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Alpha-1A adrenergic receptor
An alpha-1A adrenergic receptor that is encoded in the genome of cow. [OMA:P18130, PRO:DNx]
Synonyms
Alpha-1A adrenoreceptor;
Alpha-1A adrenoceptor;
Alpha-1C adrenergic receptor
Research
Bioassay Publications (13)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 2 (15.38) | 18.7374 |
| 1990's | 6 (46.15) | 18.2507 |
| 2000's | 3 (23.08) | 29.6817 |
| 2010's | 2 (15.38) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (33)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| octoclothepine | Bos taurus (cattle) | Ki | 0.0007 | 1 | 1 |
| alfuzosin | Bos taurus (cattle) | Ki | 0.0230 | 1 | 1 |
| bmy 7378 | Bos taurus (cattle) | Ki | 0.0430 | 1 | 1 |
| [4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2,3,4a,5,6,7,8,8a-octahydroquinoxalin-1-yl]-(2-furanyl)methanone | Bos taurus (cattle) | Ki | 0.0059 | 2 | 2 |
| doxazosin | Bos taurus (cattle) | Ki | 0.7290 | 1 | 4 |
| oxymetazoline | Bos taurus (cattle) | Ki | 0.0132 | 1 | 1 |
| prazosin | Bos taurus (cattle) | Ki | 1.0667 | 5 | 8 |
| spiperone | Bos taurus (cattle) | Ki | 0.0135 | 1 | 1 |
| terazosin | Bos taurus (cattle) | Ki | 2.4728 | 3 | 6 |
| 5-methylurapidil | Bos taurus (cattle) | Ki | 0.0025 | 2 | 2 |
| wb 4101 | Bos taurus (cattle) | Ki | 0.0025 | 3 | 6 |
| phentolamine | Bos taurus (cattle) | Ki | 0.0038 | 2 | 2 |
| phenylephrine | Bos taurus (cattle) | Ki | 0.9332 | 1 | 1 |
| yohimbine | Bos taurus (cattle) | Ki | 0.0036 | 1 | 1 |
| indoramin | Bos taurus (cattle) | Ki | 0.0120 | 1 | 1 |
| sertindole | Bos taurus (cattle) | Ki | 0.0004 | 3 | 3 |
| niguldipine | Bos taurus (cattle) | Ki | 0.0004 | 1 | 1 |
| mianserin hydrochloride | Bos taurus (cattle) | IC50 | 0.1087 | 3 | 3 |
| 1,2,3,4,6,7,12,12b-octahydroindolo(2,3-a)quinolizine | Bos taurus (cattle) | Ki | 0.0380 | 1 | 1 |
| sk&f 104078 | Bos taurus (cattle) | Ki | 0.1140 | 1 | 4 |
| tamsulosin | Bos taurus (cattle) | Ki | 0.0001 | 1 | 1 |
| cyclazosin | Bos taurus (cattle) | Ki | 0.0024 | 1 | 1 |
| abanoquil | Bos taurus (cattle) | Ki | 0.0000 | 1 | 1 |
| l 691121 | Bos taurus (cattle) | IC50 | 1.5000 | 1 | 1 |
| tretinoin | Bos taurus (cattle) | Ki | 0.0004 | 1 | 1 |
| rs 17053 | Bos taurus (cattle) | Ki | 0.0008 | 1 | 1 |
| a 61603 | Bos taurus (cattle) | Ki | 0.0302 | 1 | 1 |
| fenretinide | Bos taurus (cattle) | Ki | 2.2000 | 1 | 1 |
| octoclothepine, (s)-isomer | Bos taurus (cattle) | Ki | 0.0004 | 2 | 2 |
Drugs with Activation Measurements
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
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
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
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 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
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
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
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
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
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 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
[no title available],
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.Bioorganic & medicinal chemistry, , Jan-01, Volume: 21, Issue:1, 2013
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
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
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003