title: Inhibition of urinary bladder motility by a spinal action of U-50488H in rats.
abstract: We examined the effect of a kappa agonist, U-50488H, upon the bladder motility of anaesthetized rats. The frequency of distension-induced rhythmic bladder contractions was reduced by the intravenous (10 mg kg(-1)) or intrathecal (10-100 microg) administration of U-50488H. The effect of intravenous U-50488H was inhibited by pre-treatment with nor-binaltorphimine (10 mg kg(-1), s.c.). The inhibition of bladder contractions by intrathecal U-50488H (30 microg) was eliminated with the concomitant use of nor-binaltorphimine (10 mg kg(-1), s.c.), and diminished by reserpine (4 mg kg(-1), i.p.), yohimbine (10 microg, i.t.) or methysergide (20 microg, i.t.). The amplitude of bladder contractions induced by an electrical stimulation of the pontine micturition centre was not inhibited by intrathecal U-50488H (30 and 100 microg). These results suggested that a kappa agonist could inhibit micturition reflex as well as other opioids, and at least part of the inhibition was due to the diminishment of bladder sensation based on the activation of the descending monoaminergic systems through the spinal kappa-opioid receptors.
authors.affiliation: Division of Urology, Department of Organs Therapeutics, Faculty of Medicine, Kobe University Graduate School of Medicine, 7-5-2 Kusunoki-cho, Chuo-ku, Kobe, Hyogo 650-0017, Japan. gotoh@med.kobe-u.ac.jp
authors.forename: Akinobu
authors.initials: A
authors.lastname: Gotoh
authors.forename: Kazuhiro
authors.initials: K
authors.lastname: Goto
authors.forename: Atsushi
authors.initials: A
authors.lastname: Sengoku
authors.forename: Toshiro
authors.initials: T
authors.lastname: Shirakawa
authors.forename: Yoshinobu
authors.initials: Y
authors.lastname: Akao
authors.forename: Masato
authors.initials: M
authors.lastname: Fujisawa
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Okada
authors.forename: Soichi
authors.initials: S
authors.lastname: Arakawa
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Sasaki
authors.forename: Sadao
authors.initials: S
authors.lastname: Kamidono
mesh_terms: D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer / Q000494:pharmacology*; D018759:Adrenergic Uptake Inhibitors / Q000494:pharmacology; D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology; D000818:Animals; D019540:Area Under Curve; D004305:Dose-Response Relationship, Drug; D004558:Electric Stimulation; D007275:Injections, Intravenous; D007278:Injections, Spinal; D008297:Male; D008784:Methysergide / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000494:pharmacology; D011149:Pons / Q000502:physiology; D051381:Rats; D017208:Rats, Wistar; D017473:Receptors, Opioid, kappa / Q000819:agonists*; D012110:Reserpine / Q000494:pharmacology; D012702:Serotonin Antagonists / Q000494:pharmacology; D013314:Stress, Mechanical; D001743:Urinary Bladder / Q000187:drug effects* / Q000502:physiology; D014554:Urination / Q000187:drug effects; D015016:Yohimbine / Q000494:pharmacology
chemical_list: D018759:Adrenergic Uptake Inhibitors; D000317:Adrenergic alpha-Antagonists; D017473:Receptors, Opioid, kappa; D012702:Serotonin Antagonists; D015016:Yohimbine; C051844:norbinaltorphimine; D009271:Naltrexone; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D012110:Reserpine; D008784:Methysergide