• 약학회지
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• 제23권3_4호
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• pp.129-132
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• 1979

The ORD and CD for hyoscine-N-butylbromide present curves of negative Cotton effect in 190-250nm region. The values of .alpha./sub 232/ .alpha./sub 208/, vertical bar .alpha./sub 232/ vertical bar + vertical bar .alpha./sub 208/ and .theta./sub 221.5/ have linearities in the range of lower concentration (hyoscine-N-butylbromide 0.01-0.1w/v%). It is possible to determine the optical purity of hyoseine-N-butylbromide by using these linearities. This experiment is extremely simple and less time-consuming than other methods for estimating optical purity.

• 대한화학회지
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• 제24권2호
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• pp.115-120
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• 1980

t-Butylbromide와 benzoylchloride의 가메탄올 분해반응을 메탄올-아세토니트릴 혼합용매하에서 연구하였다. t-Butylbromide의 가메탄올 분해반응 일차속도상수는 온도 변화가 25∼$50^{\circ}C$일때 메탄올의 몰분율 0.75∼0.9 부근에서 최대치를 보였다. Benzoylchloride의 경우에는 겉보기 2차 반응속도 상수가 온도 변화 12∼$26{\circ}C$일때 메탄올의 몰분율 0.6∼0.75에서 역시 최대치를 보였다. 최대속도는 용매구조 변화에 기인함을 알았는데 메탄올에 아세토니트릴이 첨가됨에 따라 자유 메탄올 분자가 증가하여 t-butylbromide 및 benzoylchloride의 가메탄올 분해반응에서 천이상태의 안정화에 기여함을 알았다. 메탄올은 t-butylbromide의 가메탄올 분해반응의 경우 친전자 및 친핵 촉매작용을, benzoylchloride의 가메탄올 분해반응의 경우에는 친전자 촉매작용을 함을 알았다.

• Journal of Pharmaceutical Investigation
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• 제22권2호
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• pp.125-131
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• 1992

The effects of domperidone, scopolamine butylbromide and cimetidine on the absorption and bioavailability of ciprofloxacin were studied in female rats. Ciprofloxacin was given in a single oral dose of 30 mg/kg to control group. Ciprofloxacin was concurrently administered with domperidone $(T_1\;group)$, scopolamine butylbromide $(T_2\;group)$, and cimetidine $(T_3\;group)$ to rats, respectively. Significantly changed pharmacokinetic parameters observed in $T_2$group when compared with control group were first-order absorption rate constant, $Ka(4.43{\pm}0.85$\;versus\;2.86{\pm}0.41\;hr^{-1},\;p<0.05)$, time needed to reach peak concentration, $T_{max}\;(32.27{\pm}2.46\;versus\;51.75{\pm}5.51\;min,\;p<0.05)$, area under the plasma concentration-time curve, AUC $(332{\pm}19\;versus\;477{\pm}27\;{\mu}g{\cdot}min/ml,\;p<0.05)$ and absolute bioavailability, Fabs $(60.6{\pm}3.6\;versus\;87.0{\pm}5.0%,\;p<0.05)$. On the other hand, domperidone and cimetidine did not significantly affect the absorption of ciprofloxacin. It is suggested that when scopolamine butylbromide is selected for clinical use, there is need for awareness of the reduction in absorption rate and the enhancement in absorption extent of ciprofloxacin.

• 약학회지
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• 제38권5호
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• pp.516-519
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• 1994

The derivatives of methyl 5-hydroxy-dinaphtho[1,2-2',3']furan-7,12-dione-6-carboxylate (MHDDC) were synthesized by condensing alkyl sulfate or alkyl halide with MHDDC in organic solvent, and their structures were identified by NMR, MS, UV, IR etc. We also investigated the physico-chemical properties, physiological activities, and set up the micro-analytical method of the compounds.

• Journal of Plant Biotechnology
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• 제29권3호
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• pp.199-207
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• 2002

The tropane alkaloids hyoscyamine (its racemic form being atropine) and scopolamine are used medicinally as anticholinergic agents that act on the parasympathetic nerve system. Because they differ in their actions on the central nervous system, currently there is a 10-fold higher commercial demand for scopolamine, in the N-butylbromide form, than there is for hyoscyamine and atropine combined. Several solanaceous species have been used as the commercial sources of these alkaloids, but the scopolamine contents in these plants often are much lower than those of hyoscyamine. For this reason there has been long-standing interest in increasing the scopolamine contents of cultivated medicinal plants. Naturally occurring and artificial interspecific hybrids of Duboisia have high scopolamine contents and are cultivated as a commercial source of scopolamine in Australia and other countries. Anther culture combined with conventional interspecific hybridization also has been used to breed high scopolamine-containing plants in the genera Datura and Hyoscyamus, but without much success. The use of recombinant DNA technology for the manipulation of metabolic processes in cells promises to provide important contributions to basic science, agriculture, and medicine. In this review, I introduce on the enzymes and genes involved in tropane alkaloid biosynthesis and current progress in metabolic engineering approaches for tropane alkaloid, especially scopolamine, production.

