Focalin

HCID 154100CAS 19262-68-1

기본 정보

표준 SMILES
COC(=O)[C@H](c1ccccc1)[C@H]1CCCCN1.Cl
InChIKey
JUMYIBMBTDDLNG-OJERSXHUSA-N
분자식
C14H20ClNO2
평균 분자량
269.77 g/mol
단동위원소 질량
269.11825656

개요

Dexmethylphenidate Hydrochloride is a synthetic sympathomimetic amine with CNS stimulating properties. Dexmethylphenidate hydrochloride acts by facilitating the release of catecholamines, particularly noradrenaline and dopamine, from nerve terminals in the brain and inhibits their uptake. This leads to an increase in motor activity, causes euphoria, mental alertness and excitement and suppresses appetite. This drug causes dependence and may cause an increase in heart rate and blood pressure. It is used in the treatment of attention deficit hyperactivity disorder. It may also be used in the treatment of fatigue and other nervous system effects seen with chemotherapy.

이름 및 식별자

우선 이름
Focalin
IUPAC
methyl (2R)-2-phenyl-2-[(2R)-piperidin-2-yl]acetate;hydrochloride

이름 및 동의어

Dexmethylphenidate hydrochlorideFocalinD-threo-Methylphenidate hydrochloride19262-68-1dex-methylphenidate hydrochloride1678OK0E08Methylphenidate d-threo-form hydrochloride2-Piperidineacetic acid, alpha-phenyl-, methyl ester, hydrochloride, (alphaR,2R)-AZSTARYS COMPONENT DEXMETHYLPHENIDATE HYDROCHLORIDEFocalinxrXR, FocalinRefChem:56470
이름 더 보기
Hydrochloride, DexmethylphenidateDexmethylphenidate Hydrochloride Extended-releaseDexmethylphenidate HCl23655-65-4Focalin XRDexmethylphenidate hydrochloride [USAN]methyl (2R)-2-phenyl-2-[(2R)-piperidin-2-yl]acetate;hydrochloriderac-threo-Methylphenidate Hydrochloride

데이터베이스 식별자

CAS
19262-68-1、23655-65-4
PubChem CID
154100
DTXSID
DTXSID50940927
ChEMBL
CHEMBL904
UNII
1678OK0E08、4B3SC438HI
EC Number
111-173-8

물성

구조 계산 물성

극성 표면적
38.3 Ų
수소 결합 공여자 수
2
수소 결합 수용자 수
3
회전 가능 결합 수
4
무거운 원자 수
18

실험 및 물리화학적 성질

Human Drugs · 3건

Breast Feeding; Lactation; Milk, Human; Adrenergic Agents; Central Nervous System Stimulants; Dopamine Agents; Sympathomimetics; Wakefulness-Promoting Agents

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

안전 및 규제

GHS 분류

GHS Classification · 4건

Warning

H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]

P264, P270, P301+P317, P330, and P501 (click each P-code to see the statement)

The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

유해성 정보

Hazard Classes and CategoriesAcute Tox. 4 (100%)

독성 정보

Exposure Routes11-52%
Toxicity Summary · 1건

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.

Signs and Symptoms · 1건

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.

Carcinogen ClassificationNo indication of carcinogenicity to humans (not listed by IARC).
Drug Induced Liver Injury · 6건

Drug Induced Liver Injury Rank (DILIrank 2.0)

Dexmethylphenidate hydrochloride

vLess-DILI-concern

7

Adverse reactions

DOI:10.1016/j.drudis.2016.02.015

Effects During Pregnancy and Lactation◉ Summary of Use during Lactation

화학 및 산업

약리 정보

Metabolism/Metabolitesepatic, 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
FDA Pharmacological Classification · 2건

DEXMETHYLPHENIDATE HYDROCHLORIDE

Central Nervous System Stimulation [PE]; Central Nervous System Stimulant [EPC]

MeSH Pharmacological Classification · 2건

A loosely defined group of drugs that tend to increase behavioral alertness, agitation, or excitation. They work by a variety of mechanisms, but usually not by direct excitation of neurons. The many drugs that have such actions as side effects to their main therapeutic use are not included here.

Drugs that block the transport of DOPAMINE into axon terminals or into storage vesicles within terminals. Most of the ADRENERGIC UPTAKE INHIBITORS also inhibit dopamine uptake.

용도 및 제조

UsesDexmethylphenidate is used as a treatment for ADHD, ideally in conjunction with psychological, educational, behavioral or other forms of treatment.

관련 반응

2건

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