Disease relevance of FEDOTOZINE

• The kappa agonist fedotozine relieves hypersensitivity to colonic distention in patients with irritable bowel syndrome [1].
• CONCLUSION: Fedotozine reverses experimental ileus via an action at peripheral kappa-opioid receptors [2].
• Fedotozine seems capable of reversing visceral hypersensitivity observed in these patients and could have some beneficial action on their symptoms [1].
• Fedotozine reverses ileus induced by surgery or peritonitis: action at peripheral kappa-opioid receptors [2].
• Efficacy and safety of the peripheral kappa agonist fedotozine versus placebo in the treatment of functional dyspepsia [3].

Psychiatry related information on FEDOTOZINE

• Once trained, rats were used to conduct tests of stimulus generalization with morphine, U50,488 and fedotozine along with another kappa agonist, CI-977, and another mu agonist, fentanyl [4].

High impact information on FEDOTOZINE

• Fedotozine had additional inhibitory effects acting within the spinal cord [5].
• AIMS: To evaluate, in a large multicentre trial, the use of the kappa receptor agonist fedotozine to improve symptoms associated with functional dyspepsia [3].
• CONCLUSIONS: Fedotozine has no effect on gastric emptying in patients with diabetic gastroparesis [6].
• AIM: To evaluate the effects of fedotozine on gastric emptying and gastrointestinal symptoms in diabetic gastroparesis [6].
• When administered in the lateral ventricle of the brain, U-50,488h and dynorphin A(1-17) induced water diuresis, unlike fedotozine (100 micrograms), DYN A(1-13) and DYN B(1-13) that had no effect on urine output [7].

Chemical compound and disease context of FEDOTOZINE

• Opiates, including morphine as well as compounds such as trimebutine or fedotozine designed for therapeutic use in irritable bowel syndrome, are effective in reducing visceral nociception [8].
• The CRF effects were blocked by alpha-helical-CRF9-41 (10 nmol/rat) given i.c. but not i.v. Fedotozine (1-10 mg/kg s.c. but not 300 micrograms/rat i.c.v. or intrathecally) and (+/-)U-50,488H (0.3-3 mg/kg s.c. but not 100 micrograms/kg i.c.v.) reversed PI- but not CRF-induced ileus [9].

Biological context of FEDOTOZINE

• Differential effects of fedotozine compared to other kappa agonists on diuresis in rats [7].
• Effects of fedotozine on gastric emptying and upper gastrointestinal symptoms in diabetic gastroparesis [6].
• Competition of [3H]U69,593 binding to the KOR by bremazocine, alpha-neoendorphin, fedotozine and oxymorphindole resolved a single class of binding sites at which these agents had binding affinities similar to that of the kappa 1b site present in mouse brain [10].
• Effects of fedotozine on gastrointestinal motility in dogs: mechanism of action and related pharmacokinetics [11].
• Between 1 to 5 mg kg-1, fedotozine exhibited a sustained and potent stimulatory effect on the small intestine inducing 1 to 4 phases III of the migrating motor complex (MMC) lasting up to 32 min in the duodenum and migrating to the jejunum [11].

Anatomical context of FEDOTOZINE

• CONCLUSION: Fedotozine decreases gastric sensitivity to distension by exerting specific action on gastric afferent pathways [12].
• The effects of fedotozine, (+)-(1R)-1-phenyl-1-[(3,4,5-trimethoxy)benzyloxymethyl]-N,N-dim eth yl- n-propylamine, on motility of the antrum and small intestine were investigated in dog [11].
• These results indicate that fedotozine can have direct excitatory effects on intestinal smooth muscle cells from the guinea pig ileum not mediated by activation of kappa opioid receptors [13].
• The compound fedotozine, recently described as a peripheral kappa opioid receptor agonist, was tested on smooth muscle cells isolated from the longitudinal muscle layer of the guinea pig ileum, in comparison with the selective kappa receptor agonist, compound U-50488 [13].
• The kappa receptor agonist fedotozine exerts its antinociceptive effect by acting on peripheral nerve endings of sensory vagal and nonvagal afferent pathways [14].

Associations of FEDOTOZINE with other chemical compounds

• In colonic strips incubated with [3H]-choline, fedotozine (10(-5)-10(-4) M) induced an erratic decrease of acetylcholine-release induced by electric stimulation [15].

Gene context of FEDOTOZINE

• The aims of this study were: to map, in conscious rats, central pathways activated by AA using Fos as a marker of neuronal activation; to characterize primary afferent fibres involved in this activation; and to investigate the effect of fedotozine on AA-induced Fos expression [16].
• Since altered visceral perception is thought to play an important role in the genesis of abdominal pain and bloating in many patients with IBS, new drugs are targeted at modulating the sensitivity, such as 5HT3 antagonists (e.g. alosetron), kappa-agonists (e.g. fedotozine) and somatostatin analogues [17].

Analytical, diagnostic and therapeutic context of FEDOTOZINE

• However, naloxone prevented the effect of morphine on the transit after skin incision and of fedotozine on the laparotomy plus manipulation [18].
• The aim of the study was to evaluate the discriminative stimulus effects of fedotozine at doses previously reported to produce maximal effects in in vivo assays measuring kappa-mediated analgesia [4].
• Fedotozine, a kappa (kappa) opioid receptor agonist, has been tried as a visccral analgesic in various clinical trials with conflicting results [19].
• Following oral administration, fedotozine at 2.5 and 5 mg kg-1 constantly stimulated both antrum and small intestinal motility [11].

References