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Muscarinic acetylcholine receptors in the rabbit ciliary body smooth muscle: spare receptors and threshold phenomenon.
Interactions of several muscarinic drugs with their receptors were studied in the ciliary body smooth muscles of the rabbit, and atropine produced a parallel shift to the right in the concentration-response curves for carbachol. Expand
Benzoxazole derivatives as novel 5-HT3 receptor partial agonists in the gut.
- Y. Sato, M. Yamada, +5 authors F. Konno
- Medicine, Chemistry
- Journal of medicinal chemistry
- 30 June 1998
Compound 6v inhibited 5-HT-evoked diarrhea but did not prolong the transition time of glass beads in the normal distal colon even at a dose of 100 times the ED50 for diarrhea inhibition in mice. Expand
Characterization of postsynaptic alpha1-adrenoceptors in the rabbit iris dilator smooth muscle
The results suggest that alpha1-adrenoceptors in the rabbit dilator muscle and aortic strips may not be identical and that both selective and nonselective antagonists which act on these receptor sites exist. Expand
Comparison of the muscarinic cholinoceptors in the rabbit ciliary body and the guinea-pig ileum.
The results suggest the importance of both receptor density and threshold as determinants of agonist potency. Expand
Involvement of threshold level in the contractile responses for some alpha 1-andrenoceptor agonists in the rabbit iris dilators.
The results suggest that the threshold phenomena in the tissue used may be an important factor in determining the agonist sensitivity, and the pD2-values of tizanidine and clonidine were significantly lower than the corresponding pKB-values. Expand
Pharmacological properties of codeine-7,8-oxide (codeine epoxide), a new metabolite of codeine.
- I. Takayanagi, F. Konno, N. Miyata, K. Watanabe, M. Hirobe
- Chemistry, Biology
- Japanese journal of pharmacology
The antinociceptive activity, development of tolerance and the inhibitory activity of abstinence syndrome are studied to clarify pharmacological properties of this new metabolite of codeine. Expand
Relationship between synaptosomal calcium uptake and antinociceptive action of morphine.
Investigation of the relationship between inhibition of 45Ca2+ uptake and the antinociceptive action induced by morphine and effects of papaverine and 1,1-diphenyl-3-piperidinobutanol hydrochloride shows that the inhibition of synaptosomal calcium uptake plays an important role in the production of morphine-antinocption. Expand
Some pharmacological properties of morphine-7,8-oxide (morphine epoxide).
- I. Takayanagi, R. Shibata, F. Konno, N. Miyata, M. Hirobe
- Chemistry, Medicine
- Journal of pharmacobio-dynamics
- 1 July 1982
Morphine-7,8-oxide (morphine epoxide) is assumed to be a metabolite of morphine, and was less potent than morphine in the inhibition of abstinence syndrome and in the development of tolerance in antinociceptive action. Expand
Interaction of morphine- and codeine-epoxides with opiate receptor.
Effect of morphine on the stimuli-induced calcium uptake into synaptosomes isolated from morphine-tolerant rats.
The results suggested that adaptive changes ofsynaptosomal calcium uptake produced by exposure to morphine may be involved in tolerance and physical dependence development, but influence of morphine on calcium uptake by the synaptosomes isolated from the rats acutely tolerance to morphine was differed from that of chronic tolerant rats. Expand