Mirogabalin besylate（DS 5565 besylate）

Mirogabalin besylate(美洛加巴林) 是一种选择性的，可口服的电压门控性钙通道 (voltage-gated calcium channels) 亚基 α2δ 的有效配体，对人 α2δ-1 和 α2δ-2，大鼠 α2δ-1 和 α2δ-2 的 Kd 值分别为 13.5 nM，22.7 nM，27 nM 和 47.6 nM。

Mirogabalin besylate is a selective, orally active, and potent ligand for the α2δ subunit of voltage-gated calcium channels, with Kd values of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1 and α2δ-2, and rat α2δ-1 and α2δ-2, respectively.

Category: Diabetes; Aromatic

Purity/Specification: 99% / Kilogram scale （Mirogabalin besylate -Synonyms: DS 5565 besylate）

CAS: 1138245-21-2

Molecular Formula: C18H25NO5S

Molecular Weight: 367.46

Density: 1.53 ± 0.1 g/cm³ (Predicted)

Acidity constant (pKa): 2.56 ± 0.40 (Predicted)

Form: Solid

Color: White to off-white

Synonyms：Mirogabalinbesylate;MIROGABALINBENZENESULFONICACID;[(1R,5S,6S)-6-(Aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]aceticacidbenzenesulfonate;2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetiChemicalbookcacidcompoundwithbenzenesulfonicacid(1:1);MirogabalinBesylate10928;Mirogabalinbesylate(DS5565besylate);2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)aceticacidbesylate;LinagliptinImpurityCD10126

Indication

Mirogabalin besylate is a novel analgesic belonging to the gabapentinoid class of drugs; developed by Daiichi Sankyo, it was initially approved in Japan for the treatment of peripheral neuropathic pain (including diabetic peripheral neuropathy and postherpetic neuralgia).

米洛巴林苯磺酸盐是一种属于加巴喷丁类药物类别的新型止痛药，由 Daiichi Sankyo 开发，最初在日本获批用于治疗周围神经病疼痛（包括糖尿病性周围神经病和带状疱疹后神经痛）。

Mechanism of Action

Mirogabalin besylate exerts its analgesic effect by inhibiting calcium-mediated neurotransmitter release via voltage-gated calcium channels (VGCCs), specifically through binding to the α2δ-1 subunit. It exhibits high affinity for both α2δ-1 and α2δ-2 subunits; these subunits are associated with analgesic efficacy (α2δ-1) and central nervous system side effects (α2δ-2), respectively.

米洛巴林苯磺酸盐通过抑制电压门控钙通道（VGCCs）内的钙介导的神经递质释放来发挥镇痛作用，特别是通过与α2δ-1亚单Chemicalbook位结合。它对α2δ-1和α2δ-2亚单位具有高亲和力，这些亚单位与镇痛效果（α2δ-1）和中枢神经系统副作用（α2δ-2）相关。

Characteristics

A notable feature of mirogabalin besylate is its long dissociation half-life (exceeding 11 hours at the α2δ-1 subunit), which is significantly longer than that of pregabalin (approximately 1.5 hours at α2δ-1 and α2δ-2). This characteristic is believed to contribute to its potent and sustained analgesic effect while reducing side effects associated with gabapentinoids.

米洛巴林苯磺酸盐的一个显著特点是它具有较长的解离半衰期（在α2δ-1上超过11小时），这比pregabalin的半衰期（在αChemicalbook2δ-1和α2δ-2上约为1.5小时）长得多，这一特性被认为有助于其强效且持久的镇痛效果，同时减少与加巴喷丁类药物相关的副作用。

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