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BUTORPHANOL
BUTORPHANOL
- CAS:
- 42408-82-2
- MF:
- C21H29NO2
- MW:
- 327.46
Properties
- Melting point:
- 215-217°
- alpha
- D -70.0° (c = 0.1 in methanol)
- Boiling point:
- 507.3±50.0 °C(Predicted)
- Density
- 1.24±0.1 g/cm3(Predicted)
- pka
- pKa 8.6 (Uncertain)
Safety Information
Use
Structurally, butorphanol is a morphinan and shares the samecyclobutyl methyl group on the nitrogen as nalbuphine. Likenalbuphine, butorphanol is an agonist at the κ-receptor but atthe μ-receptor butorphanol is both a partial agonist and anantagonist. The affinity for opioid receptors in vitro is1:4:25 for the μ-, δ-, and κ-receptors respectively. Thehigh affinity for the κ-receptors is proposed to give butorphanolits analgesic properties and is also responsible for theCNS adverse effects such as hallucinations, psychosis, andparanoid reactions. Butorphanol binds with μ-receptors as apartial agonist, and administration to humans maintained onhigh-potency μ-agonists such as morphine may precipitatewithdrawal. Butorphanol was found to produce convulsionsin morphine-deprived, morphine-dependent monkeys.
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