Mirogabalin
- CAS NO.:1138245-13-2
- Empirical Formula: C12H19NO2
- Molecular Weight: 209.28
- MDL number: MFCD28411425
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-08 21:13:59
What is Mirogabalin?
Description
Mirogabalin is a calcium channel blocker with analgesic effects. It binds to the α2δ-1 and α2δ-2 subunits of voltage-dependent Ca2+ channels. Mirogabalin has potent and sustained analgesic effects (ED50 = 2.5 mg/kg) in rats with diabetes induced by streptozotocin (STZ; ). Mirogabalin does not inhibit activities associated with CNS adverse effects of analgesics, such as rotarod performance (ID50 = 9.4 mg/kg) or locomotor activity (ID50 = 43.9 mg/kg), at its effective dose. Formulations containing mirogabalin are in clinical trials for diabetic peripheral neuropathic pain.
The Uses of Mirogabalin
Mirogabalin is a two alpha2delta ligand which is investigated for the treatment of peripheral neuropathic pain, postherpetic neuralgia and fibromyalgia, showing promising results in patients with diabetic peripheral neuropathy.
brand name
Mirogabalin (brand name Tarlige; developmental code name DS-5565) is a gabapentinoid medication developed by Daiichi Sankyo.
Side Effects
The most typical clinical adverse reactions of mirogabalin were dizziness (7.6%) and somnolence (5.1%). However, the occurrence rate was lower than with pregabalin, whose adverse effects were reported to include somnolence, balance disorder, fatigue, and peripheral edema, with an occurrence rate of 8.0%, 4.0%, 4.0%, and 4.0%, respectively[1].
Mode of action
Mirogabalin is an analog of the neurotransmitter, gamma-aminobutyric acid (GABA). It is a potent and specific ligand of the α2δ subunit of voltage-dependent Ca2+channels, which reduces calcium (Ca2+) influx and neurotransmission in dorsal root ganglia (DRGs), inhibiting neurotransmitter release in presynaptic neuron endings.
References
[1] Hui Tang. “The Clinical Application and Progress of Mirogabalin on Neuropathic Pain as a Novel Selective Gabapentinoids.” Mediators of Inflammation 2023 (2023): 4893436.
Properties of Mirogabalin
Boiling point: | 357.5±15.0 °C(Predicted) |
Density | 1.104±0.06 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | DMF:0.5(Max Conc. mg/mL);2.39(Max Conc. mM) Ethanol:1.25(Max Conc. mg/mL);5.97(Max Conc. mM) PBS (pH 7.2):0.5(Max Conc. mg/mL);2.39(Max Conc. mM) Water:5.36(Max Conc. mg/mL);25.61(Max Conc. mM) |
form | A crystalline solid |
pka | 4.65±0.10(Predicted) |
color | Light yellow to light brown |
InChI | InChI=1S/C12H19NO2/c1-2-8-3-9-5-12(7-13,6-11(14)15)10(9)4-8/h4,9-10H,2-3,5-7,13H2,1H3,(H,14,15)/t9-,10-,12-/m1/s1 |
Safety information for Mirogabalin
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Mirogabalin
InChIKey | FTBQORVNHOIASH-CKYFFXLPSA-N |
SMILES | [C@]12([H])[C@]([H])([C@@](CN)(CC(O)=O)C1)C=C(CC)C2 |
Abamectin manufacturer
Integrin Life Sciences. Pvt. Ltd.
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