Electron-donating properties of phenothiazine and related compounds

Bloor, J. E.; Gilson, Bruce R.; Haas, R.; Zirkle, Charles L.

doi:10.1021/jm00299a029

Cited by 43 publications

(16 citation statements)

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“…An additional explanation for our findings is given by the fact that phenothiazines, par ticularly thioproperazines, act as electron donors (22,23). Thioproperazine shows only little inhibition of our system at low concen trations of serine but activates it at higher tion of 14C-glycine.…”

Section: Resultsmentioning

confidence: 63%

Influence of Phenothiazines or Reserpine on the Formation of 14C-Glycine from U-14C-Serine

Gründig¹,

Birnbaumer²,

Hawrylewicz³

1981

Enzyme

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The influence of the psychopharmaceuticals reserpine, thioproperazine and chlorpromazine on the synthesis of 14C-glycine from U-l4C-serine was examined in a rat brain preparation. At low serine concentration (2 • 10^-5 mol/l) glycine synthesis is inhibited by all drugs tested, probably due to the inhibition of the serine influx into mitochondria. At higher concentration (10^-3 mol/l) and physiological cofactor levels, phenothiazines increase to the measurable amount of 14C-glycine while reserpine has no effect. We assume that at this higher concentration serine transport through the mitochondrial membranes is no longer rate limiting; following phenothiazine action, the membrane-bound glycine cleavage system might be inhibited more strongly than the partly soluble serine hydroxymethyltransferase.

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Section: Resultsmentioning

confidence: 63%

Influence of Phenothiazines or Reserpine on the Formation of 14C-Glycine from U-14C-Serine

Gründig¹,

Birnbaumer²,

Hawrylewicz³

1981

Enzyme

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“…A single methyl group added to PE (PE Me) sees a 28% increase in hydration while successive methylations increase the hydration by 7% and 16%, respectively. 46,47 Such hydration increases are also seen for successive methylations of dioctanoyl-PE and dimyristoyl-PE. [48][49][50] We thus infer that full PL hydration is observed in all our experiments.…”

Section: Inuence Of the Headgroupmentioning

confidence: 97%

Molar ratios of therapeutic water-soluble phenothiazine·water-insoluble phospholipid adducts reveal a Fibonacci correlation and a putative link for structure–activity relationships

et al. 2015

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“…This dye has a superior donor character than many of the amines and N-heterocycles such as triphenylamine, phenoxazine, carbazole, etc. 26,27 The versatility of its core, derived from the multiple modifiable active sites and the facile tunability into various states (such as neutral, cation radical, and oxygenated sulfoxide forms), allows functionalizing it with a variety of substituents and generate a plethora of derivatives with tuneable optoelectronic properties. For instance, D-A chromophores can be built by covalently attaching electron-withdrawing (EW) or donating groups at C-3 and C-7 positions.…”

Section: Modifications Of the Phenothiazine Corementioning

confidence: 99%