Name | cyclopenthiazide |
Synonyms | su8341 salimid salimed navidrix tsiklometiazid cyclomethiazide Cyclopenthiazide cyclopenthiazide 3-cyclopentylmethylhydrochlorothiazidederiv 2h-1,2,4-benzothiadiazine-7-sulfonamide,6-chloro-3-(cyclopentylmethyl)-3,4-dih 6-chloro-3-cyclopentylmethyl-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulphonamide 1,1-dioxide 6-chloro-3-(cyclopentylmethyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide |
CAS | 742-20-1 |
EINECS | 212-012-5 |
InChI | InChI=1/C13H18ClN3O4S2/c14-9-6-10-12(7-11(9)22(15,18)19)23(20,21)17-13(16-10)5-8-3-1-2-4-8/h6-8,13,16-17H,1-5H2,(H2,15,18,19) |
Molecular Formula | C13H18ClN3O4S2 |
Molar Mass | 379.88 |
Density | 1.3650 (rough estimate) |
Melting Point | 230° |
Boling Point | 605.6±65.0 °C(Predicted) |
Flash Point | 320.1°C |
Water Solubility | 50mg/L(room temperature) |
Solubility | Acetonitrile (Slightly), DMSO (Slightly), Methanol (Sparingly) |
Vapor Presure | 1.29E-14mmHg at 25°C |
Appearance | Solid |
Color | White to Off-White |
pKa | 9.00±0.40(Predicted) |
Storage Condition | Refrigerator |
Refractive Index | 1.6100 (estimate) |
Physical and Chemical Properties | White powder. Melting point 238-242 ℃, soluble in ethanol, ether, acetone, slightly soluble in chloroform, insoluble in water, odorless, almost tasteless. |
Use | Content determination |
Toxicity | LD50 in rats, mice (mg/kg): 141.8 ±24, 232.4 ±25 i.v. (Barrett) |
indications | cyclopentothiazide is suitable for patients with various types of edema and hypertension, and can also be used for diabetes insipidus. It can inhibit the reabsorption of Na and Cl-by the cortex of the ascending branch of the renal tubules and the distal convoluted tubules, thereby exerting a diuretic effect. This product also has a blood pressure lowering effect. In the early stage of medication, it reduces blood volume due to diuresis and reduces blood volume. In the later stage of medication, the body loses sodium slightly, and the cells of the arteriolar wall are low in sodium. The amount of Ca2 in the cell is reduced by Na -Ca2 exchange. The responsiveness of blood vessels to vasoconstriction substances is reduced, which causes vasodilation and blood pressure drop. Cyclopentothiazine also has the antihypertensive effect of other antihypertensive drugs and in patients with diabetes insipidus, this product has antidiuretic effect and can reduce the urine output of patients with diabetes insipidus. Long-term or large-dose users should pay attention to supplement potassium salt or combined with potassium supplementation diuretics to prevent hypokalemia. Cyclopentothiazide tablets are currently on the market. |
Application | Cyclopentothiazide inhibits the co-transport of sodium ions and chloride ions in the cortex of the ascending branch of the medulina and the distal tubules, reducing the reabsorption of sodium ions in the original urine and exerting a diuretic effect. Cyclopentothiazide is often used in hypertension. Hypertension can cause cerebral arteriosclerosis, cerebral infarction, cerebral hemorrhage, renal arteriosclerosis and even uremia. Cyclopentenethiazine has been widely used as a diuretic clinically in the last century. Since Cyclopentenethiazine is a compound that cannot penetrate the blood-brain barrier, recent studies have found that Cyclopentenethiazine can act on both excitatory (glutamate) and inhibitory (GABA) neurotransmitter receptors in the brain, and can enhance the excitability of glutamate receptors while inhibiting the inhibitory effect of GABA receptors, this leads to increased excitability of the central nervous system. |
precautions | 1. patients with hepatic coma or tendency of hepatic coma are prohibited. 2. Pay attention to correct the electrolyte imbalance in the body. 3. Don't avoid salt, long-term users should give potassium salt. |
chemical properties | white powder. Melting point 238-242 ℃, soluble in ethanol, ether, acetone, slightly soluble in chloroform, insoluble in water, odorless, almost tasteless. |
use | is used to treat edema and hypertension. |
production method | cyclopentyl acetaldehyde and 4, 6-disulfonamido-3-chloroaniline are cyclocyclic. |
EPA chemical information | information provided by: ofmpub.epa.gov (external link) |