N-(t-Aminoalkynyl)-substituted pyrrolidones as oxotremorine antagonists

Zusammenfassung Eine Anzahl von Antagonisten zu Oxotremorin wurden durch kleine Modifikationen der Struktur des Oxotremorins erhalten. Die aktivste Verbindung, N-(1-Methyl-4-pyrrolidino-2-butinyl)pyrrolidon, ist mehr als sechsmal wirksamer als Atropin und hat eine grössere Spezifizität mit Bezug auf das Zentralnervensystem.     

Stereoselectivity of a radioimmunoassay for the insecticide S-bioallethrin

Summary The stereoselectivity of a radioimmunoassay (RIA) system using an S-bioallethrin specific antiserum was studied by observing the abilities of the 8 allethrin isomers and other selected compounds to compete with a radiolabelled S-bioallethrin tyramine derivative for antibody binding sites. The results demonstrate the feasibility of RIA as a rapid, sensitive and stereoselective residue technique for compounds difficult to analyze by classical methods.This work was supported in part by grant No. 5-R01-ES01260-02 from the National Institutes of Health.     

Stereoselectivity of a radioimmunoassay for the insecticide S-bioallethrin

The stereoselectivity of a radioimmunoassay (RIA) system using an S-bioallethrin specific antiserum was studied by observing the abilities of the 8 allethrin isomers and other selected compounds to compete with a radiolabelled S-bioallethrin tyramine derivative for antibody binding sites. The results demonstrate the feasibility of RIA as a rapid, sensitive and steroselective residue technique for compounds difficult to analyze by classical methods.     

A biologically active analogue of oxytocin not containing a disulfide group

Zusammenfassung Die Synthese eines Analogen des Deamino-oxytocins, in dem ein Schwefelatom der Disulfidbrücke durch eine Methylengruppe ersetzt ist (I,X = CH₂,R=H), wird beschrieben. Die Verbindung hat oxytocinähnliche biologische Wirkungen.     

Metabolism of a pharmacologically active pyrrolidine derivative (prolintane) by lactam formation

Zusammenfassung Prolintan, N-1-(-Benzylbutyl)-Pyrrolidin, wurde in Kaninchen durch ein Mikrosomensystem der Leber in das entsprechende Laktam, N-1-(-Benzylbutyl)-Pyrrolidin-2-on, umgebaut. Das gleiche Stoffwechselprodukt fand sich auch im Gewebe von Ratten, denen das Medikament gegeben wurde; allenfalls Spuren davon wurden im Urin der Ratten ausgeschieden.

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We thank Dr.D. C. Remy for a sample of syntheticdl-1-(-propylphenethyl)-pyrrolidin-2-one.     

Cyclic and linear vasopressin V1 and V1/V2 antagonists containing arginine in the 4-position

Substitution of arginine for glutamine in the 4-position of a vasopressin V1 antagonist has been reported to turn it into an agonist. We resynthesized this 4-arginine analog and synthesized additional cyclic and linear vasopressin antagonists containing a 4-arginine. The presence of a 4-arginine in the resynthesized and new analogs had relatively minor effects on their antivasopressin V1 and V2 antagonistic potencies.     

Cyclic and linear vasopressin V1 and V1/V2 antagonists containing arginine in the 4-position

Summary Substitution of arginine for glutamine in the 4-position of a vasopressin V₁ antagonist has been reported to turn it into an agonist. We resynthesized this 4-arginine analog and synthesized additional cyclic and linear vasopressin antagonists containing a 4-arginine. The presence of a 4-arginine in the resynthesized and new analogs had relatively minor effects on their antivasopressin V₁ and V₂ antagonistic potencies.     

Gluconolactonase: a zinc containing metalloprotein

Summary A metal analysis of bovine hepatic gluconolactonase indicates the presence of at least 1 atom of tightly bound zinc per enzyme subunit in this hexameric protein. Other divalent metals are present in lesser quantities and are subject to removal by EDTA. Activation energies for the manganese and magnesium catalyzed reactions are 5.3 and 11.0 kcal/mole, respectively.     

The effect of cholinergic antagonists on a central response to nicotine

Summary Mecamylamine and hexamethonium antagonize the prostration response of rats to centrally-administered nicotine; decamethonium and d-tubocurarine are less effective. Physostigmine does not elicit the response. Nicotine's central cholinergic effect thus may contribute to but does not fully account for its action.The authors thank the Public Health Service for its generous support of this project (grant No. 1 F32 NS 06334-01 NEUB).     

Stereoselective activity of chiral neuroleptics

Summary Attention is drawn to the evidence in favour of the stereoselective activity of chiral neuroleptics. The results reported by Gupta et al.¹, which suggest that their chiral dibenzothiepins do not fit in with that evidence, are questioned.Comments on the publication of Gupta et al.¹.     

A novel cannabinoid containing a 1,8-cineol moiety

Summary The synthesis of a novel cannabinoid containing a 1,8-cineol moiety (1) is described. It is much less biologically active than ¹-tetrahydrocannabinol.Acknowledgment. This work was supported by NIDA (grant No. DA-00574-01).     

Chicken gizzard,a myoglobin containing smooth muscle

Zusammenfassung In der glatten Muskulatur des Hühnermuskelmagens konnte ein wasserlösliches Hämoprotein nachgewiesen werden, das sich chromatographisch und spektrophotometrisch wie Myoglobin verhält.

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This work is supported by a grant from the Deutsche Forschungsgemeinschaft.