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Biomedical subjects

H Maeno

Publications and source records attributed to H Maeno.

At least 73 records · Page 4Linked to original sources
PubMed1979

Pharmacological and biochemical studies on a new potential neuroleptic, N-(1-benzyl-3-pyrrolidinyl)-5-chloro-2-methoxy-4-methylaminobenzamide (YM-08050).

Pharmacological and biochemical properties of a novel compound, N-(1-benzyl-3-pyrrolidinyl)-5-chloro-2-methoxy-4-methylaminobenzamide (YM-08050) were compared with those of haloperidol (HPD) and chlorpromazine (CPZ) in animals. YM-08050 was more potent than either HPD or CPZ in inhibitory effects on a variety of behaviors such as apomorphine-induced stereotypes behavior and emesis, methamphetamine-induced stereotyped behavior, conditioned avoidance response and open field behavior. YM-08050 induced catalepsy only at much higher doses than to exhibit the inhibitory activities. The inhibitory effects of YM-08050 on [3H]dopamine binding and dopamine-sensitive adenylate cyclase in the synaptic membrane fractions of canine caudate nucleus were much greater than those of HPD and CPZ. The results suggest that YM-08050, a potent central dopaminergic blocker, is a potential antipsychotic drug with less extrapyramidal side effects than those of HPD and CPZ.

Animals↗
PubMed1979

Pharmacological and biochemical studies on a new compound, 2-(7-indeyloxymethyl)morpholine hydrochloride (YM-08054-1), and its derivatives with potential antidepressant properties.

Antidepressant properties of a new indene derivative, YM-08054-1, and its related compounds were compared with those of tricyclic antidepressants and viloxazine. The potencies of YM-08054-1 to inhibit uptake of both 14C-norepinephrine (14C-NE) and 14C-5-hydroxytryptamine (14C-5-HT) by the rat brain synaptosomes were similar to those of amitriptyline and imipramine. Other indene derivatives with an N-alkylated morpholine ring were proved to have less effect on the uptake of either 5-HT or NE than was YM-08054-1. YM-08054-1 was the most potent among all of the tested antidepressants in the inhibition of reserpine-induced facilitation of convulsions as well as in the potentiation of reserpine-induced facilitation of convulsions as well as in the potentiation of 5-hydroxytryptophan (5-HTP)-induced syndromes in mice, though the inhibitory effect of this agent on reserpine-induced hypothermia was weaker than that of either amitriptyline or desipramine, suggesting relatively selective effects of YM-08054-1 upon 5-HT rather than NE uptake in vivo. Neither viloxazine nor iprindole potentiated the responses to 5-HTP. YM-08054-1 was devoid of peripheral anticholinergic activity and exhibited weak local anesthetic effect as well as low acute toxicity when compared with amitriptyline. The results indicate that YM-08054-1 has a novel profile as an antidepressant agent which is quite different from that of either viloxazine or tricyclic compounds.

Anesthetics, Local↗
PubMed1978

Effects of indenolol (YB-2), a new beta-adrenergic blocking agent, and its dextro isomer on the central nervous system of mice and rabbits.

Central depressant actions of a new beta-adrenergic blocking agent, indenolol (YB-2), and its dextro isomer were studied in mice and rabbits. d-Indenolol was less active than dl-indenolol in lowering of methamphetamine group toxicity and calming of fighting behavior, though muscle relaxant, hypolocomotive and anticonvulsant effects of d-indenolol were virtually equal to those of the racemate. dl-Propranolol showed a similar profile of central depressant actions to dl-indenolol, whereas dl-practolol revealed no significant central effects in mice. The dose-response relationship between beta-blocking and central effects in the same animal species suggested that both taming and anti-methamphetamine group toxicity effects of dl-indenolol s.c. do not directly relate to either the peripheral beta-blocking or the membrane stabilizing activity. Intravenous as well as intracerebroventricular administration of dl-indenolol resulted in suppression of pressor responses to the electrical stimulation of the brain stem of unanesthetized rabbits. Neither d-indenolol nor dl-practolol was effective against the pressor responses, suggesting that these two compounds acted on the CNS in a manner different from dl-indenolol even when intracerebroventricularly administered. A possible central beta-adrenergic blocking effect of dl-indenolol was discussed in the light of mechanisms of an antihypertensive action of this compound.

Adrenergic beta-Antagonists↗
PubMed1977

Oral bronchodilator effect of 16(S)-methyl-20-methoxy-PGE2 (YPG-209) in guinea-pigs.

The bronchodilator activity of synthetic 16(S)-methyl-20-methoxy-PGE2 (YPG-209) was investigated in guinea-pigs. The potency of YPG-209 in relaxing the isolated trachea contracted by histamine was 10 times smaller than that of PGE2, and was not reduced by propranolol, while in the anesthetized animals YPG-209 given by an intravenous route was 230 times as potent in inhibiting an increase in the airway resistance induced by histamine as PGE2. When administered either intraduodenally to the anesthetized animals or orally to the conscious ones, YPG-209 showed a pronounced protection against histamine-induced bronchoconstriction, in contrast to PGE2 which had no significant protecting effect. Neither hypotension nor diarrhea could be observed at the doses of YPG-209 exhibiting a considerable bronchodilator effect. The hydroxyl group at carbon-15 of YPG-209 was little oxidized by 15-hydroxy prostaglandin dehydrogenase which was purified from the lung of guinea-pigs, consistent with the comparably long lasting bronchodilator activity of YPG-209 in vivo.

Airway Resistance↗
PubMed1976

Vasodilator profile of a new 1,4-dihydropyridine derivative, 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-[2-(N-benzyl-N-methylamino)]-ethyl ester 5-methyl ester hydrochloride (YC-93).

A new 1,4-dihydropyridine derivative, 2,6-dimethyl-4-(3-nitrophenyl)-4,4-dihydropyridine-3,5-dicarboxylic acid 3-[2-(N-benzyl-N-methylamino)]-ethyl ester 5-methyl ester hydrochloride (YC-93), when i.v. injected into anesthetized dogs, exhibited not only a greated vasodilation in both cerebral and coronary than in femoral vessels, but also about 100 to 300 times higher potency as well as longer durability than any of reference drugs such as isoxsupurine, papaverine and cinnarizine. YC-93 was also effective in vasodilation by i.m. and i.d. administration. When administered into vertebral and coronary arteries, YC-93 caused vasodilation at the doses that did not affect systemic blood pressure. YC-93 did not potentiate the vasodilator effect of adenosine, and vasodilation by YC-93 was influenced by neither propranolol, atropine, diphenhydramine nor aminophylline. Acute toxicity (LD50) of YC-93 was almost the same as that of papaverine in mice and rats. Thus, YC-93 is a potent bu low-toxic vasodilator agent acting preferentially and perhaps directly on cerebral and coronary vascular beds and is well absorbed from gastrointestinal tract into blood stream.

Animals↗