Cannabinoid type-1 receptor reduces pain and neurotoxicity produced by chemotherapy

J Neurosci. 2012 May 16;32(20):7091-101. doi: 10.1523/JNEUROSCI.0403-12.2012.

Abstract

Painful peripheral neuropathy is a dose-limiting complication of chemotherapy. Cisplatin produces a cumulative toxic effect on peripheral nerves, and 30-40% of cancer patients receiving this agent experience pain. By modeling cisplatin-induced hyperalgesia in mice with daily injections of cisplatin (1 mg/kg, i.p.) for 7 d, we investigated the anti-hyperalgesic effects of anandamide (AEA) and cyclohexylcarbamic acid 3'-carbamoyl-biphenyl-3-yl ester (URB597), an inhibitor of AEA hydrolysis. Cisplatin-induced mechanical and heat hyperalgesia were accompanied by a decrease in the level of AEA in plantar paw skin. No changes in motor activity were observed after seven injections of cisplatin. Intraplantar injection of AEA (10 μg/10 μl) or URB597 (9 μg/10 μl) transiently attenuated hyperalgesia through activation of peripheral CB₁ receptors. Co-injections of URB597 (0.3 mg/kg daily, i.p.) with cisplatin decreased and delayed the development of mechanical and heat hyperalgesia. The effect of URB597 was mediated by CB₁ receptors since AM281 (0.33 mg/kg daily, i.p.) blocked the effect of URB597. Co-injection of URB597 also normalized the cisplatin-induced decrease in conduction velocity of Aα/Aβ-fibers and reduced the increase of ATF-3 and TRPV1 immunoreactivity in dorsal root ganglion (DRG) neurons. Since DRGs are a primary site of toxicity by cisplatin, effects of cisplatin were studied on cultured DRG neurons. Incubation of DRG neurons with cisplatin (4 μg/ml) for 24 h decreased the total length of neurites. URB597 (100 nM) attenuated these changes through activation of CB₁ receptors. Collectively, these results suggest that pharmacological facilitation of AEA signaling is a promising strategy for attenuating cisplatin-associated sensory neuropathy.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Activating Transcription Factor 3 / metabolism
  • Animals
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / antagonists & inhibitors
  • Arachidonic Acids / pharmacokinetics
  • Arachidonic Acids / pharmacology
  • Arachidonic Acids / therapeutic use*
  • Benzamides / antagonists & inhibitors
  • Benzamides / pharmacology
  • Benzamides / therapeutic use*
  • Cannabinoid Receptor Modulators / pharmacokinetics
  • Cannabinoid Receptor Modulators / pharmacology
  • Cannabinoid Receptor Modulators / therapeutic use
  • Carbamates / antagonists & inhibitors
  • Carbamates / pharmacology
  • Carbamates / therapeutic use*
  • Cells, Cultured
  • Cisplatin / adverse effects
  • Cisplatin / antagonists & inhibitors*
  • Disease Models, Animal
  • Drug Interactions
  • Endocannabinoids
  • Enzyme Inhibitors / pharmacology
  • Enzyme Inhibitors / therapeutic use
  • Ganglia, Spinal / drug effects
  • Ganglia, Spinal / metabolism
  • Hyperalgesia / chemically induced
  • Hyperalgesia / drug therapy*
  • Male
  • Mice
  • Mice, Inbred C3H
  • Morpholines / pharmacology
  • Motor Activity / drug effects
  • Neurites / drug effects
  • Neurotoxicity Syndromes / drug therapy*
  • Peripheral Nervous System Diseases / chemically induced
  • Peripheral Nervous System Diseases / drug therapy*
  • Polyunsaturated Alkamides / pharmacokinetics
  • Polyunsaturated Alkamides / pharmacology
  • Polyunsaturated Alkamides / therapeutic use*
  • Pyrazoles / pharmacology
  • Receptor, Cannabinoid, CB1 / agonists*
  • TRPV Cation Channels / metabolism

Substances

  • Activating Transcription Factor 3
  • Antineoplastic Agents
  • Arachidonic Acids
  • Atf3 protein, mouse
  • Benzamides
  • Cannabinoid Receptor Modulators
  • Carbamates
  • Endocannabinoids
  • Enzyme Inhibitors
  • Morpholines
  • Polyunsaturated Alkamides
  • Pyrazoles
  • Receptor, Cannabinoid, CB1
  • TRPV Cation Channels
  • TRPV1 protein, mouse
  • cyclohexyl carbamic acid 3'-carbamoylbiphenyl-3-yl ester
  • Cisplatin
  • AM 281
  • anandamide