73218-79-8
中文名稱
鹽酸安普樂定
英文名稱
Apraclonidine hydrochloride
CAS
73218-79-8
分子式
C9H11Cl3N4
MDL 編號
MFCD00135922
分子量
281.57
MOL 文件
73218-79-8.mol
更新日期
2024/11/14 17:46:49
73218-79-8 結(jié)構(gòu)式
基本信息
中文別名
鹽酸阿可樂定鹽酸安普樂定
2-(4-氨基-2,6-二氯苯胺基)-2-咪唑啉鹽酸鹽
英文別名
2-[4-AMINO-2,6-DICHLOROANILINO]-2-IMIDAZOLINE HYDROCHLORIDE2-[(4-AMINO-2,6-DICHLOROPHENYL)IMINO]IMIDAZOLIDINE MONOHYDROCHLORIDE
APRACLONIDINE HCL
APRACLONIDINE HYDROCHLORIDE
P-AMINOCLONIDINE HYDROCHLORIDE
2-(4-amino-2,6-dichlorophenylimino)imidazolidinehydrochloride
2,6-dichloro-n(sup1)-(2-imidazolidinylidene)-1,4-benzenediaminehydrochlorid
2,6-dichloro-n(sup1)-(4,5-dihydro-1h-imidazol-2-yl)-1,4-benzenediaminemonoh
3,5-dichloro-4-(2-imidazolidinylidenimino)anilinehydrochloride
4-benzenediamine,2,6-dichloro-n(sup1)-(4,5-dihydro-1h-imidazol-2-yl)-mono
alo-2145
iopidine
iopidineophthalmicsolution
nc14hydrochloride
2,6-Dichloro-N1-(4,5-dihydro-1H-imidazol-2-yl)-1,4-benzenediamine Hydrochloride
AL 02145
p-Aminoclonidine Monohydrochloride
2-(4-Amino-2,6-dichloroanilino)-2-imidazoline hydrochloride, Apraclonidine hydrochloride
Iopidine UD
所屬類別
原料藥：眼科用藥物理化學(xué)性質(zhì)
熔點>2300C
儲存條件2-8°C
溶解度45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 1.4 mg/mL Solutions may be stored for several days at 4?#x00b0;C
形態(tài)solid
顏色white
穩(wěn)定性濕氣敏感
CAS 數(shù)據(jù)庫73218-79-8(CAS DataBase Reference)
安全數(shù)據(jù)
常見問題列表
作用
安普樂定具有較強的α2-腎上腺素能受體的作用，通過激活眼內(nèi)α2-腎上腺素能受 體，降低眼內(nèi)壓。本品血腦屏障通透率低，中樞和心血管作用弱，全身性副作用低且無明顯 擴瞳作用，因而有很好的應(yīng)用前景，其是治療激光手術(shù)所引起的眼內(nèi)壓升高的特效藥物。制備
以2,6-二氯-4-硝基苯胺、甲酸和乙酸酐等為反應(yīng)起始原料，進(jìn)行甲?；磻?yīng)得到N-(2,6-二氯-4-硝基苯基)甲酰胺；而后經(jīng)氯化、環(huán)合得到2-(2’,6’-二氯-4’-硝基 苯胺基)-2-咪唑啉，最后用水合肼將2-(2’,6’-二氯-4’-硝基苯胺基)-2-咪唑啉中硝基還 原，制得鹽酸安普樂定(1)，總收率達(dá)45％。其中用水合肼作為還原劑2-(2’,6’-二氯-4’-硝 基苯胺基)-2-咪唑啉中硝基還原為首次報道，對亞胺鍵未見影響，該步收率達(dá)80％以上。生物活性
Apraclonidine (Iopidine)是一種擬交感神經(jīng)要，用于治療青光眼。它是α2-腎上腺素能受體激動劑。體外研究
Apraclonidine hydrochloride (ALO 2145) is more commonly used topically for glaucoma, as it penetrates the cornea and blood-brain barrier to a lesser extent and, thus, has fewer adverse systemic effects.
體內(nèi)研究
Apraclonidine hydrochloride (ALO 2145) is effective in animal models of elevated IOP as well as glaucoma in humans. The ocular hypotensive effects of Apraclonidine are usually attributed to reduced aqueous humor synthesis and vasoconstrictor actions at the anterior segment branches of the ophthalmic artery.