Pharmacodynamic profile of CQP 201-403, a novel 8α-amino-ergoline

Summary The profile of action in animals of CQP 201-403, a novel 8-amino-ergoline, is in most aspects that of a very potent dopaminomimetic, both as a prolactin secretion inhibitor, and at the levels of the CNS and the cardiovascular system. Qualitatively CQP 201-403 differs slightly from bromocriptine and apomorphine in its effects on the CNS (no influence on serotonin metabolism in the rat cortex; induction of masculine mounting behavior in rats) and the cardiovascular system of the dog (reflex tachycardia in response to a blood-pressure fall). In man the new compound proved to be highly active in lowering prolactin serum levels and to be more potent than bromocriptine (Parlodel^®).In memory of Dr Annemarie Closse, who died 14 June 1987.     

Comparative aspects of structure and action of molluscan neuropeptides

A number of neuropeptides were isolated from the ganglia and muscles of molluscs, and their actions were examined. Diverse neuropeptides, in addition to several classical neurotransmitters, were suggested to be involved in the regulation of the anterior byssus retractor muscle ofMytilus. A wide structural variety of members of theMytilus inhibitory peptide family was observed in each of the generaMytilus, Achatina andHelix. Gly-Trp-NH₂, the C-terminal dipeptide fragment of the neuropeptide AGPWamide, showed a more potent action than the parent peptide in all of the muscles examined. Peptides related to some molluscan neuropeptides were found to be distributed interphyletically. Some neuropeptides containing ad-amino acid residue were found inAchatina andMytilus. These aspects of molluscan neuropeptides are thought not to be exceptional.     

Biosynthesis of 1-aminocyclopropanecarboxylic acid: Steric course of the reaction at the C-4 position

Summary Under the action of the appropriate synthase from ripe tomatoes a 11 mixture of (3S, 4R)-[3,4-²H₂] and (3R, 4S)-[3,4-²H₂]-(2S)-adenosylmethionine is transformed into a 11 mixture of the two meso forms of [²H₂]-1-aminocyclopropanecarboxylic acid, a result which proves the operation of an inversion mechanism and which is consistent with direct nucleophilic displacement of the leaving group in the substrate.     

Bicuculline and picrotoxin block γ-aminobutryic acid-gated Cl− conductance by different mechanisms

Summary Using isolated, internally perfused bullfrog dorsal root ganglion cells we have studied the dose-response curves for -aminobutyric acid (GABA) in the presence of internally or externally applied GABA antagonists. With external application of antagonists the inhibition of the GABA current by bicuculline was competitive and that by picrotoxin was noncompetitive. Picrotoxin but not bicuculline blocked when internally perfused.To whom reprint requests should be addressed.Acknowledgments. We thank Drs S. Minakami and S. Yasui for helpful discussions and comments.     

A new semisynthetic ergot peptide alkaloid: DCN 203-922

Summary We report the synthesis, stereochemistry and preliminary pharmacological evaluation of DCN 203-922, a novel ergot alkaloid of the cyclol type, which contains in its peptide moiety the uncommon amino acid L-allo-isoleucine.Part of this paper was reported by this author at the Herbstversammlung der Schweizerischen Chemischen Gesellschaft, Bern, in October 1986.     

Eicosapentaenoic acid in tissue lipids ofPieris brassicae

Summary Larvae of the cabbage white butterfly,Pieris brassicae, have a dietary requirement for linolenic acid (C183n3) and were found to accumulate two other members of the n-3 family, C203n3 and C205n3 (eicosapentaenoic acid) especially in testicular phospholipids. Arachidonic acid was observed in trace amounts only. During diapause the relative titer of eicosapentaenoic acid increased in testicular phospholipids to about 4.2% of the fatty acids. Eicosapentaenoic acid is a possible precursor of prostaglandins, suggesting that prostaglandins of the 3-series predominate in this insect.     

重组大肠杆菌利用醋酸及乳酸为碳源合成PHB

以廉价的工业副产物醋酸及乳酸为碳源,对产PHB重组大肠杆菌进行培养,考察醋酸及乳酸的添加对重组大肠杆菌生长及PHB产量的影响。将来自Cupriavidusnecator的PHB合成操纵子phaCAB基因簇克隆至pBAD载体,得到产PHB菌株BL21＿pBAD＿phaCAB,以阿拉伯糖为诱导剂,在大肠杆菌中进行重组表达。分别使用LB及M9培养基,对重组菌株BL21＿pBAD＿phaCAB进行培养,研究其生长速度及PHB产量,探索产PHB重组大肠杆菌最适培养基。以添加0.04 g/L乳酸、1.2 g/L乳酸、0.02 g/L醋酸、0.6 g/L醋酸、0.04 g/L乳酸+0.02g/L醋酸、1.2g/L乳酸+0.4g/L醋酸的M9培养基(均含2 g/L葡萄糖)为实验组,以M9培养基(含2g/L葡萄糖)为对照组,考察醋酸及乳酸的添加对重组大肠杆菌生长及PHB产量的影响。分别取第6,12,24和36小时的培养液,分析其葡萄糖、醋酸及乳酸含量的变化。结果表明,低氮型M9培养基更适合产PHB重组大肠杆菌在低糖培养环境中生长。在葡萄糖消耗殆尽后,大肠杆菌能够以醋酸及乳酸为碳源进行代谢,因此在培养基中...     

NTA强化Fe(Ⅱ)/PMS体系降解橙黄G的效能与机制

针对二价铁/过一硫酸盐(Fe(Ⅱ)/PMS)体系存在近中性pH条件下氧化效能低的问题,采用氨基三乙酸(NTA)强化Fe(Ⅱ)/PMS体系降解橙黄G(OG),研究NTA/Fe(Ⅱ)/PMS体系中OG降解的效能和机制,考察NTA,Fe(Ⅱ),PMS等反应物浓度和溶液pH值对OG降解效能的影响.实验结果表明：当pH=6.5时,NTA可显著强化Fe(Ⅱ)/PMS体系的氧化效能,OG的去除率从11.7%提高到92.5%,NTA的加入提高了溶液中有效活化剂的浓度,促进PMS分解生成活性物质;NTA/Fe(Ⅱ)/PMS体系中主导的活性物质为Fe(Ⅳ)和SO^-₄·,二者对体系氧化效能的贡献分别为72.0%和28.0%;增加NTA,Fe(Ⅱ)和PMS的浓度有助于OG的降解,但当三者浓度分别超过1.5,1.5,2.0 mmol·L^-1时,出现抑制现象;引入NTA既提高了Fe(Ⅱ)/PMS体系在近中性pH条件下的氧化能力,又拓宽了该体系的pH应用范围.