Page last updated: 2024-08-07 16:13:36
Alpha-2A adrenergic receptor
An alpha-2A adrenergic receptor that is encoded in the genome of rat. [OMA:P22909, PRO:DNx]
Synonyms
Alpha-2A adrenoreceptor;
Alpha-2A adrenoceptor;
Alpha-2AAR;
Alpha-2D adrenergic receptor;
CA2-47
Research
Bioassay Publications (123)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 27 (21.95) | 18.7374 |
| 1990's | 49 (39.84) | 18.2507 |
| 2000's | 30 (24.39) | 29.6817 |
| 2010's | 17 (13.82) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (155)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| agmatine | Rattus norvegicus (Norway rat) | Ki | 31.7000 | 1 | 1 |
| tryptamine | Rattus norvegicus (Norway rat) | Ki | 19.0000 | 1 | 1 |
| 8-hydroxy-2-(di-n-propylamino)tetralin | Rattus norvegicus (Norway rat) | IC50 | 0.8100 | 1 | 3 |
| 8-hydroxy-2-(di-n-propylamino)tetralin | Rattus norvegicus (Norway rat) | Ki | 0.8318 | 1 | 1 |
| 6-fluoronorepinephrine | Rattus norvegicus (Norway rat) | Ki | 0.0427 | 3 | 4 |
| 6-methoxytryptoline | Rattus norvegicus (Norway rat) | Ki | 7.8300 | 1 | 1 |
| alfuzosin | Rattus norvegicus (Norway rat) | Ki | 0.0036 | 1 | 1 |
| amlodipine | Rattus norvegicus (Norway rat) | Ki | 5.3700 | 1 | 1 |
| benextramine | Rattus norvegicus (Norway rat) | IC50 | 4.0200 | 1 | 1 |
| bmy 7378 | Rattus norvegicus (Norway rat) | Ki | 0.2696 | 3 | 6 |
| brimonidine | Rattus norvegicus (Norway rat) | Ki | 0.0300 | 1 | 1 |
| buspirone | Rattus norvegicus (Norway rat) | IC50 | 7.7500 | 2 | 4 |
| chlorpromazine | Rattus norvegicus (Norway rat) | IC50 | 1.4791 | 1 | 1 |
| chlorpromazine | Rattus norvegicus (Norway rat) | Ki | 0.1259 | 1 | 1 |
| cisapride | Rattus norvegicus (Norway rat) | IC50 | 5.0032 | 2 | 2 |
| cisapride | Rattus norvegicus (Norway rat) | Ki | 2.2650 | 2 | 2 |
| clebopride | Rattus norvegicus (Norway rat) | Ki | 0.6000 | 1 | 1 |
| clomipramine | Rattus norvegicus (Norway rat) | Ki | 0.0510 | 1 | 2 |
| clonidine | Rattus norvegicus (Norway rat) | IC50 | 0.0173 | 1 | 1 |
| clonidine | Rattus norvegicus (Norway rat) | Ki | 0.1162 | 8 | 8 |
| doxazosin | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 1 | 1 |
| fluoxetine | Rattus norvegicus (Norway rat) | Ki | 4.4965 | 2 | 2 |
| granisetron | Rattus norvegicus (Norway rat) | IC50 | 3.8019 | 1 | 1 |
| haloperidol | Rattus norvegicus (Norway rat) | Ki | 9.6000 | 1 | 1 |
| imipramine | Rattus norvegicus (Norway rat) | IC50 | 3.3884 | 1 | 1 |
| imipramine | Rattus norvegicus (Norway rat) | Ki | 4.9000 | 1 | 2 |
| isoproterenol | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| isoproterenol | Rattus norvegicus (Norway rat) | Ki | 21.0000 | 1 | 1 |
| metoclopramide | Rattus norvegicus (Norway rat) | IC50 | 7.7000 | 1 | 1 |
| mianserin | Rattus norvegicus (Norway rat) | IC50 | 0.2100 | 1 | 1 |
| mianserin | Rattus norvegicus (Norway rat) | Ki | 0.0620 | 1 | 1 |
| naphazoline | Rattus norvegicus (Norway rat) | Ki | 0.0057 | 1 | 1 |
| ondansetron | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| oxymetazoline | Rattus norvegicus (Norway rat) | Ki | 0.2073 | 11 | 13 |
| perhexiline | Rattus norvegicus (Norway rat) | IC50 | 7.7625 | 1 | 1 |
| prazosin | Rattus norvegicus (Norway rat) | Ki | 1.7048 | 16 | 17 |
| quetiapine | Rattus norvegicus (Norway rat) | Ki | 0.3981 | 1 | 1 |
| risperidone | Rattus norvegicus (Norway rat) | Ki | 0.0144 | 2 | 2 |
| sk&f 29661 | Rattus norvegicus (Norway rat) | Ki | 555,555,650.0000 | 13 | 18 |
| spiperone | Rattus norvegicus (Norway rat) | Ki | 0.0072 | 1 | 1 |
| terazosin | Rattus norvegicus (Norway rat) | Ki | 0.0058 | 2 | 3 |
| terfenadine | Rattus norvegicus (Norway rat) | IC50 | 0.1288 | 1 | 1 |
| tetrahydropapaverine | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 2 |
| thioridazine | Rattus norvegicus (Norway rat) | IC50 | 0.0355 | 1 | 1 |
| tolazoline | Rattus norvegicus (Norway rat) | Ki | 0.1800 | 1 | 1 |
| tramazoline | Rattus norvegicus (Norway rat) | Ki | 0.0042 | 1 | 1 |
| 5-methylurapidil | Rattus norvegicus (Norway rat) | Ki | 0.0108 | 2 | 2 |
| wb 4101 | Rattus norvegicus (Norway rat) | Ki | 0.0293 | 6 | 9 |
| phentolamine | Rattus norvegicus (Norway rat) | IC50 | 0.0492 | 3 | 3 |
| phentolamine | Rattus norvegicus (Norway rat) | Ki | 0.0134 | 2 | 2 |
| apomorphine | Rattus norvegicus (Norway rat) | IC50 | 0.0630 | 1 | 1 |
| piperoxan | Rattus norvegicus (Norway rat) | IC50 | 0.1400 | 1 | 1 |
| piperoxan | Rattus norvegicus (Norway rat) | Ki | 0.0950 | 1 | 1 |
| phenylephrine | Rattus norvegicus (Norway rat) | Ki | 0.3300 | 2 | 2 |
| 1,2,3,4-tetrahydroisoquinoline | Rattus norvegicus (Norway rat) | Ki | 281,838,000,000.3150 | 8 | 10 |
| benzylamine | Rattus norvegicus (Norway rat) | Ki | 25,059,350,010.0000 | 2 | 2 |
| yohimbine | Rattus norvegicus (Norway rat) | IC50 | 0.0682 | 4 | 6 |
| yohimbine | Rattus norvegicus (Norway rat) | Ki | 0.0593 | 14 | 17 |
| phenylpropanolamine | Rattus norvegicus (Norway rat) | Ki | 8.4000 | 1 | 1 |
| hesperidin | Rattus norvegicus (Norway rat) | IC50 | 74.0000 | 1 | 1 |
| vinblastine | Rattus norvegicus (Norway rat) | IC50 | 2.1000 | 1 | 1 |
| vancomycin | Rattus norvegicus (Norway rat) | Ki | 0.5629 | 2 | 2 |
| 2-methyl-1,2,3,4-tetrahydroisoquinoline | Rattus norvegicus (Norway rat) | Ki | 4,168,690,000,000.0000 | 1 | 1 |
| tetrahydropapaveroline | Rattus norvegicus (Norway rat) | Ki | 40.0000 | 1 | 2 |
| bromocriptine | Rattus norvegicus (Norway rat) | IC50 | 0.5140 | 1 | 1 |
| indoramin | Rattus norvegicus (Norway rat) | Ki | 0.1100 | 1 | 1 |
| buspirone hydrochloride | Rattus norvegicus (Norway rat) | Ki | 5.0119 | 1 | 1 |
| norsalsolinol | Rattus norvegicus (Norway rat) | Ki | 2,089,300,000,000.0000 | 1 | 1 |
| st 1059 | Rattus norvegicus (Norway rat) | Ki | 6.9000 | 1 | 1 |
| paroxetine | Rattus norvegicus (Norway rat) | Ki | 6.3100 | 1 | 1 |
| pergolide | Rattus norvegicus (Norway rat) | IC50 | 0.0410 | 1 | 1 |
| idazoxan | Rattus norvegicus (Norway rat) | Ki | 0.2068 | 3 | 4 |
| ipsapirone | Rattus norvegicus (Norway rat) | Ki | 0.2200 | 1 | 1 |
| besipirdine | Rattus norvegicus (Norway rat) | IC50 | 0.2950 | 6 | 6 |
| delequamine | Rattus norvegicus (Norway rat) | Ki | 3.4114 | 2 | 3 |
| ziprasidone | Rattus norvegicus (Norway rat) | IC50 | 0.1514 | 1 | 1 |
| mizolastine | Rattus norvegicus (Norway rat) | IC50 | 0.3548 | 1 | 1 |
| mianserin hydrochloride | Rattus norvegicus (Norway rat) | IC50 | 1.2000 | 1 | 1 |
| medetomidine | Rattus norvegicus (Norway rat) | Ki | 0.0250 | 2 | 5 |
| mezilamine | Rattus norvegicus (Norway rat) | Ki | 0.0105 | 2 | 2 |
| atipamezole | Rattus norvegicus (Norway rat) | Ki | 0.9977 | 2 | 2 |
| hp 873 | Rattus norvegicus (Norway rat) | IC50 | 0.0004 | 1 | 1 |
| 1-phenethylamine, (s)-isomer | Rattus norvegicus (Norway rat) | Ki | 8,317,640,000.0000 | 1 | 1 |
| corynanthine | Rattus norvegicus (Norway rat) | IC50 | 17.5000 | 1 | 1 |
| tryptoline | Rattus norvegicus (Norway rat) | Ki | 1.3775 | 3 | 4 |
| mosapride | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| ly 134046 | Rattus norvegicus (Norway rat) | Ki | 24,547,100,004.0500 | 6 | 10 |
| 5-fluorodopamine | Rattus norvegicus (Norway rat) | Ki | 0.0400 | 1 | 2 |
| sk&f 104078 | Rattus norvegicus (Norway rat) | Ki | 0.3130 | 1 | 1 |
| a 68930 | Rattus norvegicus (Norway rat) | Ki | 0.0400 | 1 | 1 |
| 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline | Rattus norvegicus (Norway rat) | Ki | 2,688,752,941,176.4920 | 12 | 17 |
| sk&f 86466 | Rattus norvegicus (Norway rat) | Ki | 0.0079 | 1 | 1 |
| 5,6-dihydroxy-1-(2-imidazolinyl)tetralin | Rattus norvegicus (Norway rat) | Ki | 0.0065 | 1 | 1 |
| fluoroclebopride | Rattus norvegicus (Norway rat) | Ki | 1.3000 | 1 | 1 |
| cyclazosin | Rattus norvegicus (Norway rat) | Ki | 0.0316 | 1 | 3 |
| sc 53116 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| dc 015 | Rattus norvegicus (Norway rat) | Ki | 0.5930 | 1 | 1 |
| sonepiprazole | Rattus norvegicus (Norway rat) | Ki | 2.6000 | 1 | 1 |
| rec 15-2739 | Rattus norvegicus (Norway rat) | Ki | 0.0015 | 1 | 2 |
| abanoquil | Rattus norvegicus (Norway rat) | Ki | 0.0000 | 1 | 1 |
| corbadrine | Rattus norvegicus (Norway rat) | Ki | 0.1557 | 2 | 4 |
| 5-methoxytryptoline | Rattus norvegicus (Norway rat) | Ki | 0.8250 | 1 | 1 |
| 4,9-dihydro-7-methoxy-3h-pyrido(3,4b)indole | Rattus norvegicus (Norway rat) | Ki | 11.7500 | 4 | 8 |
| 3-fluoronorepinephrine | Rattus norvegicus (Norway rat) | Ki | 1.1750 | 3 | 4 |
| 5'-o-(n-(alanyl)sulfamoyl)adenosine | Rattus norvegicus (Norway rat) | Ki | 2.5000 | 1 | 1 |
| latrepirdine | Rattus norvegicus (Norway rat) | Ki | 0.0759 | 1 | 1 |
| 2-fluorodopamine | Rattus norvegicus (Norway rat) | Ki | 0.1200 | 1 | 2 |
| bmy 7378 | Rattus norvegicus (Norway rat) | Ki | 0.0014 | 2 | 5 |
| epitrate | Rattus norvegicus (Norway rat) | Ki | 0.0450 | 1 | 2 |
| (R)-norlaudanosoline | Rattus norvegicus (Norway rat) | Ki | 25.0000 | 1 | 2 |
| cocaine | Rattus norvegicus (Norway rat) | IC50 | 5.7544 | 1 | 1 |
| adenosine-5'-(n-ethylcarboxamide) | Rattus norvegicus (Norway rat) | IC50 | 0.0370 | 1 | 1 |
| 3-methyl-1,2,3,4-tetrahydroisoquinoline | Rattus norvegicus (Norway rat) | Ki | 0.7689 | 5 | 9 |
| 2-(1-piperazinyl)-4-amino-6,7-dimethoxyquinazoline | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 2 |
| 1-phenethylamine, (r)-isomer | Rattus norvegicus (Norway rat) | Ki | 3,467,370,000.0000 | 1 | 1 |
| rauwolscine | Rattus norvegicus (Norway rat) | IC50 | 0.1650 | 1 | 1 |
| rauwolscine | Rattus norvegicus (Norway rat) | Ki | 0.0419 | 13 | 19 |
| bp 897 | Rattus norvegicus (Norway rat) | Ki | 0.0830 | 1 | 1 |
| 2-(2-benzofuranyl)-2-imidazoline | Rattus norvegicus (Norway rat) | Ki | 4.0000 | 2 | 3 |
| rs 100329 | Rattus norvegicus (Norway rat) | Ki | 0.0126 | 1 | 2 |
| pd 168,077 | Rattus norvegicus (Norway rat) | Ki | 0.1680 | 1 | 1 |
| a 61603 | Rattus norvegicus (Norway rat) | Ki | 2.9000 | 1 | 1 |
| dexmedetomidine | Rattus norvegicus (Norway rat) | Ki | 0.0013 | 4 | 4 |
| vinorelbine | Rattus norvegicus (Norway rat) | IC50 | 0.7000 | 1 | 1 |
| tracizoline | Rattus norvegicus (Norway rat) | Ki | 12.4473 | 3 | 4 |
| a 77636 | Rattus norvegicus (Norway rat) | Ki | 1.3000 | 1 | 2 |
| dihydrexidine | Rattus norvegicus (Norway rat) | Ki | 3.0000 | 2 | 3 |
| sk&f-38393 | Rattus norvegicus (Norway rat) | Ki | 3.0500 | 1 | 2 |
| cilansetron | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| n-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide | Rattus norvegicus (Norway rat) | Ki | 7.9433 | 1 | 1 |
| sodium selenate | Rattus norvegicus (Norway rat) | Ki | 0.0001 | 1 | 1 |
| rwj 52353 | Rattus norvegicus (Norway rat) | Ki | 0.0857 | 3 | 3 |
| 2-propyl-4,5,5a,6,7,11b-hexahydro-3-thia-5-azacyclopent-1-ena(c)phenanthrene-9,10-diol | Rattus norvegicus (Norway rat) | Ki | 4.0200 | 1 | 2 |
| ro 70-0004 | Rattus norvegicus (Norway rat) | Ki | 0.0631 | 1 | 2 |
| pi103 | Rattus norvegicus (Norway rat) | IC50 | 0.0110 | 1 | 1 |
| vn2222 | Rattus norvegicus (Norway rat) | Ki | 2.0000 | 1 | 1 |
| kni 10006 | Rattus norvegicus (Norway rat) | IC50 | 0.6900 | 1 | 1 |
| pnu 96415e | Rattus norvegicus (Norway rat) | Ki | 0.1400 | 1 | 1 |
| st 1936 | Rattus norvegicus (Norway rat) | Ki | 0.3000 | 1 | 1 |
| 3-trifluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline | Rattus norvegicus (Norway rat) | Ki | 800.2000 | 3 | 5 |
| abt-737 | Rattus norvegicus (Norway rat) | IC50 | 0.0003 | 1 | 1 |
| f21 | Rattus norvegicus (Norway rat) | Ki | 200.0000 | 1 | 1 |
| lassbio-579 | Rattus norvegicus (Norway rat) | Ki | 2.4900 | 1 | 1 |
| gsk 2126458 | Rattus norvegicus (Norway rat) | IC50 | 0.0012 | 1 | 1 |
| lgk974 | Rattus norvegicus (Norway rat) | IC50 | 0.0009 | 1 | 1 |
| clozapine | Rattus norvegicus (Norway rat) | IC50 | 3.5772 | 2 | 2 |
| clozapine | Rattus norvegicus (Norway rat) | Ki | 0.0758 | 6 | 7 |
| olanzapine | Rattus norvegicus (Norway rat) | Ki | 0.0100 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
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
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 (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
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
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
(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
A two-state homology model of the hERG K+ channel: application to ligand binding.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 15, Issue:6, 2005
A two-state homology model of the hERG K+ channel: application to ligand binding.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 15, Issue:6, 2005
The serotonin 5-HT4 receptor. 1. Design of a new class of agonists and receptor map of the agonist recognition site.Journal of medicinal chemistry, , Jun-23, Volume: 38, Issue:13, 1995
SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype.Journal of medicinal chemistry, , Apr-17, Volume: 35, Issue:8, 1992
Novel benzamides as selective and potent gastrokinetic agents. 2. Synthesis and structure-activity relationships of 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2- morpholinyl]methyl] benzamide citrate (AS-4370) and related compounds.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
New imidazoline/α(2)-adrenoceptors affecting compounds-4(5)-(2-aminoethyl)imidazoline (dihydrohistamine) derivatives. Synthesis and receptor affinity studies.Bioorganic & medicinal chemistry, , Jan-01, Volume: 19, Issue:1, 2011
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
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
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
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.Journal of medicinal chemistry, , Volume: 29, Issue:8, 1986
Two stereoisomeric imidazoline derivatives: synthesis and optical and alpha 2-adrenoceptor activities.Journal of medicinal chemistry, , Volume: 29, Issue:7, 1986
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
alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.Journal of medicinal chemistry, , Volume: 25, Issue:12, 1982
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
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
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
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
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
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 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
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
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 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.Journal of medicinal chemistry, , Volume: 25, Issue:12, 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
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
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
Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors.Bioorganic & medicinal chemistry, , Feb-01, Volume: 15, Issue:3, 2007
Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity towJournal of medicinal chemistry, , Aug-26, Volume: 47, Issue:18, 2004
Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Oct-21, Volume: 42, Issue:21, 1999
Synthesis, biochemical evaluation, and classical and three-dimensional quantitative structure-activity relationship studies of 7-substituted-1,2,3,4-tetrahydroisoquinolines and their relative affinities toward phenylethanolamine N-methyltransferase and thJournal of medicinal chemistry, , Jan-14, Volume: 42, Issue:1, 1999
3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor.Journal of medicinal chemistry, , Jun-03, Volume: 42, Issue:11, 1999
Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT.Bioorganic & medicinal chemistry letters, , Feb-08, Volume: 9, Issue:3, 1999
Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Sep-09, Volume: 42, Issue:18, 1999
Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
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
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
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 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.Journal of medicinal chemistry, , Volume: 25, Issue:12, 1982
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
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
1,3-dioxolane-based ligands as a novel class of alpha1-adrenoceptor antagonists.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
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
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 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.Journal of medicinal chemistry, , Volume: 25, Issue:12, 1982
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
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
Two stereoisomeric imidazoline derivatives: synthesis and optical and alpha 2-adrenoceptor activities.Journal of medicinal chemistry, , Volume: 29, Issue:7, 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
alpha-Adrenergic activities of some substituted 2-(aminomethyl)imidazolines.Journal of medicinal chemistry, , Volume: 26, Issue:12, 1983
Syntheses and adrenergic agonist properties of ring-fluorinated isoproterenols.Journal of medicinal chemistry, , Volume: 25, Issue:6, 1982
alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.Journal of medicinal chemistry, , Volume: 25, Issue:12, 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
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 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.Journal of medicinal chemistry, , Volume: 25, Issue:12, 1982
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
alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.Journal of medicinal chemistry, , Volume: 25, Issue:12, 1982
Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors.Bioorganic & medicinal chemistry, , Feb-01, Volume: 15, Issue:3, 2007
Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
Synthesis, biochemical evaluation, and classical and three-dimensional quantitative structure-activity relationship studies of 7-substituted-1,2,3,4-tetrahydroisoquinolines and their relative affinities toward phenylethanolamine N-methyltransferase and thJournal of medicinal chemistry, , Jan-14, Volume: 42, Issue:1, 1999
Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Oct-21, Volume: 42, Issue:21, 1999
Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor.Journal of medicinal chemistry, , Jun-03, Volume: 42, Issue:11, 1999
Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT.Bioorganic & medicinal chemistry letters, , Feb-08, Volume: 9, Issue:3, 1999
Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT.Bioorganic & medicinal chemistry letters, , Feb-08, Volume: 9, Issue:3, 1999
Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
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
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
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
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-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
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
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.Journal of medicinal chemistry, , Volume: 29, Issue:8, 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
Pyridinylpiperazines, a new class of selective alpha 2-adrenoceptor antagonists.Journal of medicinal chemistry, , Volume: 26, Issue:12, 1983
alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.Journal of medicinal chemistry, , Volume: 25, Issue:12, 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
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
Synthesis and alpha 2-adrenoceptor antagonist activity of some disulfonamidobenzoquinolizines.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
(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
Pyridinylpiperazines, a new class of selective alpha 2-adrenoceptor antagonists.Journal of medicinal chemistry, , Volume: 26, Issue:12, 1983
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.Journal of medicinal chemistry, , Jan-19, Volume: 39, Issue:2, 1996
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.Journal of medicinal chemistry, , Jan-19, Volume: 39, Issue:2, 1996
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
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
Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Binding of an imidazopyridoindole at imidazoline I2 receptors.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT.Bioorganic & medicinal chemistry letters, , Feb-08, Volume: 9, Issue:3, 1999
Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Sep-09, Volume: 42, Issue:18, 1999
Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors.Bioorganic & medicinal chemistry, , Feb-01, Volume: 15, Issue:3, 2007
Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity towJournal of medicinal chemistry, , Aug-26, Volume: 47, Issue:18, 2004
Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Oct-21, Volume: 42, Issue:21, 1999
Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT.Bioorganic & medicinal chemistry letters, , Feb-08, Volume: 9, Issue:3, 1999
Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Sep-09, Volume: 42, Issue:18, 1999
Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
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
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
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
alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.Journal of medicinal chemistry, , Volume: 25, Issue:12, 1982
Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Sep-09, Volume: 42, Issue:18, 1999
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
6-methoxy-7-benzofuranoxy and 6-methoxy-7-indolyloxy analogues of 2-[2-(2,6-Dimethoxyphenoxy)ethyl]aminomethyl-1,4-benzodioxane (WB4101):1 discovery of a potent and selective α1D-adrenoceptor antagonist.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
1,3-dioxolane-based ligands as a novel class of alpha1-adrenoceptor antagonists.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Oct-21, Volume: 42, Issue:21, 1999
Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor.Journal of medicinal chemistry, , Jun-03, Volume: 42, Issue:11, 1999
Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Sep-09, Volume: 42, Issue:18, 1999
Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
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
Structure-activity studies for a novel series of N-(arylethyl)-N-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)-N-methylamine s possessing dual 5-HT uptake inhibiting and alpha2-antagonistic activities.Journal of medicinal chemistry, , Mar-28, Volume: 40, Issue:7, 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
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
alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.Journal of medicinal chemistry, , Volume: 25, Issue:12, 1982
Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Binding of an imidazopyridoindole at imidazoline I2 receptors.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
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
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. 1. (Imidazolylmethyl)oxazoles and -thiazoles.Journal of medicinal chemistry, , Dec-16, Volume: 42, Issue:25, 1999
Binding of an imidazopyridoindole at imidazoline I2 receptors.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
2-(2-Phenylcyclopropyl)imidazolines: reversed enantioselective interaction at I(1) and I(2) imidazoline receptors.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.Journal of medicinal chemistry, , May-23, Volume: 40, Issue:11, 1997
(5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacJournal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
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
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
Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT.Bioorganic & medicinal chemistry letters, , Feb-08, Volume: 9, Issue:3, 1999
Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.Journal of medicinal chemistry, , Sep-09, Volume: 42, Issue:18, 1999
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
Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.European journal of medicinal chemistry, , Volume: 62, 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
A two-state homology model of the hERG K+ channel: application to ligand binding.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 15, Issue:6, 2005
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
N-aryl-N'-benzylpiperazines as potential antipsychotic agents.Journal of medicinal chemistry, , Oct-13, Volume: 38, Issue:21, 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