Mirogabalin Struktur

Mirogabalin

Bezeichnung:Mirogabalin

CAS-Nr1138245-13-2

Englisch Name:Mirogabalin

CBNumberCB23051612

SummenformelC12H19NO2

Molgewicht209.28

MOL-Datei1138245-13-2.mol

Mirogabalin physikalisch-chemischer Eigenschaften

Siedepunkt	357.5±15.0 °C(Predicted)
Dichte	1.104±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	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)
Aggregatzustand	A crystalline solid
pka	4.65±0.10(Predicted)
Farbe	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
InChIKey	FTBQORVNHOIASH-CKYFFXLPSA-N
SMILES	[C@]12([H])[C@]([H])([C@@](CN)(CC(O)=O)C1)C=C(CC)C2

Gefahreninformationscode (GHS)

Mirogabalin Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Verwenden
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.
Trademarks
Mirogabalin (brand name Tarlige; developmental code name DS-5565) is a gabapentinoid medication developed by Daiichi Sankyo.
Nebenwirkungen
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.
Einzelnachweise
[1] Hui Tang. “The Clinical Application and Progress of Mirogabalin on Neuropathic Pain as a Novel Selective Gabapentinoids.” Mediators of Inflammation 2023 (2023): 4893436.

Mirogabalin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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