Loescher, W.’s team published research in Neuropharmacology in 24 | CAS: 3115-28-4

Neuropharmacology published new progress about 3115-28-4. 3115-28-4 belongs to catalysis-chemistry, auxiliary class Aliphatic Chain, name is 2-Butylhexanoic acid, and the molecular formula is C10H20O2, SDS of cas: 3115-28-4.

Loescher, W. published the artcilePharmacological evaluation of various metabolites and analogs of valproic acid. Anticonvulsant and toxic potencies in mice, SDS of cas: 3115-28-4, the publication is Neuropharmacology (1985), 24(5), 427-35, database is CAplus and MEDLINE.

Thirty-two metabolites and analogs of the antiepileptic drug valproic acid (2-propylpentanoic acid) (VPA) were tested for anticonvulsant and toxic effects in mice, in an attempt to find out if any of these compounds were more potent than valproic acid. Valproic acid and ethosuximide, another clin. established antiepileptic drug, were included in these studies for comparison. After i.p. administration, the anticonvulsant potency of the various drugs was determined in 3 seizure tests: the threshold for maximal electroconvulsants, the maximal electroshock seizure test and seizures induced by s.c. injection of pentylenetetrazole. For the most potent compounds median minimal neurotoxic doses (TD50s) and LD50s (after i.p. and i.v. injection) were determined Valpramide??[2430-27-5], the primary amide of valproic acid, proved to be the most potent compound in the 3 seizure tests, used, being 2-5 times as potent as valproic acid, but valpramide was also considerably more sedative and toxic than valproic acid or ethosuximide. Of the metabolites of valproic acid tested, the unsaturated compounds 4-en-valproic?acid (4-en-VPA) [1575-72-0] and the trans-isomer of 2-en-valproic acid (2-en-VPA) [33786-47-9] were the most potent and, depending on the seizure test used, reached 60-100% of the efficacy of the parent drug. Both metabolites had LD50 values which were similar or greater than those of valproic acid but they were more sedative than the parent compound Analogs of valproic acid with shorter side-chain lengths were only weakly active as anticonvulsants, whereas elongation of the side-chains led to increases in anticonvulsant cyclic compounds in which the side-chains have been closed to a ring were inactive or only weakly active. However, addition of a Me group in position 1 at the ring of cyclohexanoic acid markedly increased the anticonvulsant potency without altering LD50 values. Similarly, introduction of an addnl. branching with a Me group at C2 of analogs of valproic acid led to considerable enhancement of anticonvulsant effectiveness. Although these methyl substituted compounds were more sedative than valproic acid, they seem to be interesting tools with regard to the structural prerequisites of anticonvulsant, toxic and teratogenic effects of branched fatty acids.

Neuropharmacology published new progress about 3115-28-4. 3115-28-4 belongs to catalysis-chemistry, auxiliary class Aliphatic Chain, name is 2-Butylhexanoic acid, and the molecular formula is C10H20O2, SDS of cas: 3115-28-4.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia