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Alpha-1B adrenergic receptor
An alpha-1B adrenergic receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P35368]
Synonyms
Alpha-1B adrenoreceptor;
Alpha-1B adrenoceptor
Research
Bioassay Publications (143)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 11 (7.69) | 18.7374 |
| 1990's | 28 (19.58) | 18.2507 |
| 2000's | 54 (37.76) | 29.6817 |
| 2010's | 44 (30.77) | 24.3611 |
| 2020's | 6 (4.20) | 2.80 |
Compounds (129)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 8-hydroxy-2-(di-n-propylamino)tetralin | Homo sapiens (human) | Ki | 2.1056 | 9 | 9 |
| 1-(2-methoxyphenyl)piperazine | Homo sapiens (human) | Ki | 0.5100 | 1 | 1 |
| 1-(3-chlorophenyl)piperazine | Homo sapiens (human) | Ki | 0.2360 | 1 | 1 |
| alfuzosin | Homo sapiens (human) | IC50 | 0.0230 | 1 | 1 |
| alfuzosin | Homo sapiens (human) | Ki | 0.0083 | 3 | 3 |
| amlodipine | Homo sapiens (human) | Ki | 7.9430 | 1 | 1 |
| apraclonidine | Homo sapiens (human) | Ki | 0.1800 | 1 | 1 |
| atenolol | Homo sapiens (human) | IC50 | 0.2300 | 1 | 1 |
| azelastine | Homo sapiens (human) | Ki | 0.0501 | 3 | 3 |
| bmy 7378 | Homo sapiens (human) | Ki | 0.5075 | 15 | 15 |
| bunazosin | Homo sapiens (human) | IC50 | 0.0012 | 1 | 1 |
| cisapride | Homo sapiens (human) | IC50 | 0.0300 | 2 | 2 |
| clonidine | Homo sapiens (human) | Ki | 0.3428 | 3 | 3 |
| [4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2,3,4a,5,6,7,8,8a-octahydroquinoxalin-1-yl]-(2-furanyl)methanone | Homo sapiens (human) | Ki | 0.0006 | 1 | 1 |
| doxazosin | Homo sapiens (human) | Ki | 0.0008 | 5 | 5 |
| ebastine | Homo sapiens (human) | IC50 | 0.1830 | 1 | 1 |
| haloperidol | Homo sapiens (human) | Ki | 0.0124 | 2 | 2 |
| kojic acid | Homo sapiens (human) | IC50 | 8.3300 | 1 | 1 |
| 1-(3-trifluoromethylphenyl)piperazine | Homo sapiens (human) | Ki | 0.3370 | 1 | 1 |
| naftopidil | Homo sapiens (human) | IC50 | 0.6340 | 2 | 2 |
| naftopidil | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| nan 190 | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| oxymetazoline | Homo sapiens (human) | Ki | 0.3593 | 3 | 3 |
| moxonidine | Homo sapiens (human) | Ki | 15.5000 | 2 | 2 |
| prazosin | Homo sapiens (human) | IC50 | 0.0006 | 4 | 4 |
| prazosin | Homo sapiens (human) | Ki | 0.0021 | 17 | 18 |
| quetiapine | Homo sapiens (human) | Ki | 0.0232 | 3 | 3 |
| risperidone | Homo sapiens (human) | Ki | 0.0053 | 5 | 5 |
| spiperone | Homo sapiens (human) | Ki | 0.0071 | 1 | 1 |
| terazosin | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| terazosin | Homo sapiens (human) | Ki | 0.0504 | 11 | 13 |
| terfenadine | Homo sapiens (human) | IC50 | 2.3400 | 1 | 1 |
| 5-methylurapidil | Homo sapiens (human) | Ki | 0.2223 | 3 | 3 |
| n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamide | Homo sapiens (human) | Ki | 0.1301 | 4 | 4 |
| wb 4101 | Homo sapiens (human) | Ki | 0.0174 | 12 | 14 |
| xylometazoline | Homo sapiens (human) | Ki | 0.0910 | 1 | 1 |
| zotepine | Homo sapiens (human) | Ki | 0.0034 | 1 | 1 |
| phentolamine | Homo sapiens (human) | IC50 | 0.0108 | 1 | 1 |
| phentolamine | Homo sapiens (human) | Ki | 0.0261 | 2 | 2 |
| phenylephrine | Homo sapiens (human) | Ki | 1.2589 | 1 | 1 |
| salicylaldehyde | Homo sapiens (human) | IC50 | 833.0000 | 1 | 1 |
| phenylpiperazine | Homo sapiens (human) | Ki | 0.7940 | 1 | 1 |
| yohimbine | Homo sapiens (human) | Ki | 0.3248 | 3 | 3 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| n-methyllaurotetanine | Homo sapiens (human) | Ki | 0.9500 | 1 | 1 |
| pizotyline | Homo sapiens (human) | Ki | 0.0750 | 1 | 1 |
| indoramin | Homo sapiens (human) | Ki | 0.0313 | 3 | 3 |
| ipsapirone | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| ipsapirone | Homo sapiens (human) | Ki | 0.2245 | 2 | 2 |
| sertindole | Homo sapiens (human) | Ki | 0.0018 | 1 | 1 |
| niguldipine | Homo sapiens (human) | Ki | 0.1238 | 4 | 4 |
| 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 |
| atipamezole | Homo sapiens (human) | Ki | 1.9498 | 1 | 1 |
| corynanthine | Homo sapiens (human) | Ki | 0.5170 | 1 | 1 |
| way 100635 | Homo sapiens (human) | Ki | 0.3220 | 1 | 1 |
| gr 127935 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| 6-chloro-2-(1-piperazinyl)pyrazine | Homo sapiens (human) | Ki | 0.9130 | 1 | 1 |
| roemerine | Homo sapiens (human) | Ki | 3.1623 | 1 | 1 |
| uh 301 | Homo sapiens (human) | Ki | 6.0800 | 1 | 1 |
| sk&f 104078 | Homo sapiens (human) | Ki | 0.0870 | 1 | 1 |
| sk&f 86466 | Homo sapiens (human) | Ki | 0.4850 | 1 | 1 |
| sk&f 104856 | Homo sapiens (human) | Ki | 0.0220 | 3 | 3 |
| tamsulosin | Homo sapiens (human) | IC50 | 0.0045 | 2 | 2 |
| tamsulosin | Homo sapiens (human) | Ki | 0.0124 | 8 | 10 |
| cyclazosin | Homo sapiens (human) | Ki | 0.0003 | 6 | 6 |
| sc 53116 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sc 53116 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| rec 15-2739 | Homo sapiens (human) | Ki | 0.0178 | 2 | 2 |
| asenapine | Homo sapiens (human) | Ki | 0.0012 | 1 | 1 |
| abanoquil | Homo sapiens (human) | Ki | 0.0001 | 2 | 2 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 1.1910 | 1 | 1 |
| eptapirone | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| bmy 7378 | Homo sapiens (human) | Ki | 0.4630 | 3 | 3 |
| fipamezole | Homo sapiens (human) | Ki | 2.0893 | 1 | 1 |
| rauwolscine | Homo sapiens (human) | Ki | 0.7584 | 3 | 3 |
| mitragynine | Homo sapiens (human) | Ki | 4.7700 | 1 | 1 |
| bp 897 | Homo sapiens (human) | Ki | 0.0150 | 2 | 2 |
| rs 100329 | Homo sapiens (human) | Ki | 0.0316 | 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 | 0.0018 | 4 | 4 |
| a 61603 | Homo sapiens (human) | Ki | 2.0893 | 1 | 1 |
| le 300 | Homo sapiens (human) | Ki | 0.0110 | 1 | 1 |
| harmine | Homo sapiens (human) | Ki | 5.4050 | 2 | 2 |
| l 745870 | Homo sapiens (human) | Ki | 2.9000 | 1 | 1 |
| silodosin | Homo sapiens (human) | IC50 | 0.3287 | 2 | 2 |
| silodosin | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| sb 258719 | Homo sapiens (human) | Ki | 15.8489 | 1 | 1 |
| sb 271046 | Homo sapiens (human) | Ki | 1.9953 | 1 | 1 |
| ro 25-6981 | Homo sapiens (human) | Ki | 0.1800 | 1 | 1 |
| sb 269970 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| dexniguldipine | Homo sapiens (human) | Ki | 0.1465 | 3 | 4 |
| vilazodone | Homo sapiens (human) | IC50 | 1.9800 | 1 | 1 |
| n-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide | Homo sapiens (human) | Ki | 7.9433 | 1 | 1 |
| sb258741 | Homo sapiens (human) | Ki | 3.1623 | 1 | 1 |
| ro 70-0004 | Homo sapiens (human) | Ki | 0.0794 | 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 |
| 4-(3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl)-1-(4-fluorophenyl)butan-1-one | Homo sapiens (human) | Ki | 0.0720 | 1 | 2 |
| 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 | 0.0650 | 1 | 1 |
| tert-butyl peroxybenzoate | Homo sapiens (human) | Ki | 0.0190 | 1 | 1 |
| 77-lh-28-1 | Homo sapiens (human) | Ki | 0.7762 | 1 | 1 |
| fauc 365 | Homo sapiens (human) | Ki | 0.9133 | 3 | 3 |
| fauc 113 | Homo sapiens (human) | Ki | 0.0036 | 1 | 1 |
| a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| gsk 1004723 | Homo sapiens (human) | Ki | 0.0316 | 3 | 3 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
| bix 02565 | Homo sapiens (human) | IC50 | 0.0520 | 1 | 0 |
| clozapine | Homo sapiens (human) | Ki | 0.0203 | 5 | 5 |
| olanzapine | Homo sapiens (human) | Ki | 0.0251 | 4 | 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
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
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
The discovery of quinoline based single-ligand human HBioorganic & medicinal chemistry letters, , 12-15, Volume: 26, Issue:24, 2016
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.Bioorganic & medicinal chemistry, , Oct-15, Volume: 20, Issue:20, 2012
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
[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
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. 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
Design, synthesis, and biological activity of prazosin-related antagonists. Role of the piperazine and furan units of prazosin on the selectivity for alpha1-adrenoreceptor subtypes.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.Journal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
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
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 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
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
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
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]Bioorganic & medicinal chemistry letters, , 02-15, Volume: 28, Issue:4, 2018
[no title available]Bioorganic & medicinal chemistry letters, , 05-15, Volume: 28, Issue:9, 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 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 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
Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
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
Design, synthesis, and biological evaluation of prazosin-related derivatives as multipotent compounds.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
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
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
Design, synthesis, and biological activity of prazosin-related antagonists. Role of the piperazine and furan units of prazosin on the selectivity for alpha1-adrenoreceptor subtypes.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.Journal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Dec-17, Volume: 41, Issue:26, 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 biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.Journal of medicinal chemistry, , Nov-08, Volume: 39, Issue:23, 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
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
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]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
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as αBioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
α-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one.Bioorganic & medicinal chemistry, , May-01, Volume: 23, Issue:9, 2015
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
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
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
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
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
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
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
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptoJournal of medicinal chemistry, , May-26, Volume: 54, Issue:10, 2011
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
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
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
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Synthesis, absolute configuration, and biological profile of the enantiomers of trans-[2-(2,6-dimethoxyphenoxy)ethyl] [(3-p-tolyl-2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amine (mephendioxan), a potent competitive alpha 1A-adrenoreceptor antagonist.Journal of medicinal chemistry, , May-24, Volume: 39, Issue:11, 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
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
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
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
Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as αBioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
α-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one.Bioorganic & medicinal chemistry, , May-01, Volume: 23, Issue:9, 2015
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Alpha- 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
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
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
Synthesis, absolute configuration, and biological profile of the enantiomers of trans-[2-(2,6-dimethoxyphenoxy)ethyl] [(3-p-tolyl-2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amine (mephendioxan), a potent competitive alpha 1A-adrenoreceptor antagonist.Journal of medicinal chemistry, , May-24, Volume: 39, Issue:11, 1996
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
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]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
Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as αBioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selective αJournal of medicinal chemistry, , Oct-27, Volume: 59, Issue:20, 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
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
Pharmacological options in the treatment of benign prostatic hyperplasia.Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 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
Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.Journal of medicinal chemistry, , Nov-08, Volume: 39, Issue:23, 1996
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. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
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
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
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
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
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selective αJournal of medicinal chemistry, , Oct-27, Volume: 59, Issue:20, 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
The discovery of quinoline based single-ligand human HBioorganic & medicinal chemistry letters, , 12-15, Volume: 26, Issue:24, 2016
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.Bioorganic & medicinal chemistry, , Oct-15, Volume: 20, Issue:20, 2012
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
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]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
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| protein heterodimerization activity | molecular function | Binding to a nonidentical protein to form a heterodimer. [GOC:ai] |
| 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 5 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| 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] |
| caveola | cellular component | A membrane raft that forms small pit, depression, or invagination that communicates with the outside of a cell and extends inward, indenting the cytoplasm and the cell membrane. Examples include flask-shaped invaginations of the plasma membrane in adipocytes associated with caveolin proteins, and minute pits or incuppings of the cell membrane formed during pinocytosis. Caveolae may be pinched off to form free vesicles within the cytoplasm. [GOC:mah, ISBN:0721662544, PMID:16645198] |
| nuclear membrane | cellular component | Either of the lipid bilayers that surround the nucleus and form the nuclear envelope; excludes the intermembrane space. [GOC:mah, GOC:pz] |
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 11 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] |
| regulation of vasoconstriction | biological process | Any process that modulates the frequency, rate or extent of reductions in the diameter of blood vessels. [GOC:jl] |
| intracellular signal transduction | biological process | The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782] |
| 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] |
| regulation of cardiac muscle contraction | biological process | Any process that modulates the frequency, rate or extent of cardiac muscle contraction. [GOC:ecd] |
| 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] |
| 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] |
| 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] |
| 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] |