Naloxone hydrochloride, crystalline powder
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Naloxine is specific and competitive opiate antagonist at mu, kappa, delta and sigma receptors; it blocks the action of sigma-agonists at opioid sites. It displaces morphine and other opiate agonists from the opiate receptor. It is more potent than Nalorphine and is also an effective antagonist for mixed agonist-antagonist drugs such as pentazorcine. Naloxone has no respiratory depressant activity.
The role of naloxone (1 µM) and other opioids on apoptosis in several human cancer cell lines has been probed. Naloxone (10-100 µM) has been used to study proliferation and neurogenesis in cultured rat adult hippocampal progenitors. Naloxone has also been utilized to modulate the NMDA receptor activation capability of the µ-opioid receptor agonist DAMGO.
Soluble in water (50 mg/mL - clear, colorless to faint yellow solution), ethanol (3.3 mg/mL), or methanol (50 mg/mL - clear, colorless solution). Solutions are stable for three to four months refrigerated if protected from light. Practically insoluble in ether and chloroform.
Naloxone has an extremely high affinity for µ-opioid receptors in the central nervous system. Naloxone is a µ-opioid receptor competitive antagonist, and its rapid blockade of those receptors often produces rapid onset of withdrawal symptoms. Naloxone also has an antagonist action, though with a lower affinity, at κ- and δ-opioid receptors.
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Formula:
C₁₉H₂₂ClNO₄ MW: 363.838 g/mol |
MDL Number:
MFCD00069322 CAS Number: 357-08-4 |
Specification Test Results
| Form | Off-white Crystalline Powder |
| Storage | Store at +4 °C, Store Desiccated. |
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