Insight into the mechanism of action of neuroactive steroids

Molecular Pharmacology

Volumn 66, Issue 1, 2004, Pages 56-69

  Morris, Kendall D W ^a   Amin, Jahanshah ^a  

^a UNIVERSITY OF SOUTH FLORIDA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID RECEPTOR; 5BETA DIHYDROPROGESTERONE; ALLOTETRAHYDRODEOXYCORTICOSTERONE; ANESTHETIC AGENT; CHLORIDE CHANNEL; CORTICOSTERONE DERIVATIVE; ELTANOLONE; ION CHANNEL; ISOLEUCINE; NEUROACTIVE STEROID; SEX HORMONE; STEROID; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING SITE; CHANNEL GATING; CONCENTRATION (PARAMETERS); CONCENTRATION RESPONSE; CONTROLLED STUDY; DESENSITIZATION; DRUG BINDING; DRUG BINDING SITE; DRUG MECHANISM; DRUG POTENTIATION; GABA GATED CHLORIDE CHANNEL; GENE MUTATION; HYDROPHILICITY; KINETICS; NEUROMODULATION; NONHUMAN; OOCYTE; PRIORITY JOURNAL; RHO RECEPTOR CHANNEL; XENOPUS LAEVIS;

5-ALPHA-DIHYDROPROGESTERONE; AMINO ACID SUBSTITUTION; ANIMALS; CORTICOSTERONE; HYDROPHOBICITY; ISOLEUCINE; KINETICS; PREGNANEDIONES; PREGNANOLONE; RECEPTORS, GABA-A; SERINE; XENOPUS LAEVIS;

EID: 3042528656     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.66.1.56     Document Type: Article

References (51)

1. Amin J (1999) A single hydrophobic residue confers barbiturate sensitivity to γ-aminobutyric acid type C receptor. Mol Pharmacol 55:411-423.
2. A receptor needs two homologous domains of the beta-subunit for activation by GABA but not by pentobarbital. Nature (Lond) 366:565-569.
3. Amin J and Weiss DS (1994) Homomeric rho 1 GABA channels: activation properties and domains. Recept Channels 2:227-236.
4. Barker JL, Harrison NL, Lange GD, and Owen DG (1987) Potentiation of gamma-aminobutyric-acid-activated chloride conductance by a steroid anaesthetic in cultured rat spinal neurones. J Physiol 386:485-501.
5. Belelli D, Lambert JJ, Peters JA, Wafford K, and Whiting PJ (1997) The interaction of the general anesthetic etomidate with the gamma-aminobutyric acid type A receptor is influenced by a single amino acid. Proc Natl Acad Sci USA 94:11031-11036.
6. Belelli D, Pau D, Cabras G, Peters JA, and Lambert JJ (1999) A single amino acid confers barbiturate sensitivity upon the GABA rho 1 receptor. Br J Pharmacol 127:601-604.
7. Cantor RS (1997) The lateral pressure profile in membranes: a physical mechanism of general anesthesia. Biochemistry 36:2339-2344.
8. Chebib M and Johnston GA (2000) GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology. J Med Chem 43:1427-1447.
9. A receptors. Brain Res Brain Res Rev 37:91-97.
10. A receptor modulation and anesthesia. J Pharmacol Exp Ther 293:1009-1016.
11. A receptor complex, attenuate pain sensitivity in rats. Brain Research 643:194-203.
12. Girdler SS, Straneva PA, Light KC, Pedersen CA, and Morrow AL (2001) Allopregnanolone levels and reactivity to mental stress in premenstrual dysphoric disorder. Biol Psychiatry 49:788-797.
13. Gray HS, Holt BL, Whitaker DK, and Eadsforth P (1992) Preliminary study of a pregnanolone emulsion (Kabi 2213) for i.v. induction of general anaesthesia. Br J Anaesth 68:272-276.
14. Harrison NL and Simmonds MA (1984) Modulation of the GABA receptor complex by a steroid anaesthetic. Brain Res 323:287-292.
15. A receptor pore-lining M2 segment. Nat Neurosci 4:477-485.
16. A receptor. J Neurosci 21:RC136.
17. Kokate TG, Svensson BE, and Rogawski MA (1994) Anticonvulsant activity of neurosteroids: correlation with γ-aminobutyric acid-evoked chloride current potentiation. J Pharmacol Exp Ther 270:1223-1229.
18. Koltchine VV, Finn SE, Jenkins A, Nikolaeva N, Lin A, and Harrison NL (1999) Agonist gating and isoflurane potentiation in the human γ-aminobutyric acid type A receptor determined by the volume of a second transmembrane domain residue. Mol Pharmacol 56:1087-1093.
19. Kyte J and Doolittle RF (1982) A simple method for displaying the hydrophobic character of a protein. J Mol Biol 157:105-132.
20. A receptors, in Pharmacology of Inhibitory Amino Acid Transmitters (Mohler H ed) Handbook of Experimental Pharmacology, pp 117-140, Springer, Berlin.
21. A receptor channels. Ion Channels 3:315-343.
22. A receptors open? Neuron 12:61-71.
23. A receptor. Mechanism of action and physiological significance. Prog Neurobiol 38:379-395.
24. Majewska MD, Harrison NL, Schwartz RD, Barker JL, and Paul SM (1986) Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor. Science (Wash DC) 232:1004-1007.
25. Mellon SH and Griffin LD (2002) Neurosteroids: biochemistry and clinical significance. Trends Endocrinol Metab 13:35-43.
26. A and glycine receptors. