title: A single intravenous injection of KRN5500 (antibiotic spicamycin) produces long-term decreases in multiple sensory hypersensitivities in neuropathic pain.
abstract: Neuropathic pain is a significant clinical problem. Currently, there are no drugs that produce complete amelioration of this type of pain. We have previously shown that KRN5500, a derivative of the antibiotic spicamycin, produces a prolonged (7-day), and significant reduction in neuropathic pain, but not nociceptive pain. Herein, we provide further evidence for the efficacy of this drug in inhibiting pain after IV injection in a spared nerve injury model of neuropathic pain. A single IV dose of the drug produces an increase in pain thresholds to punctuate mechanical stimuli and to cold stimuli over a period of 7 days, whereas IV injection of the vehicle is without any effect. No change in pain threshold was observed in the contralateral foot. In addition, a significant antiallodynic effect to mechanical stimuli was observed at 1, 2, 4, and 6 wk. The drug may be a potential candidate for cancer-related neuropathic pain as well as a marker for discovery of effective analgesics for neuropathic pain.
  
  
  CONCLUSIONS
  We examined the effect of a novel drug (KRN5500) on nerve damage pain. After the successful effects of this drug in a single human, we have shown that the drug infused as a single application at different doses in a rat model of nerve damage pain produces pain relief in this model for many weeks.
authors.affiliation: Department of Radiology, Center for Functional Pain Neuroimaging and Therapy Research, Charlestown, Massachusetts 02129, USA.
authors.forename: L A
authors.initials: LA
authors.lastname: Kobierski
authors.forename: S
authors.initials: S
authors.lastname: Abdi
authors.forename: L
authors.initials: L
authors.lastname: DiLorenzo
authors.forename: N
authors.initials: N
authors.lastname: Feroz
authors.forename: D
authors.initials: D
authors.lastname: Borsook
mesh_terms: D000818:Animals; D003080:Cold Temperature; D006930:Hyperalgesia / Q000503:physiopathology; D008297:Male; D009475:Neurons, Afferent / Q000187:drug effects* / Q000473:pathology; D010146:Pain / Q000188:drug therapy* / Q000473:pathology; D017288:Pain Threshold / Q000187:drug effects; D010523:Peripheral Nervous System Diseases / Q000188:drug therapy* / Q000473:pathology; D010812:Physical Stimulation; D011684:Purine Nucleosides / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D015430:Weight Gain / Q000187:drug effects
chemical_list: D011684:Purine Nucleosides; C092296:KRN 5500