(2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Ca v 3.2 T-type Ca channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice.
性状
Solid
IC50 & Target[1][2]
T-type calcium channel
体外研究(In Vitro)
(2R/S)-6-PNG (6-Prenylnaringenin) potently blocks Cav3.2, but exhibits minor effect on high-voltage-activated Ca channels and voltage-gated Na channels in differentiated NG108-15 cells. On the basis of IC50 values, the proportion (Cav3.2/HVA) of the inhibition potency of (2R/S)-6-PNG on Cav3.2 and HVA-currents is 5.20, and that (Cav3.2/Nav) on Cav3.2 and Nav-currents is 3.54. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
(2R/S)-6-PNG (6-Prenylnaringenin; 10-30 mg/kg; i.p.; single dose; 15 min before Na2S) significantly reduced the Na 2 S-induced nociceptive behavior and/or referred hyperalgesia in onscious mice with intracolonic (i.col.) administration of Na 2 S, an H 2 S 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
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
ClinicalTrial
参考文献
[1]. Fumiko Sekiguchi, et al. Blockade of T-type calcium channels by 6-prenylnaringenin, a hop component, alleviates neuropathic and visceral pain in mice. Neuropharmacology
溶解度数据
In Vitro: DMSO : 125 mg/mL (367.25 mM; Need ultrasonic)配制储备液