Antinociception produced by the peptidase inhibitor, RB 101, in rats with adrenal medullary transplant into the spinal cord

This study was undertaken to investigate the effects induced by the systemic administration of RB 101 [ N-{( R, S)-2-benzyl-3[( S)(2-amino-4-methylthio)butyl dithio]-1-oxoprpyl}- l-phenylalanine benzyl ester], a mixed inhibitor of the enkephalin catabolism able to cross the blood–brain barrier, in a...

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Bibliographic Details
Published in:European journal of pharmacology 1998-09, Vol.356 (2), p.139-148
Main Authors: Ortega-Alvaro, Antonio, Chover-Gonzalez, Antonio J, Lai-Kuen, René, Mico, Juan A, Gibert-Rahola, Juan, Fournié-Zaluski, Marie-Claude, Roques, Bernard P, Maldonado, Rafael
Format: Article
Language:English
Subjects:
Adrenal Medulla - transplantation
Adrenal medullary transplant
Adrenergic alpha-Antagonists - pharmacology
Analgesics
Analysis of Variance
Animals
Antinociception
Biological and medical sciences
Disulfides - therapeutic use
Enkephalin
Injections, Intravenous
Male
Medical sciences
Naloxone
Naloxone - pharmacology
Narcotic Antagonists - pharmacology
Neuropharmacology
Pain - prevention & control
Pharmacology. Drug treatments
Phentolamine
Phentolamine - pharmacology
Phenylalanine - analogs & derivatives
Phenylalanine - therapeutic use
Protease Inhibitors - therapeutic use
Rats
Rats, Wistar
RB 101
Spinal Cord
Subarachnoid Space
Tail-flick
Transplantation, Autologous
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Summary:This study was undertaken to investigate the effects induced by the systemic administration of RB 101 [ N-{( R, S)-2-benzyl-3[( S)(2-amino-4-methylthio)butyl dithio]-1-oxoprpyl}- l-phenylalanine benzyl ester], a mixed inhibitor of the enkephalin catabolism able to cross the blood–brain barrier, in antinociception produced by adrenal medullary tissue transplanted in the rat spinal subarachnoid space. For this purpose, the antinociceptive responses induced by intravenous (i.v.) administration of RB 101 were evaluated in the tail-flick in rats transplanted 28 and 56 days before the test. Systemic administration of RB 101 induced antinociceptive effects in sham-operated rats, as previously reported. RB 101 also enhanced significantly the antinociception produced by the autotransplant 28 and 56 days after surgery. The antinociceptive responses of RB 101 in both sham-operated and autotransplanted rats were blocked by naloxone, but were not modified by the noradrenergic antagonist, phentolamine, suggesting a selective involvement of opioid mechanisms. The present results indicate that the inhibitors of enkephalin catabolism enhance the antinociception induced by adrenal medullary transplants.
ISSN:0014-2999
1879-0712
DOI:10.1016/S0014-2999(98)00525-1