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바클로펜

바클로펜
바클로펜 구조식 이미지
카스 번호:
1134-47-0
한글명:
바클로펜
동의어(한글):
바클로펜
상품명:
Baclofen
동의어(영문):
ofen;Clofen;Spinax;baclon;Lioresa;ba34647;Atrofen;c34647ba;BACLOFEN;LIORESAL
CBNumber:
CB8669450
분자식:
C10H12ClNO2
포뮬러 무게:
213.66
MOL 파일:
1134-47-0.mol

바클로펜 속성

녹는점
208-210°C
끓는 점
364.3±32.0 °C(Predicted)
밀도
1.2069 (rough estimate)
굴절률
1.5500 (estimate)
저장 조건
2-8°C
용해도
1 M HCl: 50 mg/mL
물리적 상태
solid
산도 계수 (pKa)
pKa 3.87±0.1(H2O) (Uncertain)
색상
white to very faintly yellow
수용성
Soluble in dilute NaOH or dilute HCl. Soluble in water at approximately 4mg/ml at pH 7.6
Merck
14,937
CAS 데이터베이스
1134-47-0(CAS DataBase Reference)
NIST
Baclofen(1134-47-0)
EPA
.beta.-(Aminomethyl)-4-chlorobenzenepropanoic acid (1134-47-0)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 T,Xn
위험 카페고리 넘버 61-25-36/37/38-42/43-20/21/22
안전지침서 53-22-36/37/39-45-52-36-26
유엔번호(UN No.) UN 2811 6.1/PG 3
WGK 독일 3
RTECS 번호 MW5084200
위험 등급 6.1(b)
포장분류 III
HS 번호 2922492050
독성 LD50 in male mice, rats (mg/kg): 45, 78 i.v.; 103, 115 s.c.; 200, 145 orally (Tadokoro)
기존화학 물질 KE-01454
그림문자(GHS):
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H301 삼키면 유독함 급성 독성 물질 - 경구 구분 3 위험 P264, P270, P301+P310, P321, P330,P405, P501
H315 피부에 자극을 일으킴 피부부식성 또는 자극성물질 구분 2 경고 P264, P280, P302+P352, P321,P332+P313, P362
H317 알레르기성 피부 반응을 일으킬 수 있음 피부 과민성 물질 구분 1 경고 P261, P272, P280, P302+P352,P333+P313, P321, P363, P501
H319 눈에 심한 자극을 일으킴 심한 눈 손상 또는 자극성 물질 구분 2A 경고 P264, P280, P305+P351+P338,P337+P313P
H334 흡입 시 알레르기성 반응, 천식 또는 호흡 곤란 등을 일으킬 수 있음 호흡기 과민성 물질 구분 1 위험 P261, P285, P304+P341, P342+P311,P501
H335 호흡 자극성을 일으킬 수 있음 특정 표적장기 독성 - 1회 노출;호흡기계 자극 구분 3 경고
H360 태아 또는 생식능력에 손상을 일으킬 수 있음 생식독성 물질 구분 1A, 1B 위험
예방조치문구:
P201 사용 전 취급 설명서를 확보하시오.
P261 분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P270 이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P272 작업장 밖으로 오염된 의복을 반출하지 마시오.
P280 보호장갑/보호의/보안경/안면보호구를 착용하시오.
P284 호흡 보호구를 착용하시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
P405 밀봉하여 저장하시오.
P501 ...에 내용물 / 용기를 폐기 하시오.

바클로펜 MSDS


Baclofen

바클로펜 C화학적 특성, 용도, 생산

화학적 성질

Off-White Solid

Originator

Lioresal,Ciba Geigy,Switz.,1971

용도

Specific GABA-B receptor agonist. Muscle relaxant (skeletal)

정의

ChEBI: A monocarboxylic acid that is butanoic acid substituted by an amino group at position 4 and a 4-chlorophenyl group at position 3. It acts as a central nervous system depressant, GABA agonist and muscle relaxant.

Manufacturing Process

42.45 g of β-(p-chlorophenyl)glutaric acid imide are stirred into a solution of 8.32 g of sodium hydroxide in 200 ml of water. The mixture is heated for 10 minutes at 50°C, and the solution thus formed is cooled to 10° to 15°C. At this temperature there are then added dropwise a solution of 40.9 g of sodium hydroxide in 200 ml of water and then, in the course of 20 minutes, 38.8 g of bromine. When all has been dropped in, the batch is stirred for 8 hours at 20° to 25°C. The reaction solution is then cautiously adjusted with concentrated hydrochloric acid to pH 7, whereupon finely crystalline γ-amino- β-(p-chlorophenyl)butyric acid settles out. To purify it, it is recrystallized from water. Melting point is 206°to 208°C.

상표명

Kemstro (Schwarz Pharma); Lioresal (Medtronic); Lioresal (Novartis).

