Model of the effect of 4-aminopyridine at the level of potassium channels of the giant axon of the squid, Logigo forbesi L.]

Most of the effects of 4-aminopyridine on the potassium conductance of the giant axon of the Squid can be explained in terms of a simple model based on the physicochemical properties of the molecule and what is known about the structure of the potassium "channels".     

X-ray analysis of Co-C bond cleavage in the crystalline state

During serial structure analysis of cobaloxime derivatives, aimed at interpreting the catalytic capability of the asymmetric hydrogenation, we have found that the crystal of R-alpha-cyanoethyl (S-alpha-methylbenzylamine)-cobaloxime changes its unit cell dimensions by X-ray exposure without degradation of a single crystal form. The rate of the change was so slow that it was possible to collect the intensity data for several intermediate stages. We have proved, by calculating electron density in each stage, that the change reflects the racemisation of the cyanoethyl group.     

A new one-step synthesis of hexahydrocannabinoid analogs

Summary A one-step synthesis of hexahydrocannabinoid analogs (HHC) is described making use of the condensation of phenolic ketones and aldehydes with citronellal in the presence of pyridine.Grateful thanks are accorded to Drs L. Chopard and S. Selvavinayakam for spectral measurements and Dr I. Fleming for useful discussion.R. Mechoulam and Y. Gaoni, Recent advances in the chemistry of Hashish, in: Progress in the Chemistry of Organic natural products, vol. 25, p. 175. Ed. L. Zechmeister. Springer Verlag, Wien 1967; R. Mechoulam, Marijuana Chemistry and Pharmacology, metabolism and clinical effects. Academic Press, New York 1973; R. Mechoulam, N. K. McCallum and S. Burstein, Chem. Rev.76, 75 (1976).     

Antioxidant effects on prostaglandin synthesis in rabbit kidney medulla slices

Summary Sodium diethyldithiocarbamate, 2,6-di-tert-butylphenol and N,N-diphenyl-p-phenylenediamine inhibited the generation of medullary prostaglandin E, but 1,2-dimethoxyethane (OH scavenger) and 2,5-dimethylfuran (¹O₂ scavenger) stimulated basal prostaglandin E production 1.2–1.3-fold. These results suggest that the balance between formation and removal of cellular lipid peroxides sets a peroxide level that can regulate the rate of prostaglandin formation in cells.     

Effects of several preoperative medications on fat cell lipolysis, and activity of adipose tissue cyclic AMP phosphodiesterase.

Effects were examined of atropine, diazepam, pethidene, promethazine, scopolamine, omnopon and papaverine on basal and noradrenaline-stimulated lipolysis in rat isolated fat cells and on rat adipose tissue cyclic AMP phosphodiesterase activity. Papaverine at high concentration (1 mM) inhibited both basal and hormone-stimulated lipolysis, whereas diazepam enhanced basal lipolysis. At a 'clinical dose', omnopon increased both basal and noradrenaline-stimulated lipolysis. Adipose tissue cAMP phosphodiesterase activity was strongly inhibited by 1 mM diazepam, papaverine, promethazine and omnopon (280 microgram ml-1). Lack of enhancement of lipolysis by the established cAMP phosphodiesterase antagonist papaverine, is compatible with simultaneous inhibition also of adipose adenyl cyclase. Diazepam-stimulated lipolysis is compatible with its phosphodiesterase inhibitory activity. It is proposed that papaverine-containing omnopon may offer some survival advantages during surgical stress by facilitating a caloric supply.     

Multiplicity of monoamine oxidase in chick brain

Summary The substrate- and inhibitor-related characteristics of monoamine oxidase (MAO) were studied on chick brain mitochondria. It was found that neither 5-hydroxytryptamine nor -phenylethylamine is the specific substrate for type A and type B MAO in chick brain.     

Effect of air ionization on blood serotonin in vitro

Summary The effect of negative and positive air ionisation on siliconized blood serotonin was studied in vitro. The experiments showed that within 10 min positive ionisation increased serotonin levels in total blood (+40%), plasma (+90%), erythrocytes (+50%) and thrombocytes (+200%). On the other hand, negative ionization (10 min) lowered the serotonin content of total blood (–30%), plasma (–42.5%), erythrocytes (–41.7%) and thrombocytes (–72.3%), thus confirming the Krueger Effect in vitro.This research was generously supported by a grant from the Joint Research Fund of the Hebrew University and Hadassah, and Dr. and Mrs.Leonard Appleby of Palmbeach, Florida.Acknowledgment: Our thanks are due to Mr.B. Shalita, Mrs.Zippora Adar and Mrs.Olga Fradkin for devoted technical assistance.     

仓鼠妊娠期瘦素分泌及其调节机制

对妊娠期瘦素的分泌及其调节机制进行探讨. 将100只3月龄雌性金黄仓鼠分成16组, 每组6~7只, 每天采血样用于测定其妊娠期的瘦素分泌. 实验结果表明, 瘦素于妊娠第9天开始显著升高, 于妊娠第12天达到高峰. 为验证不同生殖阶段的血清是否对瘦素分泌有不同影响, 将不同生殖阶段抽提与未抽提类固醇激素的血清加入培养液中进行培养, 发现动情期及妊娠期的血清均可刺激体外培养的脂肪细胞瘦素分泌, 动情期抽提与未抽提类固醇激素的血清对脂肪细胞瘦素分泌的刺激作用没有显著差异(P > 0.05). 与动情期血清相比, 妊娠中后期未抽提类固醇激素的血清显著刺激脂肪细胞瘦素分泌(P < 0.01). 但妊娠中后期的血清在抽提类固醇激素后对瘦素分泌的刺激作用显著下降, 与动情期的血清对瘦素分泌的刺激作用已没有显著差异(P > 0.05). 妊娠不同阶段未抽提类固醇激素的血清对瘦素分泌的刺激作用有很大差异, 妊娠第15天的血清对瘦素分泌的刺激作用显著高于妊娠第8天(P < 0.0001)和妊娠第12天(P < 0.001)的血清. 体外研究进一步表明, 肾上腺皮质素、孕酮以及胰岛素均能刺激瘦素分泌, 而雌激素却能抑制体外瘦素分泌. 研究结果提示, 妊娠期血液类固醇激素水平的上升是引起妊娠期瘦素峰出现的重要因素.