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Volume 29 (1993)
- Issue 6 Pages 239-
- Issue 5 Pages 143-
- Issue 4 Pages 101-
- Issue 3 Pages 69-
- Issue 2 Pages 37-
- Issue 1 Pages 1-
Predecessor
Volume 29, Issue 2
Displaying 1-4 of 4 articles from this issue
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D. GRUNDY1993 Volume 29 Issue 2 Pages 37-46
Published: 1993
Released on J-STAGE: July 21, 2010
JOURNAL FREE ACCESSDownload PDF (4014K) -
Kenji YAMADA, Yuichi ONODA1993 Volume 29 Issue 2 Pages 47-53
Published: 1993
Released on J-STAGE: July 21, 2010
JOURNAL FREE ACCESSThe colonic prokinetic activity of a newly synthesized compound, T-1815, administered orally, was compared with that of yohimbine and naloxone in mice. The time required to evacuate a glass bead inserted into the distal colon was taken as an index of prokinetic activity. Clonidine (3-30 μg/kg s.c.), and loperamide (0.3-3.0 mg/kg s.c.) delayed bead expulsion in a dose-dependent manner. Yohimbine (0.3-10 mg/kg) and T-1815 (0.1-10 mg/ kg) showed a dose-dependent reduction of the delay in evacuation induced by clonidine, but naloxone had no effect. The loperamide-induced retardation of colonic propulsion was reduced by naloxone (0.3-10 mg/kg) and T-1815 (0.1-10 mg/kg) in a dose-dependent manner, but yohimbine had no effect. In normal animals, yohimbine and naloxone had no significant effect on evacuation, while a slight acceleration was observed with T-1815 at 10 mg/kg. No soft feces and/or diarrhea were observed with any of the three test drugs. These results indicate that T-1815 appears to be a unique colonic prokinetic compound, the action of which may be mediated through mechanisms other than antagonism for α2-adrenoceptors or opioid receptors.View full abstractDownload PDF (686K) -
Issei TAKAYANAGI, Noriko KOKUBU, Koji SHIRAISHI1993 Volume 29 Issue 2 Pages 55-61
Published: 1993
Released on J-STAGE: July 21, 2010
JOURNAL FREE ACCESSInstillation of pilocarpine-induced a miosis in a rabbit. In an isolated iris sphincter muscle of rabbit, pilocarpine induced a small contraction and behaved as an antagonist of carbachol. The contractile response of an isolated rabbit dilator muscle to a field stimulation was inhibited by pilocarpine. This inhibitory action of pilocarpine was antagonized by atropine in a concentration-dependent manner. An amount of norepinephrine released from the electrically stimulated dilator muscle was inhibited by pilocarpine. The inhibitory effect of pilocarpine on norepinephrine release was decreased by atropine. A following explanation is proposed as a most possible mechanism for the pilocarpine-induced miosis in the rabbit. Pilocarpine activates the prejunctional cholinoceptors to inhibit norepinephrine release from the adrenergic nerve in the dilator muscle. Thus pilocarpine decreases tonus of the dilator muscle and induces the miosis.View full abstractDownload PDF (699K) -
Shun KONDO, Takashi MORITA, Shigeru HIRANO1993 Volume 29 Issue 2 Pages 63-68
Published: 1993
Released on J-STAGE: July 21, 2010
JOURNAL FREE ACCESSThe affinities of various muscarinic antagonists to human detrusor muscle were determined using radioligand binding techiniques. Saturation experiments with 3H-QNB revealed that there were significant amount of muscarinic cholinergic receptors in human detrusor muscle. Displacement of 3H-QNB binding by various muscarinic subtype selective drugs was studied in the inhibition experiment. Pirenzepine, AFDX-116 and 4-DAMP inhibited the 3H-QNB binding to human detrusor muscle with the Ki values (nM) (mean±S. D., n=6) of 243±62.5, 59.7±15.3 and 2.69±0.96, respectively. These data indicate that M3-selective drug possesses the highest affinity to human detrusor muscle. The Ki values of oxybutynin and tiquizium bromide were similar to those of 4-DAMP, suggesting that these two drugs have strong affinities to human detrusor muscle.View full abstractDownload PDF (637K)
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