(R)-Duloxetine
(R)-Duloxetine ((R)-LY248686) is a neuronal voltage-gated sodium channel blocker with analgesic activity. (R)-Duloxetine blocks Na+ currents with higher affinity for the inactivated state than for the resting state. (R)-Duloxetine alleviates postoperative mechanical allodynia and hyperalgesia. (R)-Duloxetine exerts its effects through a local peripheral mechanism of action. (R)-Duloxetine can be used for research on postoperative (post-incisional) pain.
For research use only. We do not sell to patients.
- CAS No.: 116539-60-7
- Formula: C18H19NOS
- Molecular Weight:297.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| GH3 | IC50 |
33.78 μM
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Resting-state block of voltage-gated Na+ currents in rat pituitary GH3 cells measured by whole-cell patch-clamp assay with Na+ currents evoked by a test pulse to +50 mV from a holding potential of −140 mV.
Resting-state block of voltage-gated Na+ currents in rat pituitary GH3 cells measured by whole-cell patch-clamp assay with Na+ currents evoked by a test pulse to +50 mV from a holding potential of −140 mV.
|
26646348 |
| GH3 | IC50 |
5.82 μM
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Inactivated-state block of voltage-gated Na+ currents in rat pituitary GH3 cells measured by whole-cell patch-clamp assay with a 10-second conditioning pulse to −70 mV applied prior to the test pulse to promote channel inactivation.
Inactivated-state block of voltage-gated Na+ currents in rat pituitary GH3 cells measured by whole-cell patch-clamp assay with a 10-second conditioning pulse to −70 mV applied prior to the test pulse to promote channel inactivation.
|
26646348 |
In Vitro
(R)-duloxetine (10 μM; 15-20 min) blocks voltage-gated Na+ channels in a state-dependent manner in rat GH3 cells, with approximately 5.8-fold higher potency for inactivated channels (IC50 5.82 μM) than for resting channels (IC50 33.8 μM), and produces significant use-dependent block (75% block after 60 pulses at 5 Hz)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male; weight 250-300 g; skin incision plus extension model on dorsothoracic skin)[1]
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Dosage:2 mg (ipsilateral s.c.); 10 mg (i.p.); 10 mg (contralateral s.c.)
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Administration:s.c. (ipsilateral to incision; single injection; 1 hour prior to surgery); i.p. (single injection; 1 hour prior to surgery); s.c. (contralateral to incision; single injection; 1 hour prior to surgery)
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Result:Reduced 4 g von Frey allodynia 5-day AUC to 11% of control at 0.5 cm, 27% of control at 1.0 cm, 41% of control at 2.0 cm, and 46% of control at the contralateral site following 2 mg ipsilateral subcutaneous administration.
Reduced 15 g von Frey hyperalgesia 5-day AUC to 1% of control at 0.5 cm, 11% of control at 1.0 cm, and 65% of control at the contralateral site following 2 mg ipsilateral subcutaneous administration.
Produced analgesic effects on allodynia from time 0 through 5 days at all ipsilateral sites, with contralateral allodynia relief lasting 1 day post-injection after 2 mg ipsilateral subcutaneous administration.
Produced antihyperalgesic effects persisting for 5 days at ipsilateral sites, with responses below baseline at 0.5-1 cm from day 0 to day 3 after 2 mg ipsilateral subcutaneous administration.
Reduced 4 g allodynia 5-day AUC to 31% of control at 0.5 cm, 37% of control at 1.0 cm, 54% of control at 2.0 cm, and 72% of control at the contralateral site following 10 mg intraperitoneal administration.
Reduced 15 g hyperalgesia 5-day AUC to 35% of control at 0.5 cm, 40% of control at 1.0 cm, 48% of control at 2.0 cm, and 52% of control at the contralateral site following 10 mg intraperitoneal administration.
Produced immediate systemic allodynia reduction post-injection following 10 mg intraperitoneal administration.
Produced minimal analgesic effects on allodynia and hyperalgesia at the ipsilateral incision side, with 4 g allodynia AUC values at 89%-105% of control and 15 g hyperalgesia AUC values at 84%-92% of control across 0.5-2.0 cm ipsilateral sites following 10 mg contralateral subcutaneous administration.
Chemical Information
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CAS No. 116539-60-7
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Molecular Weight 297.41
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Formula C18H19NOS
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SMILES
CNCC[C@@H](OC1=CC=CC2=C1C=CC=C2)C3=CC=CS3
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Synonyms
(R)-LY248686
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- (R)-Duloxetine
- 116539-60-7
- (R)-LY248686
- Sodium Channel
- local peripheral mechanism of action
- analgesic activity
- rat GH3 cells
- Na+ currents
- neuronal voltage-gated sodium channel blocker
- voltage-gated Na+ channels
- rat postoperative pain model
- postoperative mechanical allodynia
- postincisional pain
- hyperalgesia
- Inhibitor
- inhibitor
- inhibit