Radiprodil

Research use only, not for human use.

Radiprodil (RGH-896) is an orally active and selective NMDA NR2B receptors antagonist. It was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP).

Radiprodil (RGH-896) is an orally active and selective NMDA NR2B receptors antagonist. It was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP).(In Vitro):Preincubation with Radiprodil (10 nM) restores long-term potentiation (LTP) in the presence of Aβ1-42, 3NTyr10-Aβ and Aβ1-40, but not AβpE3.As for LTP, Radiprodil (10 nM) reverses the synaptic toxicity of 3NTyr-AβAβ1-40 and Aβ1-42 but not that AβpE3-42.(In Vivo):Radiprodil could block NMDA currents in Mg2+ insensitive variants, with potencies similar to those obtained without Mg2+.Radiprodil's potency is higher at pH 7.0 than at pH 7.6, suggesting that radiprodil may retain its ability to block glutamate-induced NMDA currents even under acidic conditions that manifest under long term seizures.

Preincubation with Radiprodil (10 nM) restores long-term potentiation (LTP) in the presence of Aβ1-42, 3NTyr10-Aβ and Aβ1-40, but not AβpE3.As for LTP, Radiprodil (10 nM) reverses the synaptic toxicity of 3NTyr-AβAβ1-40 and Aβ1-42 but not that AβpE3-42.

Radiprodil could block NMDA currents in Mg2+ insensitive variants, with potencies similar to those obtained without Mg2+.Radiprodil's potency is higher at pH 7.0 than at pH 7.6, suggesting that radiprodil may retain its ability to block glutamate-induced NMDA currents even under acidic conditions that manifest under long term seizures.

RGH-896

Membrane Transporter/Ion Channel

NMDAR

NR2B-NMDA

Neurological Disease

Epilepsy; Infantile spasms; Neuropathic pain; Pain; Parkinson's disease

496054-87-6

397.41

C21H20FN3O4

>98% (HPLC)

DMSO: 220 mg/mL (553.6 mM)

Fc1ccc(CC2CCN(CC2)C(=O)C(=O)Nc2ccc3[nH]c(=O)oc3c2)cc1

——

(-20℃)

With Ice Pack

≥ 2 years