Barnidipine
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki = 0.21 nmol/L), has selective action against CaA receptors. Barnidipine is an orally effective antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance.
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- No. CAS: 104713-75-9
- Fòrmula: C27H29N3O6
- Peso molecular:491.54
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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L-type calcium channel |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LLC-PK1 | IC50 |
8.6 μM
Compound: Barnidipine
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TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells
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[PMID: 11145223] |
| LLC-PK1 | IC50 |
12.6 μM
Compound: Barnidipine
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TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
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[PMID: 12128170] |
Barnidipine hydrochloride (53 mg/kg; Feed administration; 3 weeks) reduces the level of platelet-derived growth factor B chain mRNA in spontaneously hypertensive rats, and has a effect on lowering blood pressure[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male SHR aged 13 weeks old[3]
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Dosage:Salt form dose: 0.6 mg/g of food (average dose: 53 mg/kg of body mass/day)
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Administration:Feed administration; 3 weeks
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Result:Reduced systolic blood pressure steadily after week 1 of therapy.
Did not change renal histology after week 3 of therapy.
Significantly reduced the level of expression of PDGF B-chain mRNA in glomeruli.
Significantly reduced the excretion of urinary protein.
Chemical Information
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No. CAS 104713-75-9
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Appearance Solid
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Peso molecular 491.54
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Fòrmula C27H29N3O6
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Color Off-white to light yellow
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SMILES
O=C(C1=C(C)NC(C)=C(C(O[C@@H]2CN(CC3=CC=CC=C3)CC2)=O)[C@H]1C4=CC=CC([N+]([O-])=O)=C4)OC
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Synonyms
Mepirodipine; YM-09730-5 Free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureza y Documentación
Referencias
[1]. van Zwieten PA, et al. Pharmacological profile of barnidipine: a single optical isomer dihydropyridine calcium antagonist. Blood Press Suppl. 1998;1:5-8 [Content Brief]
[2]. Malhotra HS, et al. Barnidipine. Drugs. 2001;61(7):989-96; discussion 997-8. [Content Brief]
[3]. Hashimoto M, et al. Treatment with a Ca(2+) channel blocker, barnidipine, reduces platelet-derived growth factor B-chain mRNA in glomeruli of spontaneously hypertensive rats. Am J Nephrol. 1999;19(5):615-21. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Barnidipine Related Classifications
HY-107322A Related Classifications
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