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132112-35-7

中文名稱 鹽酸羅哌卡因
英文名稱 Ropivacaine hydrochloride
CAS 132112-35-7
分子式 C17H27ClN2O
MDL 編號 MFCD02102164
分子量 310.86
MOL 文件 132112-35-7.mol
更新日期 2024/12/23 14:57:10
132112-35-7 結構式 132112-35-7 結構式

基本信息

中文別名
鹽酸羅哌卡因一水合物
(S)-1-丙基-2',6'-二甲基苯胺甲?;哙嘻}酸鹽一水合物
(s)-羅哌卡因鹽酸鹽
(-)-S)-N-(2,6-二甲基苯基)-1-正丙基哌啶-2-甲酰胺鹽酸鹽
鹽酸羅哌卡因
英文別名
ROPIVACAINE HCL
ROPIVACAINE HYDROCHLORIDE
ROPIVACAINE HYDROCHLORIDE MONOHYDRATE
ROPIVCACAINE HYDROCHLORIDE
S-ROPIVACAINE HCL
(S)-ROPIVACAINE HYDROCHLORIDE
(S)-1-propyl-2',6'-dimethylanilinoformoxylpiperidine monohydrochloride monohydrate
(S)-1-propyl-2',6'-dimethylanilinoformoxylpiperidine,monohydrochloride,monohydrate
(S)-Ropivaxaine hydrochloride
(S)-N-(2,6-dimethylphenyl)-1-propylpiperidine-2-carboxamide hydrochloride
Ropivacaine hydrochloride
(2S)-N-(2,6-Dimethylphenyl)-1-propyl-2-piperidinecarboxamide Hydrochloride Hydrate
LEA-103
所屬類別
原料藥:局部麻醉劑

物理化學性質

熔點267-269°C
比旋光度D20 -7.28° (c = 2 in water)
儲存條件2-8°C
溶解度H2O:可溶5mg/mL,澄清
形態(tài)粉末
顏色白色至灰白色
旋光性 (optical activity)[α]/D -9 to -12, c = 1 in methanol
InChIKeyVSHFRHVKMYGBJL-CKUXDGONSA-N
CAS 數(shù)據(jù)庫132112-35-7(CAS DataBase Reference)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS05
警示詞危險
危險性描述H318
危險品標志T,Xi
危險類別碼26/27/28-41
危險品運輸編號UN 2811 6.1 / PGIII
WGK Germany3
海關編碼2933399090

常見問題列表

概述
鹽酸羅哌卡因為酰胺類長效局麻藥。其脂溶性大于利多卡因,小于布比卡因,其麻醉強度為普魯卡因的8倍。因其在肝臟代謝的產(chǎn)物也有局麻作用,故作用較持久。主要用于區(qū)域阻滯麻醉和硬膜外麻醉,用于術后和分娩的鎮(zhèn)痛。
用途
鹽酸羅哌卡因適用于:
外科手術麻醉
-----硬膜外麻醉,包括剖宮產(chǎn)術
-----蛛網(wǎng)膜下腔麻醉
-----區(qū)域阻滯
急性疼痛控制
-----持續(xù)硬膜外輸注或間歇性單次用藥,如術后或陰道分娩鎮(zhèn)痛
-----區(qū)域阻滯
副作用

鹽酸羅哌卡因的一般副作用有低血壓、惡心、心動過緩、焦慮、感覺減退。

生物活性
Ropivacaine HCl (LEA-103) 是一種麻醉劑,通過可逆地抑制鈉離子流入來阻斷神經(jīng)纖維上沖動的傳導。
靶點

IC50: sodium ion influxIC50: 402.7 μM (TREK-1 in COS-7 cell's membrane)

體外研究

Ropivacaine HCl是一種局部麻醉劑。Ropivacaine HCl通過可逆抑制神經(jīng)纖維中鈉離子流引起神經(jīng)阻滯。Ropivacaine HCl的pKa是~8.2。Ropivacaine HCl在高血漿濃度下具有誘導心血管毒性和CNS毒性的可能性。

體內研究

Epidural administration of Ropivacaine hydrochloride monohydrate effectively blocks neuropathic pain (both mechanical allodynia and heat hyperalgesia) without induction of analgesic tolerance and significantly delays the development of neuropathic pain produced by peripheral nerve injury.
Ropivacaine hydrochloride monohydrate inhibits pressure-induced increases in filtration coefficient (Kf) without affecting pulmonary artery pressure (Ppa), pulmonary capillary pressures (Ppc), and zonal characteristics (ZC).
Ropivacaine hydrochloride monohydrate prevents pressure-induced lung edema and associated hyperpermeability as evidence by maintaining PaO2, lung wet-to-dry ratio and plasma volume in levels similar to sham rats.
Ropivacaine hydrochloride monohydrate inhibits pressure-induced NO production as evidenced by decreased lung nitro-tyrosine content when compared to hypertensive lungs.

Animal Model: Adult Sprague-Dawley rats (300–400g)
Dosage: 1 μM
Administration: Infusion (added to the perfusate reservoir)
Result: Attenuated pressure-dependent increases in filtration coefficient (K f ).
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