| Description | Dorzolamide hydrochloride (MK507 hydrochloride) is the hydrochloride salt form of dorzolamide, an inhibitor of carbonic anhydrase, a zinc-containing enzyme that catalyzes the rapid conversion of carbon dioxide and water into carbonic acid, protons and bicarbonate ions. Distributed throughout many cells and tissues, various carbonic anhydrases play important roles in mineral and metabolic homeostasis. |
| In vitro | 在兔中,Dorzolamide盐酸大大降低眼压并且在晚上也有效.Dorzolamide最大限度降低了青光眼猴子的眼压,分别达22％,30％和37％.Dorzolamide（灌输药物眼1天至5天）和口服methazolamide（给药3天通过对第5天）联用明显降低眼压,这种作用在第1天,3天和5天均有效.与每日两次口服甲醋唑胺和2％多佐胺的组合相比,每天滴注三次的多佐胺（2％）产生类似的IOP下降. |
| In vivo | Dorzolamide引起视网膜血管扩张血管,通过三种不同的机制直接作用从而导致预收缩,以及独立于细胞外pH值的变化。Dorzolamide碳酸酐酶（CA）II的强效抑制剂,其穿透巩膜和角膜以达到睫状突并降低HCO3和房水的形成。 |
| Target activity | CA IV:31 nM(Ki), CA II:1.9 nM(Ki), CA I:6000 nM(Ki) |
| Synonyms | MK507 hydrochloride, L671152 hydrochloride, MK-507 (L-671152) HCl, 盐酸多佐胺, Dorzolamide HCl |
| molecular weight | 360.9 |
| Molecular formula | C10H17ClN2O4S3 |
| CAS | 130693-82-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 13.3mg/ml(36.9mM) DMSO: 1mg/ml(2.77mM) |
| References | 1. Maren TH, et al. J Ocul Pharmacol Ther, 1997, 13(1), 23-30. 2. Josefsson A1, et al. Exp Eye Res, 2004, 78(2), 215-221. 3. Gelatt KN, et al. Vet Ophthalmol, 2001, 4(1), 61-67. 4. Percicot CL, et al. J Pharmacol Toxicol Methods, 1996, 36(4), 223-228. 5. Sugrue MF, et al. J Ocul Pharmacol Ther, 1996, 12(3), 363-376. |