Detail of "35989-16-3"

Reference

Effects of N-methylamino acids and convulsants on spontaneous action potentials in guinea pig cerebellar slices

Effects of N-methylamino acids and convulsants on spontaneous action potentials in guinea pig cerebellar slices. Okamoto, K.; Quastel, J. H. (Div. Neurol. Sci., Univ. British Columbia, Vancouver, B. C., Can.). Br. J. Pharmacol., 59(4), 551-60 (English) 1977. CODEN: BJPCBM. DOCUMENT TYPE: Journal CA Section: 2 (Hormone Pharmacology) Section cross-reference(s): 1 N-methyl-GABA [1119-48-8], N-methylglycine [107-97-1], N-methyltaurine [107-68-6], and N-methyl-.beta.-alanine [2679-14-3] diminished the frequency of spontaneous spike discharges in guinea pig cerebellar slices. The convulsants, picrotoxin [124-87-8] and strychnine [57-24-9] antagonized the inhibitory actions of all the amino acids except N-methylglycine, which was only antagonized by strychnine. N-methyl-DL-glutamate (I) [35989-16-3] caused a strong inhibition followed by a strong excitation of the neurons, and both convulsants completely suppressed the inhibitory effects but had no effect on the excitation. The no. of amino acid mols. combining with the receptor site to produce a response was 3, 2, 3, 3, and 1 for N-methyl-GABA, N-methylglycine, N-methyltaurine, N-methyl-.beta.-alanine, and I resp. The no. of convulsant mols. combining with the receptor site was 2 for picrotoxin with N-methyl-GABA, N-methyl-.beta.-alanine, and I and 1 for strychnine with all the amino acids.

Excitant activity of methyl derivatives of quinolinic acid on rat cortical neurons

Excitant activity of methyl derivatives of quinolinic acid on rat cortical neurons. Stone, Trevor W. (Med. Sch., St. George's Hosp.Chemicals with cas numbers 85797-13-3 and 89-00-9 also play role., London SW17 0RE, UK). Br. J. Pharmacol., 81(1), 175-81 (English) 1984. CODEN: BJPCBM. ISSN: 0007-1188. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2 Various synthetic quinolinic acid analogs were tested for agonist and antagonist properties when applied by microiontophoresis to neurons in the rat cerebral cortex. Quinolinic acid 2-Me ester [24195-07-1] was a weak antagonist of N-methyl-D-aspartate (NMDA) [6384-92-5] and quinolinic acid [89-00-9] but also showed agonist activity, being about 50% as active as quinolinic acid. The excitant effects of the compd. could be antagonized by the NMDA receptor blocker, (±)-2-amino-7-phosphonoheptanoic acid (2APH) [78966-69-5]. N-Methylquinolinic acid 2,3-di-Me ester [73834-99-8] showed very weak agonist and antagonist activity. Homoquinolinic acid [490-75-5] was a potent excitant of cortical neurons, being about 5-times more active than quinolinic acid and approx. equipotent with NMDA. The excitations were blocked by 2APH or its pentanoate analog (±)-2-amino-5-phosphono valeric acid [76326-31-3]. Homoquinolinic acid 2-Me ester [89353-64-0] was also active as an agonist. N-Methyl-DL-glutamic acid [35989-16-3] caused excitation of 5 of the 16 units tested; N-methylglutamate was a weaker agonist than NMDA or homoquinolinate. Phthallic acid [88-99-3], caused excitation of 14 out of 16 units. Thus, the ring nitrogen of quinolinic acid is not essential for excitant activity. Since homoquinolinic acid is a rigid analog of glutamic acid, but causes excitation by acting apparently on the NMDA receptor, the results are consistent with the suggestion that activation of the NMDA receptor may require the carboxyl groups to be held in a relatively extended configuration. .