0008 | 2 | 2 |
| tamsulosin | Homo sapiens (human) | Ki | 0.0021 | 9 | 11 |
| cyclazosin | Homo sapiens (human) | Ki | 0.0096 | 4 | 4 |
| sc 53116 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sc 53116 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| alpha-ergocryptine | Homo sapiens (human) | IC50 | 0.0480 | 1 | 0 |
| alpha-ergocryptine | Homo sapiens (human) | Ki | 0.0240 | 1 | 0 |
| rec 15-2739 | Homo sapiens (human) | Ki | 0.0020 | 2 | 2 |
| asenapine | Homo sapiens (human) | Ki | 0.0012 | 1 | 1 |
| abanoquil | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
| atropine | Homo sapiens (human) | IC50 | 1.3540 | 1 | 0 |
| atropine | Homo sapiens (human) | Ki | 0.6660 | 1 | 0 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 0.3400 | 1 | 1 |
| maduramicin | Homo sapiens (human) | IC50 | 1.1280 | 1 | 0 |
| maduramicin | Homo sapiens (human) | Ki | 0.5540 | 1 | 0 |
| eptapirone | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| bmy 7378 | Homo sapiens (human) | Ki | 0.0025 | 3 | 4 |
| terconazole | Homo sapiens (human) | IC50 | 14.3850 | 1 | 0 |
| terconazole | Homo sapiens (human) | Ki | 7.0700 | 1 | 0 |
| dihydroergocristine monomesylate | Homo sapiens (human) | IC50 | 0.0074 | 1 | 0 |
| dihydroergocristine monomesylate | Homo sapiens (human) | Ki | 0.0036 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 10.8260 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 5.3210 | 1 | 0 |
| rauwolscine | Homo sapiens (human) | Ki | 0.6618 | 2 | 2 |
| flunarizine | Homo sapiens (human) | IC50 | 1.0850 | 1 | 0 |
| flunarizine | Homo sapiens (human) | Ki | 0.5330 | 1 | 0 |
| benztropine | Homo sapiens (human) | IC50 | 0.0520 | 1 | 0 |
| benztropine | Homo sapiens (human) | Ki | 0.0260 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | IC50 | 1.1670 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | Ki | 0.5730 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | IC50 | 4.9820 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 2.4490 | 1 | 0 |
| hirsutine, (16e,20beta)-isomer | Homo sapiens (human) | Ki | 0.0417 | 1 | 1 |
| dapiprazole | Homo sapiens (human) | IC50 | 0.0083 | 1 | 0 |
| dapiprazole | Homo sapiens (human) | Ki | 0.0041 | 1 | 0 |
| mitragynine | Homo sapiens (human) | Ki | 5.4800 | 1 | 1 |
| bp 897 | Homo sapiens (human) | Ki | 0.0150 | 2 | 2 |
| rs 100329 | Homo sapiens (human) | Ki | 0.0126 | 1 | 1 |
| rs 17053 | Homo sapiens (human) | Ki | 0.0158 | 1 | 1 |
| 3-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione | Homo sapiens (human) | Ki | 688,557,500,000,000.0000 | 4 | 4 |
| le 300 | Homo sapiens (human) | Ki | 0.0110 | 1 | 1 |
| harmine | Homo sapiens (human) | Ki | 0.8100 | 1 | 1 |
| dexmedetomidine | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
| silodosin | Homo sapiens (human) | IC50 | 0.0168 | 2 | 2 |
| silodosin | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| guanabenz | Homo sapiens (human) | IC50 | 0.4720 | 1 | 0 |
| guanabenz | Homo sapiens (human) | Ki | 0.2320 | 1 | 0 |
| ro 25-6981 | Homo sapiens (human) | Ki | 0.1800 | 1 | 1 |
| dexniguldipine | Homo sapiens (human) | Ki | 0.1999 | 3 | 4 |
| vilazodone | Homo sapiens (human) | IC50 | 1.9800 | 1 | 1 |
| ro 70-0004 | Homo sapiens (human) | Ki | 0.0816 | 2 | 2 |
| 10,10-bis((2-fluoro-4-pyridinyl)methyl)-9(10h)-anthracenone | Homo sapiens (human) | Ki | 3.9000 | 1 | 1 |
| fauc 346 | Homo sapiens (human) | Ki | 0.0150 | 1 | 1 |
| pnu 96415e | Homo sapiens (human) | Ki | 0.0380 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 0.0400 | 1 | 1 |
| tert-butyl peroxybenzoate | Homo sapiens (human) | Ki | 0.2900 | 1 | 1 |
| 77-lh-28-1 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| fauc 365 | Homo sapiens (human) | Ki | 0.9133 | 3 | 3 |
| fauc 113 | Homo sapiens (human) | Ki | 0.0036 | 1 | 1 |
| mk-7246 | Homo sapiens (human) | Ki | 10.0000 | 1 | 0 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
| clozapine | Homo sapiens (human) | IC50 | 0.0350 | 1 | 0 |
| clozapine | Homo sapiens (human) | Ki | 0.0198 | 6 | 5 |
| olanzapine | Homo sapiens (human) | IC50 | 0.0920 | 1 | 0 |
| olanzapine | Homo sapiens (human) | Ki | 0.0291 | 5 | 4 |
Drugs with Activation Measurements
Drugs with Other Measurements
[no title available]European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition.Journal of medicinal chemistry, , Jan-24, Volume: 56, Issue:2, 2013
Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors.Journal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
Discovery of a new series of 5-HT1A receptor agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 20, Issue:6, 2010
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
Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists.Journal of medicinal chemistry, , Jul-19, Volume: 44, Issue:15, 2001
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
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
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]European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition.Journal of medicinal chemistry, , Jan-24, Volume: 56, Issue:2, 2013
Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors.Journal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
Discovery of a new series of 5-HT1A receptor agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 20, Issue:6, 2010
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 and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
New pyrimido[5,4-b]indoles as ligands for alpha(1)-adrenoceptor subtypes.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
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
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
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
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
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines.Bioorganic & medicinal chemistry letters, , Feb-11, Volume: 12, Issue:3, 2002
Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines.Bioorganic & medicinal chemistry letters, , Dec-02, Volume: 12, Issue:23, 2002
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
[no title available],
Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent.Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
[no title available],
Quinazoline based αEuropean journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Structure-activity relationships in 1,4-benzodioxan-related compounds. 8.(1) {2-[2-(4-chlorobenzyloxy)phenoxy]ethyl}-[2-(2,6-dimethoxyphenoxy)ethyl]amine (clopenphendioxan) as a tool to highlight the involvement of alpha1D- and alpha1B-adrenoreceptor subtJournal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
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
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
[no title available],
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
[no title available],
[no title available]Bioorganic & medicinal chemistry letters, , 05-15, Volume: 28, Issue:9, 2018
[no title available]Bioorganic & medicinal chemistry letters, , 02-15, Volume: 28, Issue:4, 2018
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH.Bioorganic & medicinal chemistry, , Dec-15, Volume: 23, Issue:24, 2015
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
[no title available],
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HTMedChemComm, , Mar-01, Volume: 9, Issue:3, 2018
Quinazoline based αEuropean journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Design, synthesis, and biological evaluation of prazosin-related derivatives as multipotent compounds.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Prazosin-related compounds. Effect of transforming the piperazinylquinazoline moiety into an aminomethyltetrahydroacridine system on the affinity for alpha1-adrenoreceptors.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists.Journal of medicinal chemistry, , Jul-19, Volume: 44, Issue:15, 2001
Design and synthesis of novel dihydropyridine alpha-1a antagonists.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 9, Issue:19, 1999
Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton.Journal of medicinal chemistry, , Jan-14, Volume: 42, Issue:1, 1999
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
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
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
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
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
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
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
[no title available],
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
Cardioselectivity of beta-adrenoceptor blocking agents 1. 1-[(4-Hydroxyphenethyl)amino]-3-(aryloxy)propan-2-ols.Journal of medicinal chemistry, , Volume: 22, Issue:6, 1979
[no title available]Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
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],
[no title available]Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 30, Issue:20, 2020
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
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
[no title available],
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-22, Volume: 8, Issue:18, 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
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
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
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
[no title available],
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
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]European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
1,3-Dioxane as a scaffold for potent and selective 5-HTEuropean journal of medicinal chemistry, , Aug-15, Volume: 176, 2019
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition.Journal of medicinal chemistry, , Jan-24, Volume: 56, Issue:2, 2013
Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novel α1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, and α1d computational study.Bioorganic & medicinal chemistry, , Oct-01, Volume: 18, Issue:19, 2010
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
Prazosin-related compounds. Effect of transforming the piperazinylquinazoline moiety into an aminomethyltetrahydroacridine system on the affinity for alpha1-adrenoreceptors.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
1,3-dioxolane-based ligands as a novel class of alpha1-adrenoceptor antagonists.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Structure-activity relationships in 1,4-benzodioxan-related compounds. 7. Selectivity of 4-phenylchroman analogues for alpha(1)-adrenoreceptor subtypes.Journal of medicinal chemistry, , Apr-11, Volume: 45, Issue:8, 2002
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
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
Absolute configuration of glycerol derivatives. 7. Enantiomers of 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]methyl]-1,4-benzodioxane (WB-4101), a potent competitive alpha-adrenergic antagonist.Journal of medicinal chemistry, , Volume: 22, Issue:9, 1979
Discovery of Quinazoline-Based Fluorescent Probes to α1-Adrenergic Receptors.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
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
[no title available],
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
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
[no title available],
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
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
Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 42, 2021
Indolebutylamines as selective 5-HT(1A) agonists.Journal of medicinal chemistry, , Sep-09, Volume: 47, Issue:19, 2004
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.Bioorganic & medicinal chemistry letters, , Sep-22, Volume: 8, Issue:18, 1998
Recent advances in selective alpha1-adrenoreceptor antagonists as antihypertensive agents.Bioorganic & medicinal chemistry, , May-01, Volume: 16, Issue:9, 2008
