Inactivation of dynorphin-(1-8) in isolated preparations by three peptidases.
スポンサーリンク
概要
- 論文の詳細を見る
Inactivation of dynorphin-(1-8) in three in vitro isolated preparations, guinea-pig ileum, mouse vas deferens and rabbit vas deferens, was estimated by employing the relatively specific inhibitors of enkephalin-hydrolyzing enzymes. All three enzyme inhibitors, amastatin, captopril and phosphoramidon, significantly enhanced the inhibitory potency of dynorphin-(1-8) in the three isolated preparations. The magnitude of the enhancement of the dynorphin potency by captopril was significantly higher than that by either amastatin or phosphoramidon in guinea-pig ileum; that by amastatin was significantly higher than that by either captopril or phosphoramidon in rabbit vas deferens; and that by amastatin was similar to that by captopril, but significantly higher than that by phosphoramidon in mouse vas deferens. The K<SUB>e</SUB> values of three antagonists, naloxone, Mr 2266 and ICI 154129, against dynorphin-(1-8) in the presence of the three peptidase inhibitors indicated that dynorphin-(1-8) acted on kappa receptors in guinea-pig ileum and on both kappa and delta receptors in mouse vas deferens. Since amastatin, captopril and phosphoramidon produced the naloxone-reversible inhibition of contractions of guinea-pig ileum in the presence of dynorphin-(1-8), all three dynorphin-inactivating enzymes were indicated to be located very close to kappa receptors.
著者
-
OKA Tetsuo
Department of Pharmacology, School of Medicine, Tokai University
-
OKA Tetsuo
Department of Clinical Pharmacology, School of Medicine, Tokai University
-
NUMATA Hiroaki
Department of Pharmacology, Preclinical Research Laboratories, Central Institute for Experimental Animals
-
HIRANUMA Toyokazu
Department of Pharmacology, School of Medicine, Tokai University
関連論文
- Stimulus effects of the medial pontine reticular formation and the mesencephalic locomotor region upon medullary reticulospinal neurons in acute decerebrate cats
- Great Increase in Antinociceptive Potency of [Leu^5]Enkephalin After Peptidase Inhibition
- The Enhancing Effects of Peptidase Inhibitors on the Antinociceptive Action of [Met^5]Enkephalin-Arg^6-Phe^7 in Rats
- Time Course of Changes in μ-Opioid Receptor mRNA Levels in the Periaqueductal Gray of Rat Brain by a Single or Repeated Injections of Antisense Oligodeoxynucleotides
- Long-Term Treatment With Morphine Increases the D-Serine Content in the Rat Brain by Regulating the mRNA and Protein Expressions of Serine Racemase and D-Amino Acid Oxidase
- Effects of Peptidase Inhibitors on the Enkephalin-Induced Anti-nociception in Rats
- Effects of Fusaric (5-butylpicolinic) Acid on the Monosynaptic Reflex Neural Activity of Cat Spinal Cord
- Effects of Peripheral Monoamines on the Monosynaptic Reflex Neuronal Activity of Acute Spinal Cats
- Effects of Muscarinic Cholinergic Antagonists or p-Chlorophenylalanine on the Morphine-Induced Increase in Striatal Homovanillic Acid Concentration of Rats
- Effects of 5, 7-Dihydroxytryptamine on Brain Monoamine Contents and on Morphine-Induced Hypothermia in Rats
- 117. INFLUENCE OF 4-WEEK SIMULTANEOUS ORAL ADMINISTRATION OF DIFENAMIZOLE AND OTHER DRUGS ON LIVER FUNCTION OF RATS (The Third Meeting for the Study of Toxic Effect)
- New μ-Opioid Receptor Agonists with Phenoxyacetic Acid Moiety
- New μ-Opioid Receptor Agonists with Piperazine Moiety
- The Effect of Naloxone on C-Fiber Reflex in Cats
- EFFECTS OF NARCOTIC ANALGESICS ON SEROTONIN METABOLISM IN BRAIN OF RATS AND MICE
- The Effects of Morphine, Naloxone and Capsaicin on C-fiber Reflex and Heat Evoked Discharge in Acute Spinal Cats
- EFFECT OF HUMORAL MODULATORS ON MORPHINEINDUCED INCREASE IN LOCOMOTOR ACTIVITY OF MICE
- The Effect of Capsaicin on C-fiber Reflex and Heat Evoked Discharge in the Acute Spinal Cat
- The Effects of Droperidol and Diazepam on the Neural Excitation of Ketamine Hydrochloride
- THEBAINE METABOLITES IN THE URINE OF RHESUS MONKEYS
- Two New Opioid Delta-Receptor Ligands: A Highly Selective Agonist and a Potent Selective Antagonist in in Vitro Isolated Preparations
- Long-Term Treatment With Morphine Increases the D-Serine Content in the Rat Brain by Regulating the mRNA and Protein Expressions of Serine Racemase and D-Amino Acid Oxidase
- Characteristics of Opioid Receptors in Guinea-Pig Cerebellum and Human Placenta
- Relation of Diltiazem Binding Sites to Opioid Receptor Subtypes in the Guinea-pig Brain
- Human Serum Dopamine-β-hydroxylase Activity as a Marker of Sympathoadrenal Activity
- Inactivation of dynorphin-(1-8) in isolated preparations by three peptidases.
- Estimation of relative importance of three enzymes in the inactivation of (Met5)-enkephalin and (Met5)-enkephalin-Arg6 in three isolated preparations by employing the inhibitor specific for each enzyme.
- Agonist and antagonist actions of buprenorphine on three types of opioid receptor in isolated preparations.
- The inactivation of (Met5)-enkephalin by bestatin-sensitive aminopeptidase, captopril-sensitive peptidyl dipeptidase A and thiorphan-sensitive endopeptidase-24.11 in mouse vas deferens.
- The relative potency of enkephalins and .BETA.-endorphin in guinea-pig ileum, mouse vas deferens and rat vas deferens after the administration of peptidase inhibitors.
- The enhancing effects of amastatin, phosphoramidon and captopril on the potency of (Met5)-enkephalin in rat vas deferens.
- Regulation of opioid antagonist and mu, kappa or delta agonist binding by guanine nucleotide and sodium.
- The Enhancing Effects of Peptidase Inhibitors on the Antinociceptive Action of [Met5]Enkephalin-Arg6-Phe7 in Rats
- The role of bestatin-sensitive aminopeptidase, angiotensin converting enzyme and thiorphan-sensitive "enkephalinase" in the potency of enkephalins in the guinea-pig ileum.
- Effects of peptidase inhibitors on the (Met5)-enkephalin hydrolysis in ileal and striatal preparations of guinea-pig: Almost complete protection of degradation by the combination of amastatin, captopril and thiorphan.
- SIMPLE, SENSITIVE AND RAPID METHODS FOR THE DETECTION OF MORPHINE IN URINE