Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C18H20N4O |
| Molecular Weight | 308.3776 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O[C@H]1CC[C@@H](CC1)NC2=NC(=NC3=C2C=CN3)C4=CC=CC=C4
InChI
InChIKey=RBZNJGHIKXAKQE-HDJSIYSDSA-N
InChI=1S/C18H20N4O/c23-14-8-6-13(7-9-14)20-18-15-10-11-19-17(15)21-16(22-18)12-4-2-1-3-5-12/h1-5,10-11,13-14,23H,6-9H2,(H2,19,20,21,22)/t13-,14-
| Molecular Formula | C18H20N4O |
| Molecular Weight | 308.3776 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/19639278Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800016704 | https://www.ncbi.nlm.nih.gov/pubmed/17558436 |
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19639278
Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800016704 | https://www.ncbi.nlm.nih.gov/pubmed/17558436 |
Derenofyllin (SLV320) is a selective adenosine A1 receptor antagonist, which is under investigation for the treatment of heart failure with renal dysfunction. Adverse events considered related to SLV320 were dizziness, nausea, transient hypertension and transient hypotension.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL226 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17558436 |
9.0 null [pKi] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
245 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19919976 |
15 mg single, intravenous dose: 15 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
DERENOFYLLINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
144 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19919976 |
10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
DERENOFYLLINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
427 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19919976 |
15 mg single, intravenous dose: 15 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
DERENOFYLLINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
235 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19919976 |
10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
DERENOFYLLINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.13 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19919976 |
15 mg single, intravenous dose: 15 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
DERENOFYLLINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19919976 |
10 mg single, intravenous dose: 10 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
DERENOFYLLINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
15 mg 2 times / day multiple, intravenous Highest studied dose Dose: 15 mg, 2 times / day Route: intravenous Route: multiple Dose: 15 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
|
15 mg single, intravenous Highest studied dose Dose: 15 mg Route: intravenous Route: single Dose: 15 mg Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Cardio-renal effects of the A1 adenosine receptor antagonist SLV320 in patients with heart failure. | 2009-11 |
|
| A1 adenosine receptor antagonists, agonists, and allosteric enhancers. | 2009 |
|
| The adenosine A1 receptor antagonist SLV320 reduces myocardial fibrosis in rats with 5/6 nephrectomy without affecting blood pressure. | 2007-08 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19919976
1-hour infusion of 5, 10, and 15 mg SLV320
Route of Administration:
Intravenous
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:41:44 GMT 2025
by
admin
on
Mon Mar 31 18:41:44 GMT 2025
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| Record UNII |
O1Q96UZ63W
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| Record Status |
Validated (UNII)
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| Record Version |
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NCI_THESAURUS |
C319
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9208
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251945-92-3
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DB12446
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