Literature DB >> 3030776

Evaluation of the supraspinal analgesic activity and abuse liability of ethylketocyclazocine.

E Unterwald, S Sasson, C Kornetsky.   

Abstract

Rats were trained to escape from aversive electrical brain stimulation delivered to the midbrain reticular formation (MRF) or to obtain rewarding intracranial stimulation delivered to the medial forebrain bundle (MFB). The threshold for escape behavior was determined by a modification of the psychophysical method of limits. Likewise, reward thresholds were determined by a rate-free psychophysical method. Acute administration of ethylketocyclazocine (EKC) (0.06-1.0 mg/kg s.c.) raised escape threshold in a dose-dependent manner while having no effect on non-specific measures of sedation or motor impairment. This suggests that opioids with kappa receptor activity specifically modulate pain at a supraspinal level. Administration of EKC had no effect on the threshold for rewarding intracranial stimulation to the MFB suggesting that EKC has low potential for abuse.

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Year:  1987        PMID: 3030776     DOI: 10.1016/0014-2999(87)90023-9

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN: 0014-2999            Impact factor:   4.432


  4 in total

1.  Medial forebrain stimulation enhances intracranial nociception and attenuates morphine analgesia suggesting the existence of an endogenous opioid antagonist.

Authors:  Conan Kornetsky; Clifford M Knapp; Lisa Tozier; Arlene Pak
Journal:  Pharmacol Biochem Behav       Date:  2010-02-10       Impact factor: 3.533

2.  Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.

Authors:  K Yasuda; K Raynor; H Kong; C D Breder; J Takeda; T Reisine; G I Bell
Journal:  Proc Natl Acad Sci U S A       Date:  1993-07-15       Impact factor: 11.205

Review 3.  Kappa opioids and the modulation of pain.

Authors:  Bronwyn Kivell; Thomas E Prisinzano
Journal:  Psychopharmacology (Berl)       Date:  2010-04-07       Impact factor: 4.530

4.  kappa-Opioid agonists produce antinociception after i.v. and i.c.v. but not intrathecal administration in the rat.

Authors:  G E Leighton; R E Rodriguez; R G Hill; J Hughes
Journal:  Br J Pharmacol       Date:  1988-03       Impact factor: 8.739

  4 in total

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