Page last updated: 2024-12-11
bw a1433
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
BW A1433: adenosine receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 6439089 |
| CHEMBL ID | 16997 |
| SCHEMBL ID | 6555024 |
| SCHEMBL ID | 6555021 |
| MeSH ID | M0158059 |
Synonyms (31)
| Synonym |
|---|
| 3-[4-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1h-purin-8-yl)-phenyl]-acrylic acid |
| (e)-3-[4-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1h-purin-8-yl)-phenyl]-acrylic acid |
| bdbm50037440 |
| gtpl443 |
| (e)-3-(4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1h-purin-8-yl)phenyl)-2-propenoic acid |
| 2-propenoic acid, 3-(4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1h-purin-8-yl)phenyl)-, (e)- |
| (e)-4-(1,2,3,6-tetrahydro-2,6-dioxo-1,3-dipropyl-9h-purin-8-yl)cinnamic acid |
| PDSP2_000306 |
| PDSP1_000308 |
| PDSP2_000444 |
| PDSP1_000446 |
| bw a1433 |
| CHEMBL16997 , |
| UGCOFEOEBHUEHA-JXMROGBWSA-N , |
| (e)-3-[4-(2,6-dioxo-1,3-dipropyl-7h-purin-8-yl)phenyl]prop-2-enoic acid |
| bdbm85036 |
| nsc_129447 |
| cas_129447 |
| 106465-45-6 |
| 2-propenoic acid, 3-(4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1h-purin-8-yl)phenyl)- |
| 121496-66-0 |
| bw-a1433 |
| 1,3-dipropyl-8-(4-acrylate)phenylxanthine |
| bwa-1433 |
| 4-(1,2,3,6-tetrahydro-2,6-dioxo-1,3-dipropyl-9h-purin-8-yl)cinnamic acid |
| bwa1433 |
| bwa 1433 |
| SCHEMBL6555024 |
| SCHEMBL6555021 |
| Q27075599 |
| AKOS040750955 |
Research Excerpts
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " BWA1433U induced a parallel shift of the adenosine dose-response curve to the right; however, it had no significant inhibitory effect on the decrease in lobar arterial pressure in response to ATP." | ( Adenosine does not mediate the pulmonary vasodilator response of adenosine 5'-triphosphate in the feline pulmonary vascular bed. Hyman, AL; Kadowitz, PJ; Lippton, H; Neely, CF; Neiman, M, 1989) | 0.28 |
| " When measured in the presence of antagonists, the dose-response curves of NECA-induced inhibition of forskolin-stimulated cAMP accumulation were right-shifted." | ( Molecular cloning and characterization of the human A3 adenosine receptor. Jacobson, MA; Johnson, RG; Linden, J; Salvatore, CA; Taylor, HE, 1993) | 0.29 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (7)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 0.0300 | 0.0000 | 0.9306 | 10.0000 | AID32762; AID34864 |
| Adenosine receptor A1 | Rattus norvegicus (Norway rat) | Ki | 0.0150 | 0.0001 | 1.2092 | 9.9700 | AID32496; AID32514 |
| Adenosine receptor A3 | Rattus norvegicus (Norway rat) | Ki | 15.0000 | 0.0003 | 0.9196 | 9.0000 | AID33354; AID33486 |
| Adenosine receptor A2a | Homo sapiens (human) | Ki | 0.1900 | 0.0000 | 1.0609 | 9.7920 | AID34250 |
| Adenosine receptor A2b | Homo sapiens (human) | Ki | 0.0600 | 0.0002 | 1.6352 | 10.0000 | AID33475; AID7693 |
| Adenosine receptor A1 | Homo sapiens (human) | Ki | 0.1400 | 0.0002 | 0.9316 | 10.0000 | AID30463 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | Ki | 0.8000 | 0.0002 | 1.4940 | 10.0000 | AID33008; AID33940 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (105)
Molecular Functions (16)
Ceullar Components (19)
Bioassays (25)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID230534 | Ratio of selectivity for A3 and A1 receptors at rat brain | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors. |
| AID234382 | Selectivity ratio of hA2A to hA2B | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. |
| AID32762 | Inhibition of [3H]PSB-11 binding to human Adenosine A3 receptor | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists. |
| AID34864 | Antagonist activity against human adenosine A3 receptor expressed in HEK cells in presence of [125]IAB-MECA or [125I]IABA radioligand. | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. |
| AID33475 | Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptor | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists. |
| AID230535 | Ratio of selectivity for A3 and A2a receptors at rat brain | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors. |
| AID229658 | Selectivity ratio (A1/A2B) | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists. |
| AID33008 | Inhibition of [3H]MSX-2 binding to rat adenosine A2A receptor | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists. |
| AID32335 | Antagonist activity against adenosine A1 receptor in rat brain membrane in presence of [3H]R-PIA radioligand. | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. |
| AID33486 | Displacement of [125I]AB-MECA from membranes of CHO cells stably transfected with the rat adenosine A3 receptor cDNA | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors. |
| AID229657 | Selectivity ratio (A3/A2B). | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists. |
| AID32514 | Displacement of [3H]PIA from adenosine A1 receptors of rat brain membrane | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors. |
| AID7693 | Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. |
| AID34250 | Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand. | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. |
| AID229656 | Selectivity ratio of the compound( A2A/A2B) | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists. |
| AID30463 | Antagonist activity against recombinant human adenosine A1 receptor expressed in HEK293 cells in presence of [125I]IABA radioligand. | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. |
| AID234383 | Selectivity ratio of hA3 to hA2B | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. |
| AID32496 | Inhibition of [3H]CCPA binding to rat adenosine A1 receptor | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists. |
| AID234381 | Selectivity ratio of hA1 to hA2B | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. |
| AID33354 | Antagonist activity against rat adenosine A3 receptor using [125I]I-AB-MECA or [125 I]IABA | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. |
| AID33940 | Displacement of [3H]-CGS- 21680 from adenosine A2a receptors of rat striatal membrane | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors. |
| AID32886 | Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand. | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. |
| AID1345822 | Human A3 receptor (Adenosine receptors) | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Nov-01, Volume: 90, Issue:21 | Molecular cloning and characterization of the human A3 adenosine receptor. |
| AID1345831 | Rat A3 receptor (Adenosine receptors) | 1994 | The Journal of biological chemistry, Oct-07, Volume: 269, Issue:40 | Role of the second extracellular loop of adenosine receptors in agonist and antagonist binding. Analysis of chimeric A1/A3 adenosine receptors. |
| AID1345721 | Human A2B receptor (Adenosine receptors) | 1999 | Molecular pharmacology, Oct, Volume: 56, Issue:4 | Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (23)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 2 (8.70) | 18.7374 |
| 1990's | 15 (65.22) | 18.2507 |
| 2000's | 6 (26.09) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 11.99
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (11.99) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 23 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||