Pharmacology and clinical experience with fedotozine

Expert Opinion on Investigational Drugs

Volumn 10, Issue 1, 2001, Pages 97-110

  Delvaux, M ^a  

^a CHU RANGUEIL   (France)

Author keywords

Opioid receptors; Abdominal pain; Fedotozine; Functional digestive disorders; Opiates; Opioid receptors; Visceral sensitivity

Indexed keywords

3,4 DICHLORO N METHYL N [2 (1 PYRROLIDINYL)CYCLOHEXYL]BENZENEACETAMIDE METHANESULFONATE; 5,9 DIETHYL 2 (3 FURYLMETHYL) 2' HYDROXY 6,7 BENZOMORPHAN; ACETAMIDE DERIVATIVE; ACETIC ACID; ANTINOCICEPTIVE AGENT; CALCIUM ION; FEDOTOZINE; FENTANYL; FREUND ADJUVANT; KAPPA 1 OPIATE RECEPTOR; KAPPA OPIATE RECEPTOR; KAPPA OPIATE RECEPTOR AGONIST; KAPPA OPIATE RECEPTOR ANTAGONIST; MORPHINE; MU OPIATE RECEPTOR; N METHYL N [2 (1 PYRROLIDINYL)CYCLOHEXYL]BENZO[B]THIOPHENE 4 ACETAMIDE; NALOXONE; NEUROTRANSMITTER; NORBINALTORPHIMINE; PLACEBO; PROTEIN C FOS; RECEPTOR SUBTYPE; SIGMA OPIATE RECEPTOR; SODIUM CHLORIDE; UNCLASSIFIED DRUG;

ABDOMINAL PAIN; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINOCICEPTION; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DIGESTIVE SYSTEM FUNCTION DISORDER; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG CONFORMATION; DRUG EFFECT; DRUG METABOLISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DYSPEPSIA; ENTERITIS; FEMALE; GASTROINTESTINAL TOXICITY; HEADACHE; HUMAN; ILEUS; INTESTINE DISTENSION; INTESTINE INNERVATION; IRRITABLE COLON; MAJOR CLINICAL STUDY; MALE; NOCICEPTION; NOCICEPTIVE STIMULATION; NONHUMAN; PERITONITIS; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; PHASE 3 CLINICAL TRIAL; POSTOPERATIVE COMPLICATION; RANDOMIZED CONTROLLED TRIAL; RECEPTOR AFFINITY; STOMACH ULCER; VERTIGO;

ANIMALS; BENZYL COMPOUNDS; COLONIC DISEASES, FUNCTIONAL; DYSPEPSIA; GASTROINTESTINAL MOTILITY; HUMANS; PAIN; PROPYLAMINES; RECEPTORS, OPIOID, KAPPA;

EID: 0035190470     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543784.10.1.97     Document Type: Article

References (56)

1. The functional gastrointestinal disorders and the Rome II process
2. Fundamentals of neurogastroenterology
3. Principles of applied neurogastroenterology: Physiology/motility-sensation
4. Mediators and pharmacology of visceral sensitivity: From basic to clinical investigations
5. International Union of Pharmacology. XII. Classification of opioid receptors
6. Interaction of trimebutine and JO-1196 (fedotozine) with opioid receptors in the canine ileum
7. Opposite effects of κ-opioid agonists on gastric emptying of liquids and solids in dogs
8. Action of opiates on gastrointestinal function
9. Effects of fedotozine on gastrointestinal motility in dogs: Mechanism of action and related pharmacokinetics
10. The contractile effect of fedotozine on guinea-pig isolated intestinal cells is not mediated by κ-opioid receptors
11. Effects of selective opioid agonists on feline colonic transit
12. Intestinal sensitivity in healthy volunteers: A pilot study of the action of fedotozine
13. Double-blind controlled study of the activity of fedotozine administered by the iv. and intragastric routes, on intestinal motility and transit time in the healthy subject
14. The κ-agonist fedotozine relieves hypersensitivity to colonic distension in patients with irritable bowel syndrome (IBS)
15. Antagonism of stress-induced gastric motor alteration and plasma cortisol by fedotozine (JO-1196) in dogs
16. Fedotozine reverses ileus induced by surgery or peritonitis: Action at peripheral κ-opioid receptors
17. Effects of mu and κ-opioid receptors on post-operative ileus in rats
18. Effects of fedotozine on gastric emptying and upper gastrointestinal symptoms in diabetic gastroparesis
19. Effect of fedotozine on symptoms and delayed gastric emptying in functional dyspeptic patients
20. Prostaglandin hyperalgesia. II: The peripheral analgesic activity of morphine, enkephalins and opioid antagonists
21. Opioid analgesia at peripheral sites: A target for opioids released during stress and inflammation
22. Intrinsic mechanisms of antinociception in inflammation: Local opioid receptors and β-endorphin
23. Peripheral opioid receptors mediating antinocicieption in inflammation. Evidence for involvement of μ-, δ- and κ-receptors
24. Inflammation of the paw enhances axonal transport of opioid receptors in the sciatic nerve and increases their density in the inflamed tissue
25. Axonal transport of opiate receptors in capsaicin-sensitive nerves
26. Effect of κ-opioid receptors on mechanosensitive pelvic nerve afferent fibers innervating the colon of the rat
27. Effect of κ opioids in the inflamed rat colon
28. Peripheral κ-opioid receptors mediate the antinociceptive effect of fedotozine on the duodenal pain reflex in rat
29. Role of vagal afferents in the antinociception produced by morphine and U50,488H in the colonic pain reflex in rats
30. κ-Opioid receptors agonists differentially inhibit two classes of rat spinal neurons, excited by colorectal distension
31. κ- But not μ- or δ-opioids attenuate responses to distension of afferent fibers innervating the rat colon
32. Mechanical activation of dorsal root ganglion cells in vitro: Comparison with capsaicin and modulation by κ-opioids
33. Animal models of intestinal inflammation
34. Fedotozine reversal of peritoneal irritation-induced ileus in rats: Possible peripheral action on sensory afferents
35. Fedotozine blocks hypersensitive visceral pain in conscious rats: Action at peripheral κ-opioid receptors
36. Effect of opioid active therapeutics on the ascending reflex pathway in the rat ileum
37. Fedotozine relieves visceral pain by acting through peripheral κ-receptors. Increased potency during inflammation induced hyperalgesia in rats
38. Effect of fedotozine on the cardiovascular pain reflex induced by distension of the irritated colon in the anaesthetized rat
39. The κ-agonist fedotozine modulates colonic distension-induced inhibition of gastric motility and emptying in dogs
40. Stimulation of κ opiate receptors in intestinal wall affects stress-induced increase of plasma cortisol in dogs
41. Vagally mediated inhibition of acoustic stress involved cortisol release by orally administered κ opioid substances in dogs
42. Neuronal pathways involved in abdominal surgery-induced gastric ileus in rats
43. Fedotozine, a κ-opioid agonist, prevents spinal and supra-spinal Fos expression induced by a noxious visceral stimulus in the rat
44. Effect of the κ agonist fedotozine on perception of gastric distension in healthy humans
45. Effects of rectal distensions on nociceptive flexion reflexes in humans
46. Pain from distension of the pelvic colon by inflating a balloon in the irritable colon syndrome
47. Evidence for the hypersensitivity of lumbar splanchnic afferents in irritable bowel syndrome
48. The effect of sleep deprivation on gastric emptying and food intake in healthy volunteers: Action of fedotozine
49. The effects of sleep deprivation on rectal sensitivity in healthy volunteers
50. Human pharmacokinetic studies of fedotozine
51. Double-blind dose-response multicenter comparison of fedotozine and placebo in treatment of non-ulcer dyspepsia
52. Efficacy and safety of the peripheral κ agonist fedotozine versus placebo in the treatment of functional dyspepsia
53. Efficacy of peripheral κ-agonist fedotozine versus placebo in treatment of Irritable Bowel Syndrome. A multicenter dose-response study
54. Differential effects of fedotozine compared to other κ-agonists on diuresis in rats
55. The discriminative stimulus properties of U50,488 and morphine are not shared by fedotozine
56. Fedotozine reversion of digestive motility disturbances in ileus. Action on sensory pathways through peripheral kappa receptors