A facile one-step synthesis of cysteinyldopas using mushroom tyrosinase

Summary A convenient one-step procedure, based upon the tyrosinase co-oxidation of dopa and cysteine, is reported for the synthesis of 5-S-cysteinyldopa (I) in 74% yield. Secondary products of the reaction turned out to be 2-S-cysteinyldopa (II, 14%), 2,5-S, S-dicysteinyldopa (IV, 5%), and the hitherto unknown 6-S-cysteinyldopa (III, 1%).The generic term cysteinyldopa is proposed to designate the various cotechol amino-acids arising from addition of cysteine to dopaquinone.This work was supported in part by a grant from Consiglio Nazionale delle Ricerche, Roma.     

Some properties of the goat placental lactogen

Summary Goat placental lactogen was partially purified from a medium collected after placental tissue incubation. The data obtained by disc electrophoresis and isoelectric focusing experiments, as well as by means of radioreceptor assay methods, provide evidence of the similarity between the goat and ovine placental lactogen.The careful technical assistance of L. Tichovská is gratefuly acknowledged.     

A cannabinoid with cardiovascular activity but no overt behavioral effects

Summary Abnormal-⁸-tetrahydrocannabidiol (ABN-⁸-THC) failed to elicit central nervous system and cardiovascular effects in laboratory animals. Abnormal-cannabidiol (ABN-CBD) was also devoid of overt behavioral effects but produced marked hypotension with only slight bradycardia in anesthesized dogs.Acknowledgment. This work was supported by NIDA (grant No. DA-00574-01 and DA-00490) and Virginia Heart Society (grant No. RR-05697)     

A tissue-selective prostaglandin E2 analog with potent antifertility effects

Summary N-methanesulfonyl 16-phenoxy--tetranor PGE₂ is a prostaglandin analog which is markedly more tissue selective than PGE₂. This compound is 10–30 times more potent than PGE₂ in animal models which are considered relevant to antifertility effects in humans. In pharmacological tests which are believed to be predictive for side effects in humans, the compound has potency either equal to or less than that of PGE₂.     

Molecular analysis of spontaneous somatic mutants.

Eukaryotic structural gene mutations occurring spontaneously in a mouse myeloma cell line offer the opportunity to study somatic mutation in animal cells at the molecular level. Studies on the myeloma protein and on mRNA have enabled us to characterise four such mutants representing four different mutation mechanisms. The results may have some bearing on the origin of antibody diversity.     

Determinant selection is a macrophage dependent immune response gene function

Immune response (Ir) genes are linked to the species histocompatibility complex and define as yet uncharacterised phenotypic products which control the immune response to thymus dependent antigens. Antibody formation and antigen induced T lymphocyte proliferation are two examples of immune phenomena which, in vivo and in vitro, operate under Ir gene influence. To clarify their mechanism of action and cellular location, we have examined the contribution of antigen structure (amino acid sequence and conformation to Ir gene control of antigen recognition by T lymphocytes) as well as to the critical role played by the antigen presenting macrophage in expression of that control. We report that immune response gene control of antigen recognition operates at least in part at the level of the macrophage.     

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).     

Survival and endogenous spleen colonies of irradiated mice after skin wounding and hydroxyurea treatment

Summary Wound trauma-induced survival from radiation may be related to increased mitosis in hematopoietic cells. This is supported by the cell cycle-dependent drug hydroxyurea, which 1. blocked survival of wounded mice injected 2 or 3 days after 900 rad and 2. reduced the number of endogenous CFU-s in wounded mice injected shortly before 700 rad.Supported by the Armed Forces Radiobiology Research Institute, Defense Nuclear Agency, under Research Work Unit MJ00018. Views presented in this paper are those of the authors; no endorsement by the Defense Nuclear Agency has been given or should be inferred.Research was conducted according to the principles enunciated in the Guide for the Care and Use of Laboratory Animals prepared by the Institute of Laboratory Research, National Research Council.     

The free radical oxidation of the tetrahydrocannabinols

Summary The free radical oxidation of ¹ and ⁶-tetrahydrocannabinol has been examined by spin trapping techniques and intermediates that would lead to cannabinol have been trapped. The 1st step in the oxidation of ¹-THC involves the removal of 3-H, while for ⁶-THC, either 2-H or 5-H. Intermediates were isolated which could be pyrolysed to the diene and cannabinol.