GABA high affinity

GABA (high affinity) Palacios a/., 1981c Young and Kuhar, 1979d, 19805... 

Abalis, I.M., Eldefrawi, M.E., and Eldefrawi, A.T. (1985). High affinity stereospecific binding of cyclodiene insecticides and gamma HCH to GABA receptors in rat brain. Pesticide Biochemistry and Physiology, 24, 95-102. 

Fig. 2. Agents controlling the opening of Cl -channels. The structural formula, the name, the respeetive Cl -channel, and an appropriate reference are provided. (A) Note the similarity of GABA, taurine, and P-alanine. Note also that DPC and its analogues such as NPPB contain a -alanine backbone. (B) The structure of torasemide comes close to both DPC and furosemide or buraetanide. It blocks the Na ZCPK" -cotransporter with very high affinity and with lesser affinity also the TAL-Cl -channel. Note that IAA-94 is related to phenoxyaeetic acids (e.g., ethacrynic acid). Amidine is related to IAA-94 but it has a positive net charge. Amidine as well as IAA-94 block the ICOR channel at around lO mol/1 [63].

Larsson, O. M., Krogsgaard-Larsen, R, and Schousboe, A. (1980) High-affinity uptake of (RS)-nipecotic acid in astrocytes cultured from mouse brain. Comparison with GABA transport. J. Neurochem. 34, 970-977. 

Schousboe, A. (1979) Effects of GABA-analogues on the high-affinity uptake of GABA in astrocytes in primary cultures. Adv. Exp. Med. Biol. 123, 219-237. 

Miller, J. W Kleven, D. T., Domin, B. A., and Fremau Jr., R. T. (1997) Cloned sodium-land chloride-) dependent high affinity transporters for GABA, glycine, proline, betaine, taurine, and creatine, in Neurotransmitter Transporters Structure, Function, and Regulation (Reith, M. E. A., ed.). Humana Press, Totowa, NJ, pp. 101-150. 

Buspirone is an extremely specific drug that could possibly represent a new chemical class of anxiolytics—azaspirones. As an anxiolytic, its activity is equal to that of benzodiazepines however, it is devoid of anticonvulsant and muscle relaxant properties, which are characteristic of benzodiazepines. It does not cause dependence or addiction. The mechanism of its action is not conclusively known. It does not act on the GABA receptors, which occurs in benzodiazepine use however, it has a high affinity for seratonin (5-HT) receptors and a moderate affinity for dopamine (D2) receptors. Buspirone is effective as an anxiolytic. A few side effects of buspirone include dizziness, drowsiness, headaches, nervousness, fatigue, and weakness. This drug is intended for treatment of conditions of anxiety in which stress, muscle pain, rapid heart rate, dizziness, fear, etc. are observed in other words, conditions of anxiety not associated with somewhat common, usual, and everyday stress. Synonyms for buspirone are anizal, axoren, buspar, buspimen, buspinol, narol, travin, and others. 

---