An assessment of the antinociceptive efficacy of intrathecal and epidural Contulakin-G in rats and dogs

Contulakin-G is a novel conopeptide with an incompletely defined mechanism of action. To assess nociceptive activity we delivered Contulakin-G as a bolus intrathecally (0.03, 0.1, 0.3, 3 nmol) or epidurally (10, 30, 89 nmol) in rats. Intrathecal Contulakin G significantly decreased Phase II and, to...

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Published inAnesthesia and analgesia Vol. 104; no. 6; pp. 1505 - 1513
Main Authors ALLEN, Jeffrey W, HOFER, Katrin, MCCUMBER, Damon, WAGSTAFF, John D, LAYER, Richard T, MCCABE, R. Tyler, YAKSH, Tony L
Format Journal Article
LanguageEnglish
Published Hagerstown, MD Lippincott 01.06.2007
Subjects
Analgesia, Epidural
Analgesics - administration & dosage
Anesthesia
Anesthesia. Intensive care medicine. Transfusions. Cell therapy and gene therapy
Animals
Biological and medical sciences
Dogs
Glycoproteins - administration & dosage
Injections, Spinal
Male
Medical sciences
Neuropeptides - administration & dosage
Pain Measurement - drug effects
Rats
Rats, Sprague-Dawley
Extradural
Fissipedia
Carnivora
Vertebrata
Mammalia
Rat
Animal
Rodentia
Anesthesia
Dog
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Summary:Contulakin-G is a novel conopeptide with an incompletely defined mechanism of action. To assess nociceptive activity we delivered Contulakin-G as a bolus intrathecally (0.03, 0.1, 0.3, 3 nmol) or epidurally (10, 30, 89 nmol) in rats. Intrathecal Contulakin G significantly decreased Phase II and, to a lesser degree, Phase I paw flinching produced by intradermal formalin. Intrathecal and epidural doses of ED50s were 0.07 nmol and 45 nmol, respectively, giving an epidural/intrathecal ED50 ratio = 647). In dogs, intrathecal Contulakin-G (50-500 nmoL) produced a dose-dependent increase in the thermally evoked skin twitch latency by 30 min after administration, as did morphine (150 and 450 nmol). Epidural morphine (750 and 7500 nmol), but not epidural 1000 nmol Contulakin-G, also significantly decreased skin twitch in dogs. No changes in motor function were seen in any rats or dogs receiving these doses of Contulakin-G. In dogs, no physiologically significant dose-dependent changes in motor function, heart rate, arterial blood pressure, or body temperature were found. Contulakin-G is a potent antinociceptive drug when delivered intrathecally with no observable negative side effects in rats or dogs and may provide an alternative to opioid spinal analgesics.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0003-2999
1526-7598
DOI:10.1213/01.ANE.0000219586.65112.FA