Natural and enantiomeric etiocholanolone interact with distinct sites on the rat α1β2γ2L GABAA receptor

Molecular Pharmacology

Volumn 71, Issue 6, 2007, Pages 1582-1590

  Li, Ping ^a   Bracamontes, John ^a   Katona, Bryson W ^a   Covey, Douglas F ^a   Steinbach, Joe Henry ^a   Akk, Gustav ^a,b  

^a WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b WASHINGTON UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA1; 4 AMINOBUTYRIC ACID A RECEPTOR BETA2; 4 AMINOBUTYRIC ACID A RECEPTOR GAMMA2L; ETIOCHOLANOLONE; RECEPTOR SUBUNIT; UNCLASSIFIED DRUG;

ARTICLE; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG RECEPTOR BINDING; EMBRYO; ENANTIOMER; GENE MUTATION; HORMONE ACTION; HUMAN; HUMAN CELL; KINETICS; PRIORITY JOURNAL; PROTEIN EXPRESSION;

ANIMALS; DRUG SYNERGISM; ELECTROPHYSIOLOGY; ETIOCHOLANOLONE; KINETICS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GABA-A; STEREOISOMERISM; STEROIDS;

EID: 34347356591     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.106.033407     Document Type: Article

References (22)

1. Akk G (2002) Contributions of the non-α subunit residues (loop D) to agonist binding and channel gating in the muscle nicotinic acetylcholine receptor. J Physiol 544:695-705.
2. A receptors: mechanism and involvement of a residue in the M2 region of the α subunit. J Physiol 532:673-684.
3. A receptors. J Physiol 558:59-74.
4. A receptor. J Neurosci 25:11605-11613.
5. A receptor modulation and anesthesia. J Pharmacol Exp Ther 293:1009-1116.
6. Einhauer A and Jungbauer A (2001) The FLAG peptide, a versatile fusion tag for the purification of recombinant proteins. J Biochem Biophys Methods 49:455-465.
7. A receptor. Eur J Pharmacol 269:157-163.
8. Herzog AG, Seibel MM, Schomer DL, Vaitukaitis JL, and Geschwind N (1986) Reproductive endocrine disorders in men with partial seizures of temporal lobe origin. Arch Neurol 43:347-350.
9. A receptors through two discrete transmembrane sites. Nature (Lond) 444:486-489.
10. Kaminski RM, Marini H, Kim WJ, and Rogawski MA (2005) Anticonvulsant activity of androsterone and etiocholanolone. Epilepsia 46:819-827.
11. A receptors by ent-androgens. Eur J Med Chem, in press.
12. A receptors. Mol Pharmacol 69:2015-2026.
13. Li W, Covey DF, Alakoskela JM, Kinnunen PKJ, and Steinbach JH (2006b) Enantiomers of neuroactive steroids support a specific interaction with the GABA-C receptor as the mechanism of steroid action. Mol Pharmacol 69:1779-1782.
14. Paradiso K, Zhang J, and Steinbach JH (2001) The C terminus of the human nicotinic α4β2 receptor forms a binding site required for potentiation by an estrogenic steroid. J Neurosci 21:6561-6568.
15. A receptor at sites on the N-terminal side of the middle of TM2. Neuroreport 9:379-383.
16. Qin F, Auerbach A, and Sachs F (1996) Estimating single-channel kinetic parameters from idealized patch-clamp data containing missed events. Biophys J 70:264-280.
17. A receptor gating by pentobarbital. J Physiol 537:715-733.
18. 2+ current in adult rat sensory neurons by a steroid that lacks γ-aminobutyric acid-modulatory activity. Mol Pharmacol 54:918-927.
19. A receptor single-channel kinetic properties of mouse spinal cord neurons in culture. J Physiol 456:215-245.
20. A receptors expressed in human embryonic kidney 293 cells. Mol Pharmacol 50:931-938.
21. Watters JM, Bessey PQ, Dinarello CA, Wolff SM, and Wilmore DW (1985) The induction of interleukin-1 in humans and its metabolic effects. Surgery 98:298-306.
22. A receptor modulation and anesthesia. Mol Pharmacol 50:1581-1586.