5-(N,N-Hexamethylene)amiloride
amiloride
CAS: 1428-95-1
Molecular Formula: C12H18ClN7O
5-(N,N-Hexamethylene)amiloride - Names and Identifiers
5-(N,N-Hexamethylene)amiloride - Physico-chemical Properties
| Molecular Formula | C12H18ClN7O |
| Molar Mass | 311.77 |
| Density | 1.63±0.1 g/cm3(Predicted) |
| Melting Point | 224-225 °C |
| Boling Point | 638.2°C at 760 mmHg |
| Flash Point | 339.8°C |
| Vapor Presure | 3.47E-16mmHg at 25°C |
| pKa | 8.81±0.46(Predicted) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.742 |
5-(N,N-Hexamethylene)amiloride - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. |
| Safety Description | S22 - Do not breathe dust. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | 2811 |
| WGK Germany | 3 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
5-(N,N-Hexamethylene)amiloride - Reference Information
| indications | mainly treats edematous diseases and can also be used as adjuvant therapy for refractory hypokalemia. |
| pharmacokinetics | absorption by gastrointestinal tract after oral administration. The half-life of action is 6-9 hours, the onset time of a single oral dose is 2 hours, the peak time of serum concentration is 3-4 hours, and the effective duration is 6-10 hours. About 50% is excreted from the urine with the prototype drug, and the 40% is excreted with the feces within 72 hours. |
| drug-related effects | 1) adrenocortical hormone, especially for those with strong mineralocorticotropic hormone, adrenocorticotropic hormone can weaken the diuretic effect of this drug and antagonize the potassium retention effect of this drug. 2) Estrogen can cause water and sodium retention, thereby weakening the diuretic effect of this drug. 3) Non-steroidal anti-inflammatory analgesics, especially indomethacin, can reduce the diuretic effect of this drug, and increase renal toxicity when combined. 4) sympathomimetic drugs reduce the antihypertensive effect of this drug. 5) Dopamine enhances the diuretic effect of this drug. 6) combined with drugs that cause blood pressure drop, diuretic and antihypertensive effects are enhanced. 7) and should not be combined with co-taobao potassium diuretics or potassium salts. When combined with the following drugs, the chance of hyperkalemia increases, such as potassium-containing drugs, blood stocks (potassium containing 20mmol/L, potassium containing up to 65mmol/L if stored for more than 10 days), angiotensin converting enzyme inhibitors, Angiotensin II receptor antagonists and cyclosporine A, etc. 8) combined with glucose insulin solution, alkali agent and sodium potassium-lowering exchange resin, the chance of hyperkalemia is reduced. 9) This medicine prolongs the half-life of digoxin. 10) combined with ammonium chloride is prone to metabolic acidosis. 11) When combined with nephrotoxic drugs, nephrotoxicity increases. 12) sodium glycyrrhiza and licorice preparations have aldosterone-like effects, which can reduce the diuretic effect of this drug. |
| Biological activity | 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride), a derivative of amiloride, is also an effective Na /H exchange inhibitor, reduces the intracellular pH (pHi) of leukemia cells and induces their apoptosis. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also a HIV-1 Vpu virus ion channel inhibitor, inhibiting mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in L929 cells with EC50 values of 3.91 μM and 1.34 μM, respectively. |
| target | Na /H exchanger EC50: 3.91 μM (MHV replication), 1.34 μM (HCoV229E replication) |
Last Update：2024-04-09 20:45:29
