Relation Results

Summary

Name ADRA1A
Full Name Alpha-1A adrenergic receptor
Synonyms Alpha-1A adrenoreceptor, Alpha-1A adrenoceptor, Alpha-1C adrenergic receptor, Alpha-adrenergic receptor 1c | ADRA1C
Primary ID P35348
Links - -
Type protein
Relations 21
Pathways GPCR_HCC
Inhibitors tamsulosin; 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione; terazosin; silodosin; N-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanamine; phentolamine; (4S)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid O5-[3-(4,4-diphenyl-1-piperidinyl)propyl] ester O3-methyl ester; prazosin
Function This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system ...
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Type: Score: Layout: SPV 
0.80.5830.80.80.80.80.80.80.80.2920.5710.80.430.80.80.6210.2780.80.8oxymetazolineADRA1AGNAQtamsulosin8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione(R)-noradrenalineterazosin(S)-adrenaline(R)-adrenalinesilodosinGNASGNA11methoxamineGNA14N-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanaminephentolamineGNA13GNAL(4S)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid O5-[3-(4,4-diphenyl-1-piperidinyl)propyl] ester O3-methyl esterprazosin

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Relations
Regulator
Mechanism
target
score ℹ
+ oxymetazolineup-regulates activity img/direct-activation.png chemical activation ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258462 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ ADRA1Aup-regulates activity img/direct-activation.png binding GNAQ 0.583
Identifier Residue Sequence Organism Cell Line
SIGNOR-257084 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ tamsulosindown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258474 Cricetulus griseus
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dionedown-regulates img/direct_inhibition.png chemical inhibition ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-190604 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ (R)-noradrenalineup-regulates activity img/direct-activation.png chemical activation ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-257450 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Identifier Residue Sequence Organism Cell Line
SIGNOR-258456 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 2 Organism: Homo Sapiens, Cricetulus Griseus
+ terazosindown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258671 Homo sapiens
pmid sentence
Pharmacological management of benign prostatic hyperplasia (BPH) has most successfully been achieved by administration of α1 antagonists, which function via relaxation of prostatic smooth muscle. Terazosin2 (2), doxazosin3 (3), and alfuzosin4 (4), agents currently approved for this indication
Publications: 1 Organism: Homo Sapiens
Tissue: Smooth Muscle
+ (S)-adrenalineup-regulates activity img/direct-activation.png chemical activation ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258454 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ (R)-adrenalineup-regulates activity img/direct-activation.png chemical activation ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258458 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ silodosindown-regulates img/direct_inhibition.png chemical inhibition ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-206914 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ ADRA1Aup-regulates activity img/direct-activation.png binding GNAS 0.292
Identifier Residue Sequence Organism Cell Line
SIGNOR-256812 Homo sapiens
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ‚â• -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ‚â• -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ‚â• -1.0.
Publications: 1 Organism: Homo Sapiens
+ ADRA1Aup-regulates activity img/direct-activation.png binding GNA11 0.571
Identifier Residue Sequence Organism Cell Line
SIGNOR-278121 Chlorocebus aethiops COS-7 Cell
pmid sentence
In this report, we demonstrate that in transfected cos-7 cells Gal4 and Ga16, like Gaq and Ga11, can activate PIPLC j3l and that all three al-ARs, alA, alB and alC, can activate endogenous PI-PLC by coupling to Gaq or Ga11.
Publications: 1 Organism: Chlorocebus Aethiops
+ methoxamineup-regulates activity img/direct-activation.png chemical activation ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258455 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ ADRA1Aup-regulates activity img/direct-activation.png binding GNA14 0.43
Identifier Residue Sequence Organism Cell Line
SIGNOR-257195 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ N-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanaminedown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258472 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ phentolaminedown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258445 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ ADRA1Aup-regulates activity img/direct-activation.png binding GNA13 0.621
Identifier Residue Sequence Organism Cell Line
SIGNOR-257279 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ silodosindown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258450 Cricetulus griseus
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ ADRA1Aup-regulates activity img/direct-activation.png binding GNAL 0.278
Identifier Residue Sequence Organism Cell Line
SIGNOR-256955 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ (4S)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid O5-[3-(4,4-diphenyl-1-piperidinyl)propyl] ester O3-methyl esterdown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258463 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ prazosindown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258473 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
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