Nalfurafine is a synthetic kappa-opioid receptor (KOR) agonist and active pharmaceutical ingredient used in pharmaceutical formulations and research. It is a selective opioid receptor ligand with particular activity at the kappa-opioid receptor and is used in the treatment of uremic pruritus associated with hemodialysis.
Nalfurafine is commonly used in its hydrochloride salt form, Nalfurafine Hydrochloride, for pharmaceutical applications.
Nalfurafine is a specialized opioid receptor-modulating pharmaceutical API used in the development and manufacture of formulations for pruritus management and related pharmacological research.
Important API quality attributes include identity, assay, related substances, water content, residual solvents, elemental impurities, optical purity and other validated pharmaceutical quality parameters.
CAS Number: 58811-96-4
Molecular Formula: C28H32N2O5
Molecular Weight: 476.57 g/mol
Drug Class: Kappa-Opioid Receptor Agonist
Therapeutic Class: Antipruritic / Opioid Receptor Modulator
Therapeutic Area: Nephrology / Dermatology / Pain and Pruritus Research
Molecule Type: Synthetic Small Molecule
Common Pharmaceutical Form: Nalfurafine Hydrochloride
Nalfurafine acts primarily as a selective kappa-opioid receptor agonist.
Its pharmacological activity includes:
Activation of kappa-opioid receptors is considered an important mechanism through which Nalfurafine reduces severe itching associated with certain systemic conditions.
Nalfurafine API is used in pharmaceutical development for:
Nalfurafine is particularly relevant to uremic pruritus, a common complication associated with advanced kidney disease and hemodialysis.
Its selective kappa-opioid receptor activity provides a pharmacological approach to modulating itch pathways without relying on conventional antihistaminic mechanisms.
Nalfurafine is a synthetic small-molecule compound generally handled as a pharmaceutical active ingredient. The hydrochloride salt is used for pharmaceutical applications.
Appearance, particle characteristics, water content and other physicochemical properties should be controlled according to the applicable API specification.
A controlled Nalfurafine API manufacturing process may involve:
Typical Nalfurafine API testing may include:
Store Nalfurafine API in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive heat, moisture and direct light.
Final storage conditions should follow validated stability data and the approved API specification.
Nalfurafine is relevant to research involving:
Nalfurafine is a selective kappa-opioid receptor agonist API with CAS Number 58811-96-4, molecular formula C28H32N2O5, and molecular weight 476.57 g/mol. It is primarily associated with pharmaceutical development for the management of uremic pruritus in patients undergoing hemodialysis and is commonly used as Nalfurafine Hydrochloride.
| Parameter | Specification |
|---|---|
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |