Bioactivity | Lisdexamfetamine dimesylate is an orally active and long-acting prodrug of dexamfetamine bound to lysine. Lisdexamfetamine dimesylate is enzymatically hydrolysed in the blood to the active dexamfetamine. Lisdexamfetamine dimesylate can inhibit PEPT1 and PEPT2 uptake. Lisdexamfetamine dimesylate can be used for the research of attention-deficit hyperactivity disorder (ADHD)[1][2]. |
Target | PEPT1, PEPT2 |
Invitro | LDX (10-10000 μM) inhibits uptake of Gly-Sar by CHO cells stably expressing either human PEPT1 or PEPT2 (dipeptide transporters) in a concentration-dependent manner, and exhibits uptake inhibition with IC50s of 4 mM and 246 μM for PEPT1 and PEPT2, respectively[1]. |
In Vivo | Lisdexamfetamine dimesylate is metabolized in rat whole blood and liver tissue, and rapidly decreases over time with concomitant formation of d-amphetamine[1].Lisdexamfetamine dimesylate is rapidly absorbed from the gastrointestinal (GI) tract after administration; plasma concentrations in both portal and systemic circulation peaked by 10 minutes postdose[1].Pharmacokinetic Parameters of Lisdexamfetamine dimesylate in male Sprague-Dawley rats[1]. |
Name | Lisdexamfetamine dimesylate |
CAS | 608137-33-3 |
Formula | C17H33N3O7S2 |
Molar Mass | 455.59 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Pennick M. Absorption of lisdexamfetamine dimesylate and its enzymatic conversion to d-amphetamine. Neuropsychiatr Dis Treat. 2010 Jun 24;6:317-27. [2]. Steer C, et al. Lisdexamfetamine dimesylate: a new therapeutic option for attention-deficit hyperactivity disorder. CNS Drugs. 2012 Aug 1;26(8):691-705. |