(R)-Verapamil (Dexverapamil) is an optically enantiomer of the oral-active Verapamil. (R)-Verapamil has a relatively low affinity for L-type calcium channels ( Ca v 1.2 ) ( IC50 > 300 μM), and its IC50 for sodium channels ( sodium channel ) is 3.19 μM. (R)-Verapamil exhibits SSTR2 agonistic activity, with an EC 50 of 1.3 μM. (R)-Verapamil significantly downregulates the expression of TXNIP protein in diabetic mouse models and significantly inhibits β-cell apoptosis ( apoptosis ), effectively controlling blood sugar. (R)-Verapamil can be used as a PET tracer for the function of P-glycoprotein (P-gp) [1] [2] [3].
References:
[1]. Chen YS, et al. Evaluating the antidiabetic effects of R-verapamil in type 1 and type 2 diabetes mellitus mouse models. PLoS One. 2021 Aug 6;16(8):e0255405.
[2]. Busse D, et al. Cardiovascular effects of (R)- and (S)-verapamil and racemic verapamil in humans: a placebo-controlled study. Eur J Clin Pharmacol. 2006 Aug;62(8):613-9.
[3]. Luurtsema G, et al. (R)- and (S)-[11C]verapamil as PET-tracers for measuring P-glycoprotein function: in vitro and in vivo evaluation. Nucl Med Biol. 2003 Oct;30(7):747-51.
References:
[1]. Chen YS, et al. Evaluating the antidiabetic effects of R-verapamil in type 1 and type 2 diabetes mellitus mouse models. PLoS One. 2021 Aug 6;16(8):e0255405.
[2]. Busse D, et al. Cardiovascular effects of (R)- and (S)-verapamil and racemic verapamil in humans: a placebo-controlled study. Eur J Clin Pharmacol. 2006 Aug;62(8):613-9.
[3]. Luurtsema G, et al. (R)- and (S)-[11C]verapamil as PET-tracers for measuring P-glycoprotein function: in vitro and in vivo evaluation. Nucl Med Biol. 2003 Oct;30(7):747-51.