Threo-methylphenidate hydrochloride (Synonyms: DL-threo-Methylphenidate, NSC 169868) |
| Catalog No.GC17047 |
Threo-methylphenidate hydrochloride is an inhibitor of dopamine and norepinephrine transporters..
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Cas No.: 298-59-9
Sample solution is provided at 25 µL, 10mM.
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Threo-methylphenidate hydrochloride is a catecholamine reuptake inhibitor that inhibits dopamine transporter (DAT) and norepinephrine transporter (NET)[1]. Threo-methylphenidate hydrochloride is used to treat attention deficit hyperactivity disorder (ADHD)[2]. Threo-methylphenidate hydrochloride has central nervous system excitability and sympathomimetic effects, and can also affect the cardiovascular system[3].
In vitro, when glial cells were treated with Threo-methylphenidate hydrochloride (100µM, 30 min), a significant increase in [3H]-D-Asp was detected after 2 hours, and this effect persisted after 12hours[4]. The concentration range of Threo-methylphenidate hydrochloride that inhibits NET in HEK293 cells is 0.04-0.42µM, and the concentration range that inhibits DAT is 0.08-0.34µM[5].
In vivo, Threo-methylphenidate hydrochloride(30mg/kg) caused a shortening of the QT interval in the electrocardiogram of beagle dogs and an increase in blood pressure[3]. Threo-methylphenidate hydrochloride(10mg/kg, o.p.) may reduce urine flow and glomerular filtration rate in Wistar rats, but has no harmful effect on renal tubules[6].Threo-methylphenidate hydrochloride(4 mg/kg) increased the anticipatory response of zebrafish in a 5-choice series response task and also increased the overall activity level of the experimental group [7].
References:
Markowitz J S , Patrick K S. Differential Pharmacokinetics and Pharmacodynamics of Methylphenidate Enantiomers[J]. Journal of Clinical Psychopharmacology, 2008, 28: 54-61.
[2]Heal D J , Pierce D M .Methylphenidate and its Isomers: Their Role in the Treatment of Attention-Deficit Hyperactivity Disorder Using a Transdermal Delivery System[J].Cns Drugs, 2006, 20(9):713-738.
[3]Wakamatsu A , Nomura S , Tate Y ,et al. Effects of methylphenidate hydrochloride on the cardiovascular system in vivo and in vitro: A safety pharmacology study[J].Journal of Pharmacological & Toxicological Methods, 2009, 59(3):128-134.
[4]A M. Guillem, Z Martı´nez-Lozada, L C. Herna´ndez-Kell, et al. Methylphenidate Increases Glutamate Uptake in Bergmann Glial Cells[J]. Neurochem Res. 2015(40):2317-2324.
[5]Luethi, D.K., Philine J.Brandt, Simon D. K, et al. Pharmacological profile of methylphenidate-based designer drugs[J].Neuropharmacology, 2018, 134.
[6]Luiza Herbene Macedo Soares Salviano,et al. Study of the safety of methylphenidate: Focus on nephrotoxicity aspects[J].Life Sciences. 2015:137-142.
[7]Parker M O , Brock A J , Sudwarts A ,et al.Atomoxetine reduces anticipatory responding in a 5-choice serial reaction time task for adult zebrafish[J].Psychopharmacology, 2014, 231(13):2671.
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