Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C31H44N2O10.2ClH.H2O |
| Molecular Weight | 695.626 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.Cl.Cl.COC1=CC(=CC(OC)=C1OC)C(=O)OCCCN2CCCN(CCCOC(=O)C3=CC(OC)=C(OC)C(OC)=C3)CC2
InChI
InChIKey=KJDHWPSHIIFNAK-UHFFFAOYSA-N
InChI=1S/C31H44N2O10.2ClH.H2O/c1-36-24-18-22(19-25(37-2)28(24)40-5)30(34)42-16-8-12-32-10-7-11-33(15-14-32)13-9-17-43-31(35)23-20-26(38-3)29(41-6)27(21-23)39-4;;;/h18-21H,7-17H2,1-6H3;2*1H;1H2
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C31H44N2O10 |
| Molecular Weight | 604.6885 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | H2O |
| Molecular Weight | 18.0153 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Dilazep is a coronary and cerebral vasodilator as an adenosine reuptake inhibitor. Dilazep is an inhibitor of platelet aggregation and of membrane transport of nucleosides. Dilazep is also known to have a vasodilating effect on renal vessels and is often used in patients with ischaemic heart disease, cerebral ischemia or renal dysfunction to improve tissue circulation.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL1997 |
17.5 nM [IC50] | ||
Target ID: CHEMBL3509606 |
8800.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Preventing | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Molecular cloning and characterization of a nitrobenzylthioinosine-insensitive (ei) equilibrative nucleoside transporter from human placenta. | 1997 Dec 15 |
|
| Molecular cloning and functional characterization of nitrobenzylthioinosine (NBMPR)-sensitive (es) and NBMPR-insensitive (ei) equilibrative nucleoside transporter proteins (rENT1 and rENT2) from rat tissues. | 1997 Nov 7 |
|
| Chimeric constructs between human and rat equilibrative nucleoside transporters (hENT1 and rENT1) reveal hENT1 structural domains interacting with coronary vasoactive drugs. | 1998 Aug 21 |
|
| Dipyridamole and dilazep suppress oxygen radicals in puromycin aminonucleoside nephrosis rats. | 1998 Nov |
|
| Molecular cloning and functional characterization of inhibitor-sensitive (mENT1) and inhibitor-resistant (mENT2) equilibrative nucleoside transporters from mouse brain. | 2000 Dec 1 |
|
| Endothelin-1 gene expression in endothelial cells is potently inhibited by a vasodilator, dilazep. | 2004 Jun |
|
| Nucleobase transport by human equilibrative nucleoside transporter 1 (hENT1). | 2011 Sep 16 |
|
| Screening of a chemical library reveals novel PXR-activating pharmacologic compounds. | 2015 Jan 5 |
Sample Use Guides
Dilazep dihydrochloride was administered orally at 300 mg/day for 24 months in 15 of these patients
Route of Administration:
Oral
The effect of dilazep or adenosine on the mechanical function was examined in both palmitoyl-L-camitine (PALCAR) treated heart (PALCAR-treated heart experiments) and normal (PALCAR-untreated) heart (normal heart experiments). Dilazep, adenosine or vehicle was infused into the aortic cannula for 45 mm at a constant flow rate of 0.1 ml/min. In the PALCAR-treated heart experiments, PALCAR was infused into the aortic cannula at the constant flow rate of 0.1 ml /min for 10 min from 10 min after the start of infusion of dilazep, adenosine or vehicle. The experimental condition and protocol of the normal heart experiments were essentially the same as in the PALCAR-treated heart experiments, except for an infusion of KHB buffer instead of PALCAR solution. In each group, LVSP, LVEDP and LVDP were recorded continuously before and during the infusion of dilazep, adenosine or vehicle.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 07:11:00 GMT 2023
by
admin
on
Sat Dec 16 07:11:00 GMT 2023
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| Record UNII |
6435U1X26I
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| Record Status |
Validated (UNII)
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| Record Version |
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ANHYDROUS->SOLVATE | |||
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |