CAS 298-57-7 MFCD00056037-Cinnarizine 1-二苯基甲基-4-肉桂酰基哌嗪 TAO{mole}

Cinnarizine 1-二苯基甲基-4-肉桂酰基哌嗪

CAS 298-57-7 MFCD00056037

化学结构图

SMILES: C(=Cc1ccccc1)CN1CCN(C(c2ccccc2)c2ccccc2)CC1

化学属性

Mol. Formula	C26H28N2
Mol. Weight	369
TSCA	No
Melting Point	117.0 to 121.0 deg-C
Appearance	脑益嗪盐酸盐，C26H28N2·2HCI，[7002-58-6]，熔点192℃，在水中溶解度为2mg/100ml。 powder

别名和识别编码

Chemical Name	Piperazine, 1-(diphenylmethyl)-4-(3-phenyl-2-propen-1-yl)-
MDL Number	MFCD00056037
CAS Number	298-57-7
Synonym	1-(Diphenylmethyl)-4-(3-phenyl-2-propenyl)piperazine Cinarizina Inkey Cinarizina Ratiopharm Cinarizine Cinazière Cinna Cinnarizin AL Cinnarizin Ratiopharm Cinnarizin Siegfried Cinnarizin-ratiopharm Cinnarizine Cinnarizine L Tartrate Cinnarizine L-Tartrate Cinnarizine L-Tartrate (1:1) Cinnarizine, (E)-Isomer Cinnarizine, Dihydrochloride Cinnipirine Cisaken Dihydrochloride Cinnarizine Dimitronal L-Tartrate, Cinnarizine R 516 R-516 R516 Stugeron Stugeron Forte Von Ct, Cinnarizin cinnarizin von ct {} {} {} {} {} {} 1-trans-Cinnamyl-4-diphenylmethylpiperazine
PubChem Substance ID	1547484
EC Number	206-064-8
Merck Number	2305
Chemical Name Translation	1-二苯基甲基-4-肉桂酰基哌嗪
Beilstein Registry Number	0626121
Reaxys-RN	626120
InChI	InChI=1S/C26H28N2/c1-4-11-23(12-5-1)13-10-18-27-19-21-28(22-20-27)26(24-14-6-2-7-15-24)25-16-8-3-9-17-25/h1-17,26H,18-22H2/b13-10+

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安全信息

RTECSTL3430000

WGK Germany2

Personal Protective Equipment Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter

Safety Statements

S24/25 Avoid contact with skin and eyes 避免皮肤和眼睛接触；
S22 Do not breathe dust 不要吸入粉尘；

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : >4500 mg/kg
TOXIC EFFECTS :
   Behavioral - altered sleep time (including change in righting reflex)
   Behavioral - somnolence (general depressed activity)
   Skin and Appendages - hair
REFERENCE :
   KSRNAM Kiso to Rinsho.  Clinical Report.  (Yubunsha Co., Ltd., 1-5, Kanda
   Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan)  V.1-    1960-
   Volume(issue)/page/year: 16,1735,1982

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : >500 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NIIRDN Drugs in Japan (Ethical Drugs).  (Yakugyo Jiho Co., Ltd., Tokyo,
   Japan)  Volume(issue)/page/year: -,515,1990

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : >6500 mg/kg
TOXIC EFFECTS :
   Behavioral - altered sleep time (including change in righting reflex)
   Behavioral - somnolence (general depressed activity)
   Skin and Appendages - hair
REFERENCE :
   KSRNAM Kiso to Rinsho.  Clinical Report.

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human - woman
DOSE/DURATION           : 22500 mg/kg/22W-I
TOXIC EFFECTS :
   Nutritional and Gross Metabolic - other changes
REFERENCE :
   APHRER Annals of Pharmacotherpy.  (Harvey Whitney Books Co., POB 42696,
   Cincinnati, OH 45242) V. 26-    1992-  Volume(issue)/page/year: 26,928,1992

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Mammal - do

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human - man
DOSE                    : 193 mg/kg
SEX/DURATION            : male 13 week(s) pre-mating
TOXIC EFFECTS :
   Reproductive - Paternal Effects - impotence
REFERENCE :
   APHRER Annals of Pharmacotherpy.  (Harvey Whitney Books Co., POB 42696,
   Cincinnati, OH 45242) V. 26-    1992-  Volume(issue)/page/year: 27,370,1993

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 3750 mg/kg
SEX/DURATION            : female 30 day(s) pre-mating
TOXIC EFFECTS :
   Reproductive - Maternal Effects - uterus, cervix, vagina
REFERENCE :
   KSRNAM Kiso to Rinsho.  Clinical Report.  (Yubunsha Co., Ltd., 1-5, Kanda
   Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan)  V.1-    1960-
   Volume(issue)/page/year: 16,1748,1982

Storage condition 0-10°C

Hazard statements

H302 Harmful if swallowed 吞食有害
H315 Causes skin irritation 会刺激皮肤
H317 May cause an allergic skin reaction 可能导致皮肤过敏
H319 Causes serious eye irritation 严重刺激眼睛
H332 Harmful if inhaled 吸入有害
H335 May cause respiratory irritation 可能导致呼吸道刺激
H360 May damage fertility or the unborn child 可能对生育能力或未出生婴儿造成伤害
H400 Verytoxictoaquaticlife 对水生生物毒性非常大。
H410 Verytoxictoaquaticlifewithlonglastingeffects 对水生生物毒性非常大并具有长期影响。
H413 Maycauselonglastingharmfuleffectstoaquaticlife 可能对水生生物造成长期持续有害影响。

Precautionary statements

P201 Obtain special instructions before use. 使用前获取专门指示。
P202 Do not handle until all safety precautions have been read and understood. 已阅读并理解所有的安全预防措施之前，切勿操作。
P203
P261 Avoid breathing dust/fume/gas/mist/vapours/spray. 避免吸入粉尘/烟/气体/烟雾/蒸汽/喷雾。
P264 Wash hands thoroughly after handling. 处理后要彻底洗净双手。
P264+P265
P270 Do not eat, drink or smoke when using this product. 使用本产品时不要吃东西，喝水或吸烟。
P271 Use only outdoors or in a well-ventilated area.? 只能在室外或通风良好的地方使用。
P272 Contaminated work clothing should not be allowed out of the workplace. 污染的工作服不得带出工作场所。
P273 Avoid release to the environment. 避免释放到环境中。
P280 Wear protective gloves/protective clothing/eye protection/face protection. 戴防护手套/防护服/眼睛的保护物/面部保护物。
P281 Use personal protective equipment as required. 使用所需的个人防护装备。
P301+P312
P301+P317
P302+P352
P304+P312
P304+P340
P305+P351+P338
P308+P313
P312 Call a POISON CENTER or doctor/physician if you feel unwell. 如果你感觉不适，呼叫解毒中心或医生/医师。
P317
P318
P319
P321 Specific treatment (see … on this label). 具体治疗（见本标签上的）。
P330 Rinse mouth. 漱口
P332+P313
P332+P317
P333+P313
P333+P317
P337+P313
P337+P317
P362 Take off contaminated clothing and wash before reuse. 脱掉污染的衣服，清洗后方可重新使用
P362+P364
P363 Wash contaminated clothing before reuse. 被污染的衣服洗净后方可重新使用。
P391 Collect spillage. Hazardous to the aquatic environment 收集对水环境有危害的泄漏物。
P403+P233
P405 Store locked up. 上锁保管。
P501 Dispose of contents/container to..… 处理内容物/容器.....

GHS Symbol

其他信息

用途一:长效多功能的血管收缩拮抗剂，能扩张血管，改善血循环，预防血管脆化，可用于治疗脑血管疾病，对颈性眩晕等引起的头痛，头晕失眠、记忆力减退，偏瘫，肢体麻木无力，言语不清等症也有疗效。
上游原料:四氢呋喃 --> 碳酸钾 --> 哌嗪 --> 稀盐酸 --> 己酰氯 --> 二苯甲基哌嗪 --> 二苯基溴甲烷 --> 烯丙苯 --> 二苯氯甲烷 --> 肉桂基氯
MOL 文件:298-57-7.mol
Sigma Aldrich:298-57-7(sigmaaldrich)
color:white
方法一:由无水哌嗪与溴代二苯甲烷制取二苯甲基哌嗪，再与苯丙烯氯缩合而得。二苯甲烷在光照下加热，滴加溴素，在130℃保温1h，即得溴代二苯甲烷，C13H11Br，[776-74-9]，熔点45℃。将溴代二苯甲烷滴加到哌嗪甲苯液中，于80-90℃搅拌3h，冷却后用水洗涤反应液，再用10%稀盐酸萃取，将酸层碱化析出沉淀，过滤烘干，得二苯甲基哌嗪。将其溶解在95%乙醇中，加入碳酸钠，在65℃左右滴加苯丙烯氯，滴完后，加热回流4h，趁热过滤，滤液放置过液，析出结晶，过滤，得脑益嗪粗品，经精制，得熔点117-119℃的成品。以二苯甲烷计，总收率48.2%。
周围血管扩张药:桂利嗪是一种哌嗪类钙通道阻滞剂，属于周围血管扩张药。又称肉桂嗪、肉桂苯哌嗪、桂益嗪、脑益嗪，为白色或类白色结晶或结晶性粉末，无臭，几无味。几不溶于水，溶于沸乙醇，易溶于氯仿或苯。桂利嗪对血管平滑肌有扩张作用，对各种血管收缩物质如5-羟色胺、肾上腺素、缓激肽、增压素等有拮抗作用，能缓解血管痉挛。其解痉作用比罂粟碱强，镇静作用不明显。本品能使脑血流量显著增加，能显著地改善脑循环及冠脉循环，作用持续时间也较长，且对各种血管活性物质有抑制作用，能缓解血管痉挛，防止血管脆化。在不影响心率和耗氧量的情况下能增加冠脉血流量和心输出量。静注本品可使血压短暂下降，但口服无此作用。另外，本品还有防止血管脆化作用和抗组胺作用。口服后30分钟内起效，3～7小时后血药浓度达峰值，作用可持续4小时。血药浓度半衰期3～24小时。临床上桂利嗪主要用于治疗脑血管障碍及周围血管病如脑栓塞、脑血栓形成、脑动脉硬化、高血压所致的脑循环不全、脑出血与蛛网膜下腔出血恢复期、脑外伤后遗症。对脑循环障碍所致的精神神经病变及冠状动脉硬化症等也有效。亦可用于治疗内耳眩晕症及其他迷路紊乱而引起的恶心、呕吐及运动病。桂利嗪主要不良反应为：偶见嗜睡、皮疹、胃肠道反应，发热感或头晕，静注使可使血压短暂下降；孕妇慎用；颅内出血、急性脑梗死忌用。