Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P01189 (beta-endorphin)
 21,003 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

An in vitro model system for analysis of presynaptic inhibitory actions of spinal opioids has been applied. Embryonic sensory neurons derived from chick dorsal root ganglia were grown in primary cell culture, and the release of substance P was evoked by electrical field stimulation during exposure to drugs with well-demonstrated affinity for opioid receptors. This allowed a pharmacologic characterization of the inhibitory actions of specific opioid agonists on the release of substance P as measured by radioimmunoassay (RIA). Sufentanil (0.5 microM), a high affinity mu receptor agonist, U-50,488H (25 microM), a selective kappa receptor agonist, and morphine (10 microM), an agonist with high affinity for mu and delta receptors, inhibited the evoked release of substance P by approximately 60%, 40%, and 50%, respectively. For sufentanil the response was demonstrated to be dose-dependent. As is the case for its analgesic action in vivo, morphine was approximately 50-fold less potent than sufentanil on a molar basis in this assay. The actions of sufentanil, U-50-488H and morphine were mimicked by the endogenous opioid peptide met-enkephalin, and its stable synthetic analog D-ala2-met5-enkephalinamide (DAME). Naloxone (25 microM), an opioid receptor antagonist, blocked the inhibitory action of sufentanil (0.5 microM), morphine (5 microM), and DAME (5 microM), but not U-50,488H (10 microM). The action of U-50,488H was partially blocked by the antagonist naltrexone (25 microM). Stereo-selectivity of agonist action was confirmed by the failure of dextrorphan (50 microM), an inactive opioid isomer, to inhibit the release of substance P.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Sufentanil, morphine, met-enkephalin, and kappa-agonist (U-50,488H) inhibit substance P release from primary sensory neurons: a model for presynaptic spinal opioid actions. 246 89

This pilot study examined the safety and efficacy of sufentanil in the ventilated neonate. Informed parental consent for study participation was obtained for eight infants who were admitted to the neonatal intensive care unit and required analgesic/sedative therapy as part of their medical management to support mechanical ventilation. An intravenous loading dose (0.2 microgram/kg) was administered over 20 minutes, followed by a continuous infusion (0.05 microgram/kg/hour). Whole blood samples were collected prior to onset of sufentanil therapy, immediately following the loading dose, and 24 hours after the start of the continuous sufentanil infusion for analysis of beta-endorphin and sufentanil serum content. Heart rate, respiratory rate, and blood pressure were recorded as a routine part of medical management. The ventilatory efficiency index (VEI) and ventilation index (VI) were calculated before and after sufentanil therapy. Four male and four female infants were admitted to this study; the mean gestational age was 37 weeks, and weight was 2,970 gm. Sufentanil therapy appeared to be well tolerated, as evidenced by a lack of nursing observations noting changes in heart rate or mean arterial pressure. VEI values increased in four subjects, and VI values decreased in six subjects. Overall, the mean increase in VEI was 19 percent; the decrease in VI was 27 percent. The beta-endorphin serum content decreased in all subjects, and nurses did not report any signs of patient discomfort. Serum sufentanil content was undetectable. Sufentanil appears to be a suitable agent to provide analgesia/sedation in the neonatal patient under the experimental conditions of this study.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Safety and efficacy of sufentanil therapy in the ventilated infant. 800 23