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(2R/S)-6-PNG

CAS No. : 68682-01-9

MCE 站：(2R/S)-6-PNG

产品活性：(2R/S)-6-PNG (6-Prenylnaringenin) 是一种有效且可逆的 Ca_v3.2 T 型 Ca²⁺ 通道 (T 通道)阻滞剂。(2R/S)-6-PNG 可以透过血脑屏障 (BBB)。(2R/S)-6-PNG 抑制小鼠的神经性和内脏疼痛。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：Calcium Channel

In Vitro: (2R/S)-6-PNG (6-Prenylnaringenin) potently blocks Ca_v3.2, but exhibits minor effect on high-voltage-activated Ca²⁺ channels and voltage-gated Na⁺ channels in differentiated NG108-15 cells.
On the basis of IC50 values, the proportion (Ca_v3.2/HVA) of the inhibition potency of (2R/S)-6-PNG on Ca_v3.2 and HVA-currents is 5.20, and that (Ca_v3.2/Na_v) on Ca_v3.2 and Na_v-currents is 3.54.

In Vivo: (2R/S)-6-PNG (6-Prenylnaringenin; 10-30 mg/kg; i.p.; single dose; 15 min before Na2S) significantly reduced the Na₂S-induced nociceptive behavior and/or referred hyperalgesia in onscious mice with intracolonic (i.col.) administration of Na₂S, an H₂S donor.
(2R/S)-6-PNG (30 mg/kg; i.p.) prevents the increased number of phosphorylated ERK-positive cells following i.col. Na2S in laminae I-II, V-VI and X to which the primary afferent neurons project, and the Na2S-induced increase in the phosphorylated ERK-positive cell number.
(2R/S)-6-PNG (0.01-1 and 0.1-10 nmol/paw; intraplantar administration) restores the mechanical allodynia induced by partial sciatic nerve ligation (PSNL) and by i.p. administration of Oxaliplatin (OHP) a, respectively, in a dose-dependent manner.
(2R/S)-6-PNG (20-30 mg/kg; i.p.) significantly reverses the PSNL-induced allodynia. (2R/S)-6-PNG (10-20 mg/kg; i.p.) significantly reverses the OHP-induced allodynia (5 mg/kg; i.p.; single dose).

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