• 대한약리학회지
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• 제16권2호
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• pp.25-29
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• 1980

Etomidoline ($Nonspa^{\circledR}$), which is chemically related to tertiary amine, is new synthetic antispasmodic agent with analgesic action. Antispasmodic effect of this agent is stronger than hyoscine butylbromide ($Buscopan^{\circledR}$), quaternary amine, and the absorption from intestine is also much higher. This study was undertaken to determine the effect of etomidoline on duodenal motility and other smooth muscles of rabbit. Strips of various isolated smooth muscle, 2 cm long from adult rabbits weighting about 2 kg, were suspended in a muscle chamber containing Tyrode's solution, which was bubbled with oxygen gas, and the temperature of the solution was kept constant at $38^{\circ}C$. After being washed with fresh solution several times the strips of smooth muscle attained constant motility and tonus. Etomidoline and other drugs were added in various concentrations to the chamber. Contractility of the strips was measured by using polygraph (Grass, model 7). The results are as follows: 1) In isolated rabbit atrium etomidoline produces a slight depression of contractility and the rate is also decreased. 2) On the other hand, etomidoline relaxed isolated strips of stomach, duodenal, and detrusor of rabbit. This relaxing effect of etomidoline on isolated duodenal strip of rabbit was not blocked by ${\alpha}$-adrenergic blocking agent, phenoxybenzamine, but by ${\beta}$-adrenergic blocking agent, propranolol. 3) Etomidoline did not exert any effect on isolated aorta, gall bladder, and trigone of rabbit. From the above results, it may be concluded that the relaxing effect of etomidoline on duodenal strip is related ${\beta}$-adrenergic receptor.

• Journal of Nutrition and Health
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• 제4권4호
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• pp.39-46
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• 1971

Iso-butyl bromide의 합성을 시작으로 D.L-1-amino-3-methylbutylphosphonic acid의 합성을, Diethyl phophite의 합성을 시작으로 D.L-1-amino-2-phenyl ethylphosphonic acid의 합성을 하였다. 합성되어진 필수 아미노산인 Isoleucine analogue phosphonic acid는 각각 0.2%, 0.4%를 식이에 첨가했고 Phenylalanine analogue phosphonic acid는 0.35%와 0.7%를 각각 첨가하였으며 Standard-1과 Standard-2군과 비교군인 Isoleucine 0.2%와 0.4% Phenylalanine 0.35%와 0.7%군으로써 총 100마리의 숫쥐로 각 7주씩 14주의 사육 실험을 하였다. 동물 사육 기간내의 뇨채취와 사육후의 각 장기의 채취로써 총 질소와 P, glycogen측정을 시도하였다. 이러한 일련의 실험결과 (1) D.L-1-amino-3-methylbuthylphosphonic acid나D.L-1-amino-2-phenylethylphosphonic acid의 유기 합성에 있어서는 다 수율이 낮고 상당히 높은 융점을 보였으며 ${\alpha}-NH_2$기가 Ninhydrin 반응에 예민했다. (2) Aminophosphonic acid의 첨가군(D.L-1-amino-3-methylbutyl phosphonic acid, D.L-1-amino-2-Phenylethylphosphonic acid)에서나 Amino acid(Isoleucine, Phenylalanine)첨가군에 있어서 모든 장기의 무게, 총체내질소 보유율, 간장내 총단백질량과 인의양, 및 뇨를 통한 인의 배설량에 각각 큰 차이를 보이지 않았다. 이로 보아서 Phenylalanine Aminophosphonic acid나 Isoleucine aminophosphonic acid가 다 보통 아미노산인 Isoleucine이나 Phenylalanine에 못지않게 체내에서 이용됨이 밝혀졌다. (3) 그러나 Phenylalanine aminophosphonic acid 첨가군이 간의 glycogen 함량에 있어서 Phenylalanine 첨가군과 Standard군과 비교해 보았을때 높았으며 이는 통계적인 유의성을 나타냈다.(<0.05) 이는 Phenylalanine Aminophosphonic Acid가 active state로써 간내에서 쉽게 이용되어서 Tricarboxylic cycle의 intermediate로 incorporate되는 경향으로 생각 할 수 있다.