Decreased agonist sensitivity of human GABAA receptors by an amino acid variant, isoleucine to valine, in the α1 subunit

European Journal of Pharmacology

Volumn 329, Issue 2-3, 1997, Pages 253-257

  Westh Hansen, Svend Erik ^a   Rasmussen, Poul Baad ^b   Hastrup, Svend ^b   Nabekura, Junichi ^c   Noguchi, Kazuo ^c   Akaike, Norio ^c   Witt, Michael Robin ^a   Nielsen, Mogens ^a  

^a Sct Hans Hospital   (Denmark)

^b NOVO NORDISK A S   (Denmark)

^c KYUSHU UNIVERSITY   (Japan)

Author keywords

Electrophysiology; GABAA receptor; Mutation; Radioligand binding; 1 subunit

Indexed keywords

3 AMINO 2 (3 CARBOXYPROPYL) 6 (4 METHOXYPHENYL)PYRIDAZINIUM BROMIDE; 4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; BENZODIAZEPINE RECEPTOR; BICUCULLINE METHIODIDE; COMPLEMENTARY DNA; GABOXADOL; ISOLEUCINE; MUSCIMOL; RADIOLIGAND; RECEPTOR SUBUNIT; VALINE;

AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; AMINO TERMINAL SEQUENCE; ANIMAL CELL; ARTICLE; BACULOVIRUS; CELL LINE; CHLORIDE CURRENT; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG INHIBITION; DRUG POTENCY; DRUG RECEPTOR BINDING; ELECTROPHYSIOLOGY; GENE EXPRESSION; HUMAN; INSECT; NONHUMAN; PRIORITY JOURNAL; PROTEIN VARIANT; RECEPTOR AFFINITY; RECEPTOR SENSITIVITY;

BACULOVIRIDAE; CELL LINE; DNA PRIMERS; GABA AGONISTS; GABA ANTAGONISTS; HUMANS; ISOLEUCINE; PATCH-CLAMP TECHNIQUES; POINT MUTATION; PYRIDAZINES; RECEPTORS, GABA-A; RECOMBINANT PROTEINS; VALINE;

EID: 0030975014     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(97)89186-8     Document Type: Article

References (6)

1. A receptor needs two homologous domains of the β-subunit for activation by GABA but not by penlobarbital. Nature 366, 565-569.
2. Amin, J., Dickerson, I.M., Weiss, D.S., 1994. The agonist binding site of the gamma-aminobutyric acid type A channel is not formed by the extracellular cysteine loop. Mol. Pharmacol. 45, 317-323.
3. Aprison, M.H., Galvez-Ruano, E., Robertson, D.H., Lipkowitz, K.B., 1996. Glycine and GABA receptors: molecular mechanisms controlling chloride ion flux. J. Neurosci. Res. 43, 372-381.
4. A receptors in insect cells using baculovirus expression vectors. Neuroreport 3, 597-600.
5. A receptors expressed under optimized conditions. J. Membr. Biol. 121, 195-202.
6. Bureau. M., Olsen, R.W., 1988. γ-Aminobutyric acid/benzodiazepine receptor complex carries binding sites for both ligands on both two major peptide subunits. Biochem. Biophys. Res. Commun. 153. 1006-1011.