• Journal of Life Science
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• v.12 no.1
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• pp.26-31
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• 2002

Choline esters that are used with substrate of BChE-catalyzed hydrolyses were synthesized by two methods. First, 2-chloroethyl thiohexanoate, 2-chloroethyl thioheptanoate, and 2-chloroethyl thiooctanoate were synthesized by the treatment of hexanoyl chloride with ethylene sulfide. Hexanoyl thiocholine and octanoyl thiocholine were synthesized by using 2-chloroethyl thiohexanoate and 2-chloroethyl thiooctanoate with trimethyl amine. Second, after reaction of ethylene sulfide and dimethyl amine, followed by acylation with acid anhydride and then heptanonyl thiocholine, decanoyl thiocholine were synthesized by treatment of methyl iodide.

• The Korean Journal of Zoology
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• v.12 no.2
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• pp.35-38
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• 1969

1. The sensibility of Fluta alba Zuiew to acetylcholine is more than ten times as strong as that of Ophicephalus argus Cantor which has been ever known as the most sensitive material. Fluta alba Zuiew is, therefore, considered as the best material for the bioassay of acetylcholine. 2. 5-hydorxytryptamine accelerates very much the heart activity of Misgurnus mizolepis Gunther but inhibits that of Fluta alba. 3. The sensibility of Fluta alba to norepinephrine is more than a hundred times as strong as that to epinephrine.

• The Korean Journal of Pharmacology
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• v.24 no.1
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• pp.103-109
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• 1988

Cyclobuxine D, extracted from Buxus microphylla var. koreana Nakai, is a steroidal alkaloid. Many pharmacological effects of cyclobuxine D were examined in our Lab. Cyclobuxine D showed a significant bradycardic effect in the rat heart and an inhibitory action on acetylcholine and $Ba^{++}-induced$ contraction of the longitudinal muscle isolated from the rabbit jejunum. In this study, we investigated the effect of cyclobuxine D on the contractile response-elicited by acetylcholine, oxytocin and $Ba^{++}$ in rat uterine. In order to analyse the inhibitory action of cyclobuxine D on the smooth muscle, we examined the inhibitory action of cyclobuxine D against the contractile response of the high potassium-depolarized rat ileum to calcium. Concentration-dependent decrease in the peak tension and duration of the acetylcholine, oxytocin and $Ba^{++}-induced$ contraction in the isolated rat uterus was observed when cyclobuxine D was added to the organ bath. The isolated longitudinal muscle from the rat ileum was immersed calcium-depleted potassium-depolarizing solution. Ten minutes after, 1.8 mM $CaCl_2$ was added to muscle bath and elicited a biphasic increase in muscle tension. Cyclobuxine D $(6.2{\times}10^{-5}\;M)$ produced an appreciable inhibition of both components of the mechanical response. In addition, $3.1{\times}10^{-4}\;M$ cyclobuxine D, introduced at a point when the tonic response had reached its maximum level, caused the muscle to exhibit a rapid lose of tension. Based on these experimental results, we propose the possibility that the inhibitory action of cyclobuxine D on the acetylcholine, oxytocin and $Ba^{++}-induced$ contraction in the isolated rat uterus may be due to blocking potassium-activated calcium channels, voltage-sensitive calcium channels.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.163.2-164
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• 2003

Several epidemiological studies suggested that arsenic exposure was strongly correlated with the development of cardiovascular disease such as hypertension. In order to examine whether arsenic affects vasomotor tone in blood vessels, we investigated the effect of arsenic on agonist-induced vasorelaxation using the isolated rat aortic rings in vitro organ bath system.Treatment with arsenite inhibited acetylcholine-induced relaxation of aortic rings in a concentration-dependent manner. (omitted)

• Journal of Sensor Science and Technology
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• v.6 no.6
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• pp.508-513
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• 1997

We exploited a new molecular system - acetylcholine (neurotransmitter) detection system as a building block for the perfect molecular information system (sensing membrane of the chemical sensor) - using water soluble calix[n]arene-p-sulfonates which are useful even in aqueous (water/methanol) neutral solution. This achievement is due to several outstanding properties of these calix[n]arene derivatives such as low $pK_{a}$ values, cation-interactions, and high water-solubility, etc.

• The Korean Journal of Physiology and Pharmacology
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• v.7 no.4
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• pp.217-221
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• 2003

To clarify the roles of gonadal steroids on pancreatic exocrine secretion, effects of progesterone and estradiol-$17{\beta}$ on spontaneous and secretagogue-induced exocrine response of isolated perfused rat pancreas were investigated. Intra-arterial infusion of progesterone resulted in significant increase of the spontaneous pancreatic fluid and amylase secretion dose-dependently. However, estradiol-$17{\beta}$ did not exert any influence on spontaneous pancreatic exocrine secretion. Exogenous secretin, cholecystokinin (CCK), and acetylcholine markedly stimulated pancreatic fluid and amylase secretion. Progesterone initially enhanced secretin-induced amylase secretion, but this stimulatory response declined thereafter to basal value. Moreover, secretin-induced fluid secretion was not affected by infusion of progesterone. Therefore, initial increase of secretion-induced amylase secretion by progesterone seems to be a non-specific action by washout effect of secretin. Estradiol-$17{\beta}$ failed to change the secretin-induced fluid and amylase secretion. Both progesterone and estradiol-$17{\beta}$ did not exert any influence on CCK-induced fluid and amylase secretion. Acetylcholine-induced exocrine secretion of isolated perfused pancreas also was not affected by intra-arterial infusion of progesterone or estradiol-$17{\beta}$. It is concluded from the above results that progesterone could enhance the spontaneous pancreatic fluid and amylase secretion of isolated perfused rat pancreas through non-genomic shortterm action, and that these effects could be masked by more potent stimulants such as secretin, CCK, and acetylcholine.

• The Korean Journal of Pharmacology
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• v.30 no.2
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• pp.145-152
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• 1994

As it has been reported that the depolarization induced acetylcholine(ACh) release is modulated by activation of presynaptic $A_1-adenosine$ heteroreceptor and various lines of evidence indicate the $A_2-receptor$ is present In hippocampus, this study was undertaken to delineate the role of adenosine receptors on hippocampal ACh release. Slices from the rat hippocampus were equilibrated with $[^3H]-choline$ and the release of the labelled product, $[^3H]-ACh$, which evoked by electrical stimulation(3 Hz, $5\;Vcm^{-1}$, 2 ms, rectangular pulses) was measured, and the influence of various agents on the evoked tritium outflow was Investigated. Adenosine$(0.3{\sim}100\;{\mu}M)$ and CPA$(0.1{\sim}30\;{\mu}M)$ decreased the $[^3H]-ACh$ release in a dose-dependent manner without changing the basal rate of release. DPCPX$(1{\sim}10\;{\mu}M)$, a selective $A_1-receptor$, antagonist, increased the $[^3H]-ACh$ release in a dose related fashion with slight increase of basal tritium release. And the effects of adenosine and CPA were significantly inhibited by $DPCPX(2\;{\mu}M)$ treatment. CPCA, a specific $A_2-agonist$, in concentration ranging from 0.3 to 30 ${\mu}M$, decreased the evoked tritium outflow, and these effects were also abolished by $DPCPX(2\;{\mu}M)$ treatment. But the CPCA effects were not affected by $DMPX(2\;{\mu}M)$, a specific Aa-antagonist, treatment. However, CGS 21680c, a recently introduced potent $A_2-agonist$, in concentration ranging from 0.1 to $10{\mu}M$, did not alter the evoked tritium outflow. These results indicate that the decrement of the evoked ACh release by adenosine is mediated by $A_1-heteroreceptor$, but $A_2-adenosine$ receptor is not involved in ACh release in the rat hippocampus.

• Biomedical Science Letters
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• v.13 no.2
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• pp.119-125
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• 2007

It is widely known that protein tyrosine kinases (PTKs) are involved in controlling many biological processes such as cell growth, differentiation, proliferation, survival and apoptosis. An $\alpha3\beta4$ subunit combination acts as a major functional acetylcholine receptor (nAChRs) in male rat major pelvic ganglion (MPG) neurons, and their activation induces fast inward currents and intracellular calcium increases. Recently it has been reported that the activity of acetylcholine receptors (AChRs) in some neurons can be negatively regulated by PTKs. However, the exact mechanism of regulation of nAChRs by PTKs is poorly understood. Therefore, we examined the potential role particular in nAChR by PTK using electrophysiology and calcium imaging in male rat MPG neurons. ACh induced inward currents and $(Ca^{2+})_i$ increases in MPG neurons, concomitantly. These responses were inhibited by more than 90% in $Na^+$- or $Ca^{2+}$- free solution. $\alpha$-conotoxin AuIB, a selective $\alpha3\beta4$ nAChR blocket, inhibited ACh-induced inward currents. Genistein (10 $\mu$M), a broad-spectrum tyrosine kinase inhibitor, markedly decreased ACh-induced currents and $Ca^{2+}$ transients, whereas 10 $\mu$M genistin, an inactive analogue, had little effect. Overall these data suggest that the activities of $\alpha3\beta4$ AChRs in MPG neurons are positively regulated by PTK. In conclusion, trosine kinase may be one of the key factors in the regulation of $\alpha3\beta4$ nAChRs in rat MPG neurons, which may play an important roles in the autonomic neuronal function such as synaptic transmission, autonomic reflex, and neuronal plasticity.

