152657-84-6
152657-84-6 structure
- Name: Nalfurafine
- Chemical Name: (E)-N-[(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-7-yl]-3-(furan-3-yl)-N-methylprop-2-enamide
- CAS Number: 152657-84-6
- Molecular Formula: C28H32N2O5
- Molecular Weight: 476.56400
- Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
- Create Date: 2017-02-09 19:16:17
- Modify Date: 2025-08-27 15:19:47
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Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential[1]. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment[2].
| Name | (E)-N-[(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-7-yl]-3-(furan-3-yl)-N-methylprop-2-enamide |
|---|---|
| Synonyms |
Nalfurafine
(E)-N-(17-(cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxymorphinan-6beta-yl)-3-(furan-3-yl)-N-methylprop-2-enamide TRK 820 (2E)-N-[(5R,6R)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(furan-3-yl)-N-methylprop-2-enamide TRK-820 free base |
| Description | Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential[1]. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment[2]. |
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| Related Catalog | |
| Target |
IC50: kappa opioid receptor (KOR)[1] |
| In Vivo | Nalfurafine (subcutaneous injection; 0.015 mg/kg) combines with EOM-salvinorin-B produces spinal antinociception equivalent to 5 mg/kg, it also enhances the supraspinal analgesic effect of 5 mg/kg morphine[1]. Nalfurafine (subcutaneous injection; 4 μg/kg) causes a dose-dependent increase of the inhibition of the acetic acid-induced abdominal constriction,and the inhibition of the abdominal constriction reaches its peak 30 min after injection, gradually declined and returned to the preinjection level 4 hr after[2]. Animal Model: Male and Female C57BL/6J mice[1] Dosage: 0.015 mg/kg Administration: Subcutaneous injection Result: Had the potential for enhancing the therapeutic potential of MOR-targeting analgesics, such as morphine. |
| References |
| Density | 1.41g/cm3 |
|---|---|
| Boiling Point | 700.7ºC at 760mmHg |
| Molecular Formula | C28H32N2O5 |
| Molecular Weight | 476.56400 |
| Flash Point | 377.6ºC |
| Exact Mass | 476.23100 |
| PSA | 86.38000 |
| LogP | 3.02760 |
| Vapour Pressure | 1.3E-20mmHg at 25°C |
| Index of Refraction | 1.696 |
