Sedative principles of the seeds of Zizyphus vulgaris var. sphinosus have been characterized as sanjoinine-A (frangufoline), nuciferine and their congeners. Also, heat treatment of sanjoinine-A-produced a more active artifact, sanjoinine-Ahl, which provides a scientific basis for heat-processing (roasting) of this Oriental medicine.

Sedative activity of Zizyphi fructus was evaluated by potentiation of hexobarbital-induced hypnosis test and its active principles have been characterized as nornuciferine and lysicamine. A new cyclopeptide alkaloid, daechucyclopeptide-1 was isolated together with zizyphusine.

Intact brain cell aggregates were dissociated from adult rat brains without cerebellum using a sieving technique. This proparation was used to elucidate the binding characteristics of agonist to muscarinic acetylcholine receptors (mAchR) in brain. Incubation of cells with carbamylcholine (carbachol) was shown agonist-induced receptor down-regulation depending on the concentration of agonist, not depending on the incubation time. This effect of carbachol was due to a reduction in the maximal binding capacity ($B_{max}$) to the mAchR without decreasing the affinity of the remaining receptors in incubation at 37.deg.C but was not apparent inincubation at $15^{\circ}}C$In addition, it was abolished when the receptors were blocked by atropine. The decline in ($^3H$)N-methylscopolamine (($^3H$)NMS) binding induced by agonist was reflected as a significant reduction in the receptor density with no change in receptor affinity, suggesting that 'true' receptor down-regulation takes place. Moreover, when the receptors were labeled with the lipophilic antagonist ($^3H$) quinuclidinyl benzilate (($^3H$) QNB) insted of the hydrophilic ligand ($^3H$)NMS, the magnitude of the observed receptor down-regulation was significantly lower in case of the former than the latter. This suggested that exposure of intact brain cells to muscarinic agonists might induce a slight degree of accumulation of receptors in intracellular sites before the receptors are actually degraded.

From the underground parts of Rosa rugosa(Rosaceae), 28-0-glucosides of euscaphic acid, tormentic acid and arjunic acid were isolated and characterized by spectral data.

The effects of butylated hydroxyanisole and butylated hydroxytoluene on the immune status in normal male were evaluated. They exhibited significant decrease in the circulating leukocyte counts. Relative spleen and thymus weights were slightly decreased, but not stratistically significant. These were, however, significant liver hypertrophies in theier exposed mice. Splenic IgM PFCs per one million cells in 1/20 LD50 BHA and BHT exposed mice were significantly reduced IgM PFCs per spleen were similar tothose of control, except in 1/20 LD50 BHA exposed mice, where they were significantly suppressed. The precise nature of the inhibition is not clear. Direct cytotoxicity is not responsible for the depressed antibody response, even following relatively high doses of them, because the changes in spleen cellularity are not significant. Both substances, however, did not show any effects on the arthus reaction and delayed hypersensitivity reaction induced by heat aggreagted bovine serum albumin, and in vivo phagocytosis of colloidal carbon. In the light of the present results, in vivo antibody response as well as in vitro, may be sensitive to BHA of the present results, in vivo antibody response as well as in vitro, amy be sensitie to BHA and BHT. Further elucidation of the precise nature of antibody suppression in their exposed mice, is warranted.

Studies on the adsorption of four kinds of bacteria, Staphylococcus aureus, Sarcina lutea, Escherichia coli and Serratia marcescens by activated Korean Kaoline have been carried out to innovate utilization as adsosrbent preparations. In connection with particle size and size fraction, the adsorption was examined by colony counting and spectroscopy. Korean kaolin was purified from Hadong white species of preminum grade and three size fractions were derived from passage through BS # 100, #200 and # 325 mesh sieves, respectively. These were activated at $105^{\circ}$or $280^{\circ}$ for three hours and at $550^{\circ}C$ for one hours. The results indicated that the adsorbing power of Korean kaolin was superior for S. aureus and S. lutea, but E. coli and S. marcescens were not adsorbed by clays. The smaller the particle size, the greater was adsorbing power for Gram-positive bacteria. Threre appears to be justification for its investigations as an ingredient in intestinal adsorbent preparations.

The molecular structure of naproxen determined by X-ray diffraction technique was refine to the final R-value geing 0.042. The compound was recrystallized from ethanol solution in monoclinic crystal system, space group $P2_1$ , with Z = 2, a = 13.375(5) $\AA$, b = 5.793(2) $\AA$, c = 7.914 $\AA$, $\beta$=93.91(3)$\AA$ and $d_{obs}$ = 1.26, $d_{calc}$ = 1.25 g/cm$^{3}$. The structure was solved by direct method and refined by block diagonal least squares procedure for 747 relfections (F .leq. 6.sigma.(F)). The molecules are connected by two intermolecular OH--O type hydrogen bonds.

An efficient and inexpensive method for the substitution of allylic hydroxyl group with fluoride, without allylic rearrangement, and elimination was developed. This method consists of treating an allylic alcohol with methylithium, followed by p-toluene sulfonyl fluoride, lithium fluoride and 12-Crown-4. This methodology was proved to be efficient by preparting geranyl fluoride, neryl fluoride, cinnamyl fluoride, E, E-farnesyl fluoride, retinyl fluoride and 4-fluoro-2-methyl-6-(ptolyl)-2-heptene.

Cardiovascular disease is at present the leading cause of deth in the United States and other in dustrilized countries. A major contributing factor of cardiovascular disease is essential hypertension. Untreated, essential hypertension is considered a risk factor for sudden death due to myocardial infarctions, as well as a risk factor for cerebral vascular disease, renal failure and congestive heart failure. During the last decade, significant progress has been made in the basic knowledge of the pathogenesis of hypertension as well as in the development of new antihypertensive drugs.

The development of physiologically based pharmacokinetic model for drug distribution and excretion is described. The physiological modeling procedure is useful in animal and clinical applications to obtain fundamental knowledge of the transport and metabolism of a substance in vivo. In this paper a review of physiologically based pharmacokinetics is presented in the hope of understanding and increasing the use of this modelling technique. The method of model development and the composition of equations based on the different models are explained. For the better understanding a physiological pharmacokinetic model of tenoxicam disposition in the rat is presented as an example of flow limited model.

An alkaloid was isolated form water-soluble fraction of Panax ginseng roots. It was characterized by spectroscopic data and dynthesis as 4, 5, 6, 7-tetrahydroimidazo (4, 5-c) pyridine-6-carboxylic acid or spinacine, which was first isolated from the plant kingdom.

The UV-pattern of several flavones, theier cytotoxicities against L1210 cell and their Inhibiting effects on ATPase from the cell seem to be correlated. 5.2'-Dihydroxy 6, 7, 8, 6'-tetramethoxyflavone ($ED_{50}$ = 2.3 ug/ml) and 5,2',6'-trihydroxy-6, 7, 8 trimethoxy flavone ($ED_{50}$ = 4.5 ug/ml), the most active flavones studied, have shown a narrow range of the absorbance ratio, Log $\varepsilon$ II/Log $\varepsilon$ I = 1.073 -1.109. They have inhibited the ATPase-activity to the greatest extent. These finding ssuggest that a certain angle between the flavone rings B and C plays an important role for the inhibition of the enzyme activity and thus the cytotoxicity.