Safinamide mesylate

한글명:Safinamide mesylate

카스 번호202825-46-5

상품명:Safinamide mesylate

CBNumberCB92510036

분자식C17H19FN2O2.CH4O3S

포뮬러 무게398.4490232

MOL 파일202825-46-5.mol

화학적 성질

녹는점	210° (dec)
알파	D25 +12.9° (c = 1.1% in 98% acetic acid)
저장 조건	2-8°C
용해도	H2O: ≥15mg/mL
물리적 상태	가루
색상	흰색에서 황갈색까지
optical activity	[α]/D +9.5 to +14°, c = 1 (95% acetic acid)
InChI	InChI=1/C17H19FN2O2.CH4O3S/c1-12(17(19)21)20-10-13-5-7-16(8-6-13)22-11-14-3-2-4-15(18)9-14;1-5(2,3)4/h2-9,12,20H,10-11H2,1H3,(H2,19,21);1H3,(H,2,3,4)/t12-;/s3
InChIKey	YKOCHIUQOBQIAC-ZLBVLXFENA-N
SMILES	CS(O)(=O)=O.C(N)(=O)[C@@H](NCC1=CC=C(OCC2=CC=CC(F)=C2)C=C1)C \|&1:8,r\|

위험 및 안전 성명

유엔번호(UN No.)

UN 2811 6.1 / PGIII

WGK 독일

NFPA 704:

	0
3		0

그림문자(GHS)

Safinamide mesylate 화학적 특성, 용도, 생산

개요
Safinamide methanesulfonate was approved in February 2015 by the EMA for the treatment of mid- to late-stage fluctuating Parkinson’s disease. This approval included use of the drug as an add-on therapy for use with levodopa, either alone or in combination with other existing therapies for Parkinson’s disease.51 Safinamide methanesulfonate, an oral α-aminoamide originally discovered by Farmitalia Carlo Erba and later developed by Newron/Zambon, functions as a highly selective and reversible inhibitor of MAO-B, leading to increased levels of dopamine and subsequent improvement in the motor symptoms of Parkinson’s disease, side effects that often result from use of other traditional treatments relying on dopamine replacement therapy.
화학적 성질
Safinamide mesylate is a white to off-white crystalline powder. Safinamide mesylate is freely soluble in water, methanol and dimethyl sulfoxide. Safinamide mesylate is sparingly soluble in ethanol and is practically insoluble in ethyl acetate. In aqueous buffers that span a pH range of 1.2 to 7.5, safinamide mesylate is highly soluble at pH 1.2 and 4.5 but shows low solubility (<0.4 mg/mL) at pH 6.8 and 7.5.
용도
Safinamide mesylate salt has been used as a reference drug to study its inhibitory effect on human monoamine oxidases (hMAO-A and hMAO-B).
Mechanism of action
Safinamide employs several mechanisms of action, functioning as both a dopaminergic agent through inhibition of MAO-B as well as a nondopaminergic agent via selective calcium and sodium channel modulation, leading to inhibition of glutamate release. At least one of several clinical studies of patients with mid- to late-stage Parkinson’s disease showed increased daily ON time (periods of symptom control) without accompanying motor complications (dyskinesias) upon treatment with safinamide, while studies of early stage Parkinson’s disease patients treated with this drug showed significantly improved motor symptoms during the 18-month study. Additionally, safinamide is chemically and metabolically stable, is well tolerated in patients, and has not exhibited serious adverse effects even upon treatment at higher dosage ranges.
부작용
Common adverse events in clinical trials (in more than 1% of people) included nausea, dizziness, tiredness, sleeplessness, or thostatic hypotension (low blood pressure) and headache. There was no significant difference in the occurrence of these effects between safinamide and placebo.

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