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Biomedical subjects

S Nurimoto

Publications and source records attributed to S Nurimoto.

At least 19 recordsLinked to original sources
PubMed1992

Synthesis of N-substituted C-normorphinans and their pharmacological properties.

Several N-substituted C-normorphinans (VIII and IX) were synthesized and tested for their analgetic and narcotic antagonist activities and physical dependence capacity. Treatment of N-formyl- octahydro-2-pyrindine (IIIc) with polyphosphoric acid readily gave N-formyl-C-normorphinan (IV). The N-nor bases (V and VII) obtained from IV were converted to VIII and IX. The N-methyl derivative (I), which was previously reported to be inactive by Haffner's method, exhibited potent analgetic activity by the hot plate method and the AcOH-induced writhing test. Compounds VIII and IX showed pharmacological properties similar to those of N-substituted morphinans and exhibited agonist (analgetic) and/or narcotic antagonist activities. The C-nor analogue (IXa) of cyclorphan (IIc) exhibited potent analgetic and antagonist activities with no physical dependence capacity in the single-dose suppression tests both in rats and monkeys.

Analgesics↗
PubMed1990

Selective effect of KB-2796, a new calcium entry blocker, on cerebral circulation: a comparative study of the effects of calcium entry blockers on cerebral and peripheral arterial blood flows.

The effects of a new calcium entry blocker, KB-2796, on cerebral and peripheral circulation were compared with those of four other calcium entry blockers (flunarizine, cinnarizine, nicardipine, and diltiazem) and also papaverine in anesthetized dogs. KB-2796 increased the vertebral blood flow to the same extent as the other drugs. KB-2796 and the other drugs increased the coronary blood flow, although the effect of KB-2796 was obviously weaker than that of the other drugs. The dose of KB-2796 producing a 30% increase in coronary blood flow was about 20 times higher than that producing an equivalent increase in vertebral blood flow. KB-2796 and the other calcium entry blockers caused a moderate increase in both femoral and common carotid blood flow. The renal artery showed a biphasic response to all drugs, which consisted of an initial decrease and a subsequent increase in the flow. From these results, it is suggested that KB-2796 is a new type of calcium entry blocker that selectively affects the cerebral circulation. It is also concluded that calcium entry blockers have a different spectrum of vasodilatory action on coronary and cerebral vascular beds and that a selective coronary vasodilatory action is not a common feature among all calcium entry blockers.

Animals↗
PubMed1976

[Pharmacological studies of antipsychotic drug, penfluridol. 2. General pharmacological properties].

General pharmacological properties of penfluridol (TLP-607) a long-acting antipsychotic drug, were examined in experimental animals and the following results were obtained. 1) TLP-607 produced a lowering of arterial blood pressure and bradycardia but had almost no effect on respiration and peripheral blood flow. 2) TLP-607 slightly hypertension induced by dopamine, adrenaline and noradrenaline, but had no effect on hypotension induced by acetylcholine and histamine. 3) Antagonistic actions of TLP-607 on such spasmogens as acetylcholine, histamine and barium chloride were slightly stronger than those of haloperidol and chlorpromazine. 4) TLP-607 had neither ganglionic nor neuromuscular blocking action. 5) TLP-607 had a slight or no effect in the following experiments; protection against stomach ulcer, activity of ileum and uterus in vivo and in vitro, urinary volume and electrolytes excretion, and gastro-intestinal propulsion. These results suggest that TLP-607 has no striking peripheral actions in experimental animals.

Animals↗
PubMed1976

[Pharmacological studies of an antipschotic agent, penfluridol. (1). The central pharmacological actions].

Neuropharmacological properties of penfluridol (TLP-607) were investigated in experimental animals and were compared with those of haloperidol and chlorpromazine. Locomotor activity of mice significantly decreased at doses of 16-32 mg/kg p.o. Like haloperidol and chlorpromazine, TLP-607 (4-16 mg/kg p.o.) demonstrated catalepsy lasting for 48-72 hr in rats. TLP-607 strongly inhibited apomorphine-induced emesis in dogs and the ED50 was 0.016 mg/kg p.o. This effect lasted for 192 hr when administered 0.04 mg/kg p.o. TLP-607 antagnonized methamphetamine-induced stereotyped behavior in rats, and the ED50 was 1.83 ng/kg p.o. TLP-607 also inhibited conditioned avoidance responses in rats, and the ED50's in the pole climbing and Sidman avoidance methods were 6.73 and 3.4 mg/kg p.o., respectively. TLP-607 neither inhibited motor coordination nor enhanced hexobarbital-induced anesthesia in mice. These results suggest that TLP-607 is a potent and long-acting antipsychotic drug which has less neurotoxic side-effects.

Agonistic Behavior↗