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Benzoxazole derivatives as novel 5-HT3 receptor partial agonists in the gut.
TLDR
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
Differential contribution of two serine residues of wild type and constitutively active β2‐adrenoceptors to the interaction with β2‐selective agonists
TLDR
Results suggest that Ser204 and Ser207 of the wild type and constitutively active β2‐adrenoceptors differentially interacted withβ2‐selective agonists. Expand
Measurement and pharmacokinetic analysis of imipramine and its metabolite by brain microdialysis
TLDR
The present results suggest that the brain microdialysis method reflects the intracerebral pharmacokinetics of Imip and DMI well and may be applicable to further pharmacokinetic investigations of psychotropic agents. Expand
Pharmacological properties of a new centrally acting muscle relaxant (NC-1200) in isolated muscle preparations.
TLDR
The present results are similar to the previous findings that the properties of serotonin, histamine and norepinephrine receptors in the rabbit aorta were different from those in other muscles. Expand
Interactions of codeine-7,8-oxide (codeine-epoxide), as a new metabolite of codeine, with multiple opiate receptors.
TLDR
The ability of codeine-epoxide to displace [3H]dihydromorphine binding was the most effective among three labeled ligands, suggesting that codeine -epoxide had a selectively high affinity to mu-receptors, despite the fact the affinities of codeines to opiate receptors were slightly less potent than its parent compound, codeine. Expand
Molecular characterization of pharmacological properties of T-0509 for beta-adrenoceptors.
TLDR
The results indicate that T-0509 is a relatively specific beta 1-adrenoceptor agonist with a high intrinsic activity as compared with isoproterenol. Expand
A new 5-HT3 receptor ligand. II. Structure-activity analysis of 5-HT3 receptor agonist action in the gut.
TLDR
Results suggest that, in these 5-HT3 receptor agonists, the substituents of the benzoxazole ring influence the B-J reflex-inducing activity in rats. Expand
Improvement of pentobarbital-induced heart failure by MCI-154, a novel and potent cardiotonic agent, in the dog heart-lung preparation.
The efficacy of MCI-154, a new pyridazinone cardiotonic agent, in improving heart failure was assessed in dog heart-lung preparations in which cardiac function had been severely depressed byExpand
Similarity and dissimilarity of the vasoconstrictor effects of Bay K 8644 on coronary, femoral, mesenteric and renal circulations of dogs
TLDR
Differences in potency, effectiveness and duration of the vasoconstrictor effects of Bay K 8644 between the 4 arterial beds probably derive from differences in characteristics of the smooth muscle of resistance vessels there. Expand
Sensitive determination of (-)-isoproterenol and (-)-(R)-1-(3,4- dihydroxyphenyl)-2-[(3,4-dimethoxyphenethyl)amino] ethanol (T-0509), a cardiotonic agent, in rat plasma utilizing a fully automated
TLDR
Rat plasma values for ISO and T-0509, a new cardiotonic agent, were determined in rat plasma using a fully automated catecholamine (CA) analyser that includes in-line pre-extraction of CAs, coupled with an HPLC-ethylenediamine condensation reaction and a peroxyoxalate chemiluminescence detection system. Expand
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