R모다피닐
|
|
R모다피닐 속성
- 녹는점
- 156-1580C
- 끓는 점
- 559.1±50.0 °C(Predicted)
- 밀도
- 1.283
- 저장 조건
- Controlled Substance, -20°C Freezer
- 용해도
- DMSO: ≥16mg/mL
- 산도 계수 (pKa)
- 14.88±0.40(Predicted)
- 물리적 상태
- 가루
- 색상
- 흰색에서 황갈색까지
- optical activity
- [α]/D -15 to -20° in methanol (C=1)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
R모다피닐 C화학적 특성, 용도, 생산
개요
Armodafinil, an α1-adrenoceptor agonist, was launched for the oral treatment of excessive sleepiness associated with narcolepsy, SWSD, and obstructive sleep apnea/hypopnea syndrome (OSA). It is the R-enantiomer of modafinil, which is a previously marketed wake-promoting agent. The key differentiator for armodafinil is its longer pharmacokinetic half-life as compared with the S-enantiomer (10-14 hvs.3-4h). At therapeutic concentrations, armodafinil does not bind to most of the potentially relevant receptors for sleep/wake regulation (e.g., serotonin, dopamine, and adenosine receptors) or transporters of neurotransmitters or enzymes involved in sleep/wake regulation (e.g., serotonin, norepinephrine, and phosphodiesterase VI transporters). Both armodafinil and modafinil block dopamine reuptake by binding to the dopamine transporter and increasing dopamine concentrations in certain regions of the brain. However, dopamine receptor antagonists (e.g., haloperidol) and dopamine synthesis inhibitors (e.g., α-methyl-p-tyrosine) do not block modafinil’s action.In addition to its wake-promoting effects and ability to increase locomotor activity in animals, modafinil produces psychoactive and euphoric effects, alterations in mood, perception, thinking, and feelings typical of other CNS stimulants in humans. Modafinil was also partially discriminated as stimulant-like. However, the potential for abuse and dependency appears to be lower for modafinil than amphetamine-like stimulants.The most common adverse events associated with armodafinil included headache, nausea, dizziness, and insomnia.