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テラゾシン塩酸塩二水和物
テラゾシン塩酸塩二水和物 · 4-アミノ-6,7-ジメトキシ-2-[4-(テトラヒドロ-2-フロイル)-1-ピペラジニル]キナゾリン塩酸塩二水和物 · テラゾシン塩酸塩水和物 · テラゾシン塩酸塩水和物 (JAN) · Terazosin hydrochlor · Terazosin HCL dihydrate · TERAZOSIN MONOHYDROCHLORIDE DIHYDRATE · Hytrinex

識別子と物理属性
| CAS No. | 70024-40-7 |
|---|---|
| 分子式 | C19H30ClN5O6 |
| 平均分子量 | 459.9 g/mol |
| 単同位体質量 | 459.18846136 g/mol |
| SMILES | COc1cc2nc(N3CCN(C(=O)C4CCCO4)CC3)nc(N)c2cc1OC.Cl.O.O |
| InChIKey | NZMOFYDMGFQZLS-UHFFFAOYSA-N |
| PubChem CID | 63016 |
| ChEMBL | CHEMBL1201091 |
| DTXSID | DTXSID801366621 |
| 現地名 | テラゾシン塩酸塩二水和物 |
化学・物理的性質
| 極性表面積 | 105 |
|---|---|
| 水素結合供与体数 | 4 |
| 水素結合受容体数 | 10 |
| 回転可能結合数 | 4 |
| 重原子数 | 31 |
| 形式電荷 | 0 |
| 複雑度 | 544 |
| Human Drugs | FDA approved drugs -> Active ingredient |
| 融点 | 271-274°C |
| 貯蔵条件 | Sealed in dry,Room Temperature |
| 溶解度 | 水に溶けにくく、メタノールに溶けにくく、エタノール (96%) に溶けにくく、アセトンにほとんど溶けない。 |
| 外観・状態 | Solid |
| 色 | 白い |
| 主な用途 | 医薬品(低分子化合物) |
| InChI | 1S/C19H25N5O4.ClH.2H2O/c1-26-15-10-12-13(11-16(15)27-2)21-19(22-17(12)20)24-7-5-23(6-8-24)18(25)14-4-3-9-28-14/h10-11,14H,3-9H2,1-2H3,(H2,20,21,22)1H2*1H2 |
| InChIKey | NZMOFYDMGFQZLS-UHFFFAOYSA-N |
| SMILES | O=C(C1CCCO1)N1CCN(C2N=C3C(C=C(C(=C3)OC)OC)=C(N)N=2)CC1.[H]Cl.[H]O[H].[H]O[H] |
| CAS データベース | 70024-40-7(CAS DataBase Reference) |
化学的特性
White or slightly yellow, crystalline powder.
安全性と法規制
| Treatment | Should overdosage of Terazosin lead to hypotension, support of the cardiovascular system is of first importance. Restoration of blood pressure and normalization of heart rate may be accomplished by keeping the patient in the supine position. If this measure is inadequate, shock should first be treated with volume expanders. If necessary, vasopressors should then be used and renal function should be monitored and supported as needed. Laboratory data indicate that Terazosin is highly protein boundtherefore, dialysis may not be of benefit. (L1712) |
|---|---|
| 健康影響 | Hypotension, palpitations, postural hypotension, syncope, peripheral edema, weight gain, dyspnea, nasal congestion/rhinitis, impotence. |
| 暴露経路 | Oral. Essentially completely absorbed in man (90% bioavailability). |
| 毒性の概要 | Terazosin selectively and competitively inhibits vascular postsynaptic alpha(1)-adrenergic receptors, resulting in peripheral vasodilation and a reduction of vascular resistance and blood pressure. Unlike the nonselective alph-adrenergic blockers phenoxybenzamine and phentolamine, terazosin does not block presynaptic alpha(2)-receptors and, hence, does not cause reflex activation of norepinephrine release to produce reflex tachycardia. |
| Signs and Symptoms | Asthenia, postural hypotension, dizziness, somnolence, nasal congestion/rhinitis. |
| Carcinogen Classification | No indication of carcinogenicity to humans (not listed by IARC). |
| Drug Induced Liver Injury | Drug Induced Liver Injury Rank (DILIrank 2.0)Terazosin hydrochloridevNo-DILI-concernNo matchDOI:10.1016/j.drudis.2016.02.015 |
| Toxicity Data | LD50: 259.3mg/kg (parental-intravenous, Mouse) (A308) |
| 水環境危害等級(WGK) | WGK 3 |
| RTECS 番号 | TK8046000 |
| 毒性 | LD50 in male, female rats (mg/kg): 277, 293 i.v. (Fort) |
| 税関コード | 2934990002 |
| 危険文句(R) | 22 |
用途
使用
Terazosin Hydrochloride Dihydrate is an α-1-adrenergic blocker related to prazosin.