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| 化学名: | ドルゾラミド塩酸塩 | | 英語化学名: | Dorzolamide Hydrochloride | | 别名: | 3-b)thiopyran-2-sulfonamide,5,6-dihydro-4-(ethylamino)-6-methyl-4h-thieno(;mk-0507;monohydrochloride,(4s-trans)-7-dioxide;Dorzolomide hydrochloride, >=99%;4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, hydrochloride;MK-507 (L-671152) HCl;4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, hydrochloride (1:1), (4S,6S)-;(4S,6S)-4-(Ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxid | | CAS番号: | 130693-82-2 | | 分子式: | C10H17ClN2O4S3 | | 分子量: | 360.9 | | EINECS: | 620-304-2 | | カテゴリ情報: | Inhibitors;Heterocycles;Sulfur & Selenium Compounds;Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals;Dorzolamide;API;Trusopt, Cosopt;Other APIs | | Mol File: | 130693-82-2.mol |  |
| 融点 | 265-2670C | | 比旋光度 | D24 -8.34° (c = 1 in methanol) | | 貯蔵温度 | Keep in dark place,Inert atmosphere,2-8°C | | 溶解性 | Soluble in water, slightly soluble in methanol, very slightly soluble in anhydrous ethanol. | | 色 | White to Off-White | | 極大吸収波長 (λmax) | 254nm(CHCl3:MeOH= aq.)(lit.) | | Merck | 14,3426 | | BRN | 5896026 | | CAS データベース | 130693-82-2(CAS DataBase Reference) |
| WGK Germany | 3 | | RTECS 番号 | XJ9095163 | | HSコード | 2935904000 |
| | ドルゾラミド塩酸塩 Usage And Synthesis |
| 外観 | 白色～ほとんど白色粉末～結晶 | | 効能 | 抗緑内障薬, 炭酸脱水酵素阻害薬 | | 商品名 | トルソプト (参天製薬) | | 説明 | Dorzolamide hydrochloride was introduced in the U.S.A. as eye drops
for the treatment of open-angle glaucoma and ocular hypertension. Dorzolamide is a
potent carbonic anhydrase inhibitor that, on topical administration, lowers intraocular
pressure (IOP). In a clinical study in patients with bilateral primary open-angle
glaucoma or ocular hypertension, dorzolamide (0.7-2%) was found to significantly lower
IOP throughout the day. Dorzolamide has been shown to be effective as a single
therapy or in combination with β-blockers. | | 説明 | Dorzolamide (hydrochloride) (Item No. 26303) is an analytical reference standard categorized as a carbonic anhydrase inhibitor diuretic. Diuretics have been used in sports doping to reduce weight or anabolic androgenic steroid-induced water retention, or as masking agents. This product is intended for use in analytical forensic applications. This product is also available as a general research tool . | | 化学的特性 | White Powder | | Originator | Merck (U.S.A.) | | 使用 | Carbonic anhydrase inhibitor. Antiglaucoma agent. | | 使用 | An inhibitor of carbonic anhydrase. | | 使用 | Dorzolamide HCl Ophthalmic Solution is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. | | 使用 | Antiglaucoma drug;Carbonic anhydrase inhibitor | | 使用 | analgesic | | 定義 | ChEBI: The hydrochloride salt of dorzolamide. It is used in ophthalmic solutions to lower increased intraocular pressure in the treatment of open-angle glaucoma and ocular hypertension. | | Manufacturing Process | Manufacturing process for Dorzolamide hydrochloride includes these steps as follows: Step A: Sulfuric Acid Ritter Procedure;Step B: Sulfonylation Procedure Step C: Chlorosulfonylation Procedure;Step D: Amidation Procedure;Step E: Reduction via Borane Generated in situ Procedure;Step F: Maleate Salt Formation Procedure;Step G: Crude Hydrochloride Salt Formation;Step H: Recrystallization Procedure. | | brand name | Trusopt (Merck). | | Therapeutic Function | Antiglaucoma | | Veterinary Drugs and Treatments | Dorzolamide is often used in the contralateral eye of a dog with
primary glaucoma to prevent development of bilateral disease. It
is also an excellent agent to consider for most secondary glaucomas
in dogs and cats because it has no effect on pupil size. Like the
related oral carbonic anhydrase inhibitors (dichlorphenamide or
Daranide?, methazolamide or Neptazane?), dorzolamide decreases
aqueous humor production by the ciliary body epithelium by altering
pH and affecting the H+/Na+ active transport exchange mechanism.
Oral carbonic anhydrase inhibitors cause numerous systemic
side effects such as metabolic acidosis and panting, diarrhea, vomiting,
anorexia and others, all of which can be avoided with topical
carbonic anhydrase inhibitors. |
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