Tìm theo
Dexmethylphenidate
Các tên gọi khác (5 ) :
  • Attenade
  • d-threo-methylphenidate
  • D-TMP
  • Dexmethylphenidate
  • Focalin
Thuốc Gốc
Small Molecule
CAS: 40431-64-9
ATC: N06BA11
CTHH: C14H19NO2
PTK: 233.3062
Dexmethylphenidate is the dextrorotary form of methylphenidate. It is a norepinephrine-dopamine reuptake inhibitor (NDRI) and thus a psychostimulant. It is used for treatment of Attention Deficit Hyperactivity Disorder (ADHD).
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H19NO2
Phân tử khối
233.3062
Monoisotopic mass
233.141578857
InChI
InChI=1S/C14H19NO2/c1-17-14(16)13(11-7-3-2-4-8-11)12-9-5-6-10-15-12/h2-4,7-8,12-13,15H,5-6,9-10H2,1H3/t12-,13-/m1/s1
InChI Key
InChIKey=DUGOZIWVEXMGBE-CHWSQXEVSA-N
IUPAC Name
methyl (2R)-2-phenyl-2-[(2R)-piperidin-2-yl]acetate
Traditional IUPAC Name
methylphenidate
SMILES
COC(=O)[C@@H]([C@H]1CCCCN1)C1=CC=CC=C1
Độ hòa tan
1.82e-01 g/l
logP
2.25
logS
-3.1
pKa (Strongest Basic)
9.09
PSA
38.33 Å2
Refractivity
66.73 m3·mol-1
Polarizability
26.23 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Methylphenidate is a central nervous system stimulant used most commonly in the treatment of attention-deficit disorders in children and for narcolepsy.
Cơ Chế Tác Dụng : Dexmethylphenidate is the dextrorotary form of methylphenidate. It is a norepinephrine-dopamine reuptake inhibitor (NDRI) and thus a psychostimulant. It is used for treatment of Attention Deficit Hyperactivity Disorder (ADHD). Methylphenidate blocks dopamine uptake in central adrenergic neurons by blocking dopamine transport or carrier proteins. Methylphenidate acts at the brain stem arousal system and the cerebral cortex and causes increased sympathomimetic activity in the central nervous system. Methylphenidate is a catecholamine reuptake inhibitor that indirectly increases catecholaminergic neurotransmission by inhibiting the dopamine transporter (DAT) and norepinephrine transporter (NET), which are responsible for clearing catecholamines from the synapse, particularly in the striatum and meso-limbic system.
Dược Động Học :
▧ Absorption :
11-52%
▧ Protein binding :
30%
▧ Metabolism :
epatic, methylphenidate is metabolized primarily by de-esterification to ritalinic acid (α-phenyl-2-piperidine acetic acid, PPAA), which has little to no pharmacologic activity.
▧ Route of Elimination :
Renal
▧ Half Life :
2-4 hours
Độc Tính : Insomnia, dizziness, nausea, stomach pain, euphoria, headache, anxiety, anorexia, and weight loss are common side effects. Symptoms of overdose include vomiting, agitation, tremors, hyperreflexia, muscle twitching, convulsions (may be followed by coma), euphoria, confusion, hallucinations, delirium, sweating, flushing, headache, hyperpyrexia, tachycardia, palpitations, cardiac arrhythmias, hypertension, mydriasis, and dryness of mucous membranes. LD50=190mg/kg (orally in mice)
Chỉ Định : Dexmethylphenidate is used as a treatment for ADHD, ideally in conjunction with psychological, educational, behavioral or other forms of treatment.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Celgene
    Sản phẩm biệt dược : Attenade
  • Công ty : Novartis
    Sản phẩm biệt dược : Focalin
  • Công ty :
    Sản phẩm biệt dược : FocalinXR
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