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
[no title available]Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
Polypharmacology - foe or friend?Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 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
New pyrimido[5,4-b]indoles as ligands for alpha(1)-adrenoceptor subtypes.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
The one-pot synthesis of butyl-1H-indol-3-alkylcarboxylic acid derivatives in ionic liquid as potent dual-acting agent for management of BPH.European journal of medicinal chemistry, , Nov-01, Volume: 205, 2020
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selective αJournal of medicinal chemistry, , Oct-27, Volume: 59, Issue:20, 2016
Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related GJournal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Synthesis and α1-adrenoceptor antagonist activity of tamsulosin analogues.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
(Phenylpiperazinyl)cyclohexylureas: discovery of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
(Arylpiperazinyl)cyclohexylsufonamides: discovery of alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS).Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 17, Issue:12, 2007
(Phenylpiperidinyl)cyclohexylsulfonamides: development of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 17, Issue:14, 2007
Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.Journal of medicinal chemistry, , Jun-01, Volume: 43, Issue:11, 2000
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
[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
Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.Bioorganic & medicinal chemistry, , Mar-15, Volume: 15, Issue:6, 2007
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
New potential uroselective NO-donor alpha1-antagonists.Journal of medicinal chemistry, , Aug-14, Volume: 46, Issue:17, 2003
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Novel 4-phenylpiperidine-2,6-dione derivatives. Ligands for α₁-adrenoceptor subtypes.European journal of medicinal chemistry, , Volume: 46, Issue:7, 2011
1,3-dioxolane-based ligands as a novel class of alpha1-adrenoceptor antagonists.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
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
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.Journal of medicinal chemistry, , Volume: 27, Issue:4, 1984
Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
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
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Novel 4-phenylpiperidine-2,6-dione derivatives. Ligands for α₁-adrenoceptor subtypes.European journal of medicinal chemistry, , Volume: 46, Issue:7, 2011
New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 16, Issue:24, 2006
New pyrimido[5,4-b]indoles as ligands for alpha(1)-adrenoceptor subtypes.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
7-Methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine: a new heterocyclic system and a new lead compound for dopamine receptor antagonists.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selective αJournal of medicinal chemistry, , Oct-27, Volume: 59, Issue:20, 2016
Design, Synthesis, and Biological Evaluation of Indoline and Indole Derivatives as Potent and Selective α1A-Adrenoceptor Antagonists.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
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
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
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
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
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
[no title available],
[no title available]Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
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
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
[no title available],
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| alpha1-adrenergic receptor activity | molecular function | Combining with epinephrine or norepinephrine to initiate a change in cell activity via activation of a G protein, with pharmacological characteristics of alpha1-adrenergic receptors; the activity involves transmitting the signal to the Gq alpha subunit of a heterotrimeric G protein. [GOC:cb, GOC:mah, IUPHAR_GPCR:1274] |
Located In
This protein is located 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] |
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 10 target(s):
| Target | Category | Definition |
|---|
| 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-modulating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of adenylyl cyclase activity and a subsequent change in the intracellular concentration of cyclic AMP (cAMP). [GOC:mah, GOC:signaling, ISBN:0815316194] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| neuron-glial cell signaling | biological process | Cell-cell signaling that mediates the transfer of information from a neuron to a glial cell. This signaling has been shown to be mediated by various molecules released by different types of neurons, e.g. glutamate, gamma-amino butyric acid (GABA), noradrenaline, acetylcholine, dopamine and adenosine. [GOC:aruk, GOC:bc, PMID:10195197, PMID:10196584, PMID:10377338, PMID:10493741, PMID:11356870, PMID:11399439, PMID:15252819, PMID:27788368] |
| cell-cell signaling | biological process | Any process that mediates the transfer of information from one cell to another. This process includes signal transduction in the receiving cell and, where applicable, release of a ligand and any processes that actively facilitate its transport and presentation to the receiving cell. Examples include signaling via soluble ligands, via cell adhesion molecules and via gap junctions. [GOC:dos, GOC:mah] |
| 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] |
| phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |
| 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] |