4-Oxo-1, 2, 3, 4-tetrahydroquinazolines. I. Syntheses and pharmacological properties of 2-methyl-3-aryl-4-oxo-1, 2, 3, 4-tetrahydroquinazolines and their 1-acyl …

K Okumura, T Oine, Y Yamada, G Hayashi… - Journal of Medicinal …, 1968 - ACS Publications
Reduction of J-inethyl-d-ary 1-4 (311)-quinazolinone hydrochloride (VIII, Ar=(Jells, 2-Cll» C
«Ht, and2, 3-(CIIj) jC «lí») with XaBIL gave the corresponding 2-methyl-3-aryl-4-oNo-|, 2, 3, 4-…

The type of analgesic-receptor interaction involved in certain analgesic assays

G Hayashi, AE Takemori - European journal of pharmacology, 1971 - Elsevier
The equivalent of pA 2 values were determined for morphine-naloxone in mice using the tail-flick,
hot plate and writhing analgesic assays. In spite of marked differences in the ED 50 of …

Studies on the quantitative antagonism of analgesics by naloxone and diprenorphine

AE Takemori, G Hayashi, SE Smits - European journal of pharmacology, 1972 - Elsevier
The equivalents of pA 2 values were determined for morphine, pentazocine and etorphine
using the antagonists, naloxone and diprenorphine, and the writhing analgesic assay. The …

Studies on the relationship between 5-hydroxy-tryptamine turnover in brain and tolerance and physical dependence in mice

Y MARUYAMA, G HAYASHI, SE SMITS… - Journal of Pharmacology …, 1971 - ASPET
There is a gradual increase in the brain 5-hydroxytryptamine (5-HT) turnover rate over a
three-day period after morphine pellet implantation in mice. p-Chlorophenylalanine (PCPA) …

3-Alkyl-3-phenylpiperidine derivatives as analgesics. II

…, T Oine, H Inoue, G Hayashi - Journal of Medicinal …, 1965 - ACS Publications
2-Methyl analogs of certain3-alkyl-3-phenylpiperidine derivatives havebeen synthesized and
tested for anal-gesic activity. 1-Phenacyl derivative of the 2, 3-dimethyl compound (11) was …

3-Alkyl-3-phenylpiperidine Derivatives as Analgesics

H Kugita, H Inoue, T Oine, G Hayashi… - Journal of Medicinal …, 1964 - ACS Publications
Methods.—(1) Analgesic Activity and Toxicity.—Analgesic effect was measured by the hot-plate
method. 3 ED50 values were calculated4 from the pain reaction time of each group of 10 …

Potential nonequilibrium analgetic receptor inactivators. Synthesis and biological activities of N-acylanileridines

…, VG Telang, AE Takemori, G Hayashi - Journal of medicinal …, 1971 - ACS Publications
I11 a effort to prepare nonequilibrium analgetic receptor inactivators, a variety of N-acylanileridines
having alkylating capacity were synthesized. The analgetic potencies of this series …

4-Oxo-1, 2, 3, 4-tetrahydroquinazolines. II. Synthesis of 1-Alkyl-and 1-[2,(Distributed amino) ethyl]-2-methyl-3-aryl-4-oxo-1, 2, 3, 4-tetrahydroquinazolines

K Okumura, T Oine, Y Yamada, G Hayashi… - Journal of Medicinal …, 1968 - ACS Publications
Reaction of 2-(N-ethylacet, amido) beiizanilidc with HI in ElOII afforded l-ethyl-2-methyI-3-phenyl-4-o\ndihydmquinazolinium
iodide in quantitative yield. This conversion was reversible …

Studies on the Synthetic Analgesics. XVII. Syntheses of 2-(N-tert-Aminoalkylacylamino) thiophene

…, K Okumura, N Shigematsu, G Hayashi - Chemical and …, 1962 - jstage.jst.go.jp
The synthesis of the compounds was accomplished according to the route shown in Chart 2.
The compounds prepared are listed in Tables I, II, and III. Reduction of 2-nitrothiophene …

Hydrogenated benzo [f] quinolines and benz [e] indoles as analgetics. 1

…, S Saito, H Kugita, S Nurimoto, G Hayashi - Journal of Medicinal …, 1975 - ACS Publications
A series of octahydrobenzo [/] quinolines (Ilia) and hexahydro-l/f-benz [e] indoles (Illb), rigid
structures related to 3-phenylpiperidine and pyrrolidine analgetics, has been synthesized. …