• Korean Journal of Veterinary Research
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• v.22 no.1
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• pp.1-8
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• 1982

The effect of acetylcholine, oxytocin and prostaglandin $F_{2{\alpha}}$ ($PGF_{2{\alpha}}$) on cyclic nucleotide levels in estrogen-primed rabbit whole uterus were studied in the presence and absence of 1-methyl-3-isobutyl xanthine (MIX), a phosphodiestrase inhibitor, and indomethacin, a prostagandin inhibitor. In the absence of MIX, acetylcholine increased guanosine 3', 5'-cyclic monophosphate (cGMP), but had no effect on adenosine 3', 5'-cyclic monophosphate (cAMP) levels. In contrast, oxytocin had no influence on cGMP, but decreased cAMP levels. $PGF_{2{\alpha}}$ increased cGMP and decreased cAMP levels. MIX increased both cAMP and cGMP levels. Oxytocin and $PGF_{2{\alpha}}$ further increased cGMP levels, indicating activation of guanylate cyclase activity. The ratio of cAMP/cGMP was decreased by uterine stinulants both in presence and absence of MIX. Indomethacin elevated cAMP and cGMP revels. The effects of uterine stimulants in the presence of indomethacin on cyclic nucleotide levels were varied from tissue to tisse. In general, oxytocin decreased cGMP and $PGF_{2{\alpha}}$ increased cAMP/cGMP levels, but the effects were statisically nonsignicficant. The cAMP/cGMP ratio was increased by uterine stimulant in the presence of indomethacin. In conclusion, uterine stimulants eased cAMP/cGMP ratio which indicates that the uterine stimulants have opposing effects on adenylate cyclase and guanylate cyclase activities. The endometrium plays a role in the regulation of cyclic nucleotide levels and uterine contraction by means of PG synthesis. Indomethacin has an unknown activities besides both of PG synthetase and phosphodiesterase inhibitions.

• Journal of Nutrition and Health
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• v.28 no.7
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• pp.602-611
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• 1995

This study was designed to find out the effects of $\omega$-3 and $\omega$-6 polyunsaturated and saturated fatty acid from prenatal to growing period on the brain growth and behavioral development of rats. Rats(Sprague-Dawley strain) were fed experimental diets-fish oil, corn oil or beef tallow-with different contents of $\omega$-3 and $\omega$-6 fatty acids throughout the prenatal and lactational period and up to 10 weeks of age. DNA and RNA concentration of rat brain were determined at 0, 3, 6 weeks of age and choline and acetylcholine concentrations were analyzed at 10 weeks of age. When the rats were 7 weeks of age, position reversional test in a Y-shaped water maze for 4 weeks was measured. The experimental results obtained are summarized as follows. Food intakes were significantly lower in fish oil group and body weight gain was low in the group fed beef tallow and the groups fed fish oil and corn oil were somewhat good. Food efficiency ratio was not significantly different among the groups. Brain weight was not affected by the fatty acid composition of experimental diets and DNA and RNA concentration of the rat brain were consistently maintained at the same level. It was not different significantly among the dietary groups in the DNA and RNA concentrations of the rat brain during the experimental period. The acetylcholine concentration in the fish oil group was somewhat higher than the other groups. The position reversional test in a Y-shaped water maze showed a significant difference the score of test among the experimental groups. The score of the rats fed the fish oil diet was significantly higher than the other groups and the concentration of acetylcholine in brain were too. Therefore the correlatin between the Y-shaped water maze test score and the acetylcholine concentratin in the brain was found. Above finding support the content that dietary fatty acid composition does not affect to the brain cell number and cell size but the behavior development is influenced. Therefore, the improvement of behavior development is required the effective usage of finny tribe.