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).     

Non-mendelial female sterility in Drosophila melanogaster: demonstration of an inducer chromosome 4]

Crosses between two classes of Drosophila melanogaster strains (reactive and inducer) may lead to partially sterile F1 females. This sterility, called S.F. sterility, can be characterized by its physiological features. It appears to be the result of an interaction between two factors: "R" brought into the initial croos by the reactive mother and "I" by chromosomes of the inducer father. Except for chromosome 4, each chromosome of the well known inducer strains may carry the I factor (inducer chromosomes). The present results provide evidence for the presence of an inducer fourth chromosome in the inducer strain Nagasaki.     

Lithium exchange in from epithelium: determination of unidirectional flux using the stable isotopes 6Li and 7Li in an ionic analyzer]

The use of the stable isotopes 6 and 7 of lithium, and detection with the ionic analyser, allow the measurement of unidirectional transepithelial Li-fluxes, between "external" and "internal" solutions which both contain 80% Na and 20% Li. Efflux was found to be bigger than influx. An important lag-phase on the curve, reveals the interference of a Li-compartment, with a high capacity, in the epithelium itself.     

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.     

The metabolism of the male antifertility agent 1-amino-3-chloropropan-2-ol in the rat

Summary The male antifertility agent 1-amino-3-chloropropan-2-ol (ACP,I) has been shown to be metabolized to-chlorohydrin (III) and metabolites of-chlorohydrin. This accounts for the similar antifertility and renal toxicity effects of both compounds.     

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)     

N-(5′-Phosphopyridoxyl)-4-aminobutyric acid: a stable bisubstrate adduct inhibitor of rat brain 4-aminobutyric acid aminotransferase

Summary N-(5-Phosphopyridoxyl)-4-aminobutyric acid, a stable adduct of pyridoxal phosphate and 4-aminobutyric acid, has been shown to be a potent inhibitor of rat brain 4-aminobutyric acid aminotransferase (GABA-T) with a K_i of 1.4 M.Acknowledgments. This work was supported in part by the United Parkinson Foundation, l'Association Canadienne l'Ataxie de Friedreich, and the Medical Research Council of Canada.     

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.     

Occurrence of β-chitin in the cuticle of a Pentastomid Raillietiella gowrii

Summary The purified chitin from the cuticle of a pentastomid was examined by X-ray method. The X-ray photograph discloses that the chitin in question is of -type. Since the arthropod cuticle contains -chitin, it is suggested that Pentastomida may be considered an independent phylum.Thanks are due to Prof. Dr. G. Sundara Rajulu for guidance and encouragement.