Ol out-of-plane bend 0 Frequencies in cm-1, estimated accuracy ±5 cm-1. Frequencies for C-D vibrations are given in italics. 6 Aromatic and olefinic are abbreviated as Ar and Ol, respectively.

Fluorenone-Photosensitized Isomerization of tra/z.s-Stilbene. Inefficiencies both in Intersystem Crossing and in Triplet Excitation Transfer Sir:The quantum yield of isomerization of trazzs-stilbene sensitized in benzene by fluorenone has been reported1 to be 0.41. This quantum yield is markedly lower than the quantum yield, 5 :, predicted from the previously measured2 intersystem crossing quantum yield 5 = 0.93 for fluorenone in benzene and the known1 decay fraction a = 0.59 for stilbene tripletcz's-stilbene.

This study assessed the toxicity and mode of action of a new experimental insecticide, LY219048 in insects and mammals. LY219048 produced rapid convulsions in mice and had LD50 values of 0.7 mg kg−1 and 4 mg kg−1 after intracerebral and intraperitoneal injection, respectively. In initial screens against insects, LY219048 showed low activity against the German cockroach (Blatella germanica L.). Lethality from dietary exposure required one to two weeks, even at concentrations as high as 10000 mg kg−1 (LC50 = 485 mg kg−1). In contrast, it had an LC50 value of 8.3 mg kg−1 against insecticide‐susceptible Drosophila melanogaster (Meig.) when synergized with piperonyl butoxide. Significant resistance to LY219048 (> 12‐fold) was detected in a cyclodiene‐resistant strain of D. melanogaster possessing an altered target site resistance mechanism. This finding suggested that LY219048 blocked the 4‐aminobutyric acid (GABA)‐gated chloride channel in a manner similar to that of the cyclodienes. In physiological studies in larval D. melanogaster central neurons, LY219048 antagonized the reduction of firing caused by 1 mM GABA. Dose‐response experiments showed that the ED50 for blocking inhibition under these conditions was c. 1 μ. Studies of 36CI uptake into bovine brain synaptosomes found that LY219048 was a potent antagonist. At 10 μ it completely blocked chloride flux stimulated by 50 μM GABA. LY219048 competitively displaced [3H]TBOB binding from bovine brain membranes, with an IC50 of 42 nM, which was comparable to values determined for TBPS (35 nM) and picrotoxinin (267 nM). There was little or no displacement (<25%) of [3H]flunitrazepam or [3H]muscimol binding by 10 μM LY219048. Taken together, these results provide strong evidence that this new chemical class of insecticide manifests its acute toxicity by blocking the GABA‐gated chloride channel.

5‐Amino‐1‐aryl‐1H‐pyrazole‐4‐carboxylate esters are converted to the corresponding desamino, chloro, bromo, iodo, and methylthio esters by processes involving nonaqueous diazotization. Diazotizing agents are alkyl nitrites except in the case of chlorine where nitrosyl chloride is used. Evidence is presented that the latter reagent leads to the formation of cationic rather than radical intermediates.

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