Therapeutic Function

Muscle relaxant

Biological Functions

Baclofen (Lioresal) is the parachlorophenol analogue of the naturally occurring neurotransmitter γ-aminobutyric acid (GABA).

일반 설명

Odorless or practically odorless white to off-white crystalline powder.

공기와 물의 반응

Insoluble in water.

반응 프로필

Baclofen is an amine. Amines are chemical bases. They neutralize acids to form salts plus water. These acid-base reactions are exothermic. The amount of heat that is evolved per mole of amine in a neutralization is largely independent of the strength of the amine as a base. Amines may be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable gaseous hydrogen is generated by amines in combination with strong reducing agents, such as hydrides.

건강위험

SYMPTOMS: Symptoms of exposure to Baclofen via ingestion may include drowsiness, insomnia, dizziness, weakness, mental confusion, nausea, constipation, anorexia, urinary retention, impotence, nystagmus, diplopia and incoordination. Ingestion may lead to cholinergic effects and lassitude. It may also lead to ataxia. Other symptoms due to ingestion may include impaired renal function, fatigue, headache, hypotension, urinary frequency, rash, pruritis, ankle edema, excessive perspiration, weight gain, nasal congestion, and rarely, euphoria, excitement, depression, hallucinations, paresthesia, muscle pain, tinnitus, slurred speech, tremor, rigidity, dystonia, blurred vision, strabismus, miosis, mydriasis, dysarthia, epileptic seizure, dyspnea, palpitation, chest pain, syncope, dryness of the mouth, taste disorder, abdominal pain, vomiting, diarrhea, blood in the stools, enuresis, dysuria, inability to ejaculate, nocturia and hematuria. Overexposure through ingestion may result in seizures, and coma with respiratory depression. Aspiration pneumonia is a frequent complication of coma with respiratory depression. Other symptoms due to overdosage may include vomiting, muscular hypotonia, drowsiness, and accommodation disorders. Cyanosis has been reported. Chronic ingestion may result in drowsiness, depression, weakness, anxiety, ataxia, headaches, blurred vision, gastric upset and pruritic skin rashes characterized by urticaria or erythematous macular eruptions. Sudden withdrawal after chronic ingestion may cause auditory and visual hallucinations, anxiety and tachycardia. Seizures may also occur after sudden withdrawal. Abuse may lead to drug dependence.

화재위험

Flash point data for Baclofen are not available. Baclofen is probably combustible.

생물학적 활성

Selective GABA B receptor agonist. Skeletal muscle relaxant.

Mechanism of action

Baclofen appears to affect the neuromuscular axis by acting directly on sensory afferents, γ-motor neurons, and collateral neurons in the spinal cord to inhibit both monosynaptic and polysynaptic reflexes. The principal effect is to reduce the release of excitatory neurotransmitters by activation of presynaptic GABAB receptors. This seems to involve a G protein and second-messenger link that either increases K+ conductance or decreases Ca++ conductance.

Clinical Use

Baclofen is an agent of choice for treating spinal spasticity and spasticity associated with multiple sclerosis. It is not useful for treating spasticity of supraspinal origin. Doses should be increased gradually to a maximum of 100 to 150 mg per day, divided into four doses.

부작용

Side effects are not a major problem, and they can be minimized by graduated dosage increases.They include lassitude, slight nausea, and mental disturbances (in including confusion, euphoria, and depression). The drowsiness is less pronounced than that produced by diazepam—an important therapeutic advantage. Hypotension has been noted, particularly following overdose. Elderly patients and patients with multiple sclerosis may require lower doses and may display increased sensitivity to the central side effects. Baclofen may increase the frequency of seizures in epileptics.

Safety Profile

Poison by ingestion,subcutaneous and intravenous routes. Human systemiceffects by ingestion: blood pressure lowering, coma,muscle weakness, pulse rate decrease, respiratorydepression. When heated to decomposition it emits toxicfumes of Cl-

Chemical Synthesis

Baclofen, 4-amino-3-(4-chlorophenyl)butyric acid (15.3.5), is synthesized in two ways. According to the first, 4-chlorobenzaldehyde is condensed with two moles of acetoacetic ester, giving the product (15.3.1), which initially undergoes alkaline hydrolysis and decarboxylation forming 3-(4-chlorphenyl)glutaric acid (15.3.2). Dehydration of this gives 3-(4-chlorophenyl)glutaric acid anhydride (15.3.3), and further treatment with ammonia gives the corresponding glutarimide (15.3.4). Reacting this with an alkaline solution of a halogen (Hofmann rearrangement) gives baclofen (15.3.6).

Veterinary Drugs and Treatments

Baclofen may be useful to decrease urethral resistance in dogs to treat urinary retention. It is not recommended for cats.

신진 대사

Baclofen is rapidly and effectively absorbed after oral administration. It is lipophilic and able to penetrate the blood-brain barrier.Approximately 35% of the drug is excreted unchanged in the urine and feces.

바클로펜 준비 용품 및 원자재

원자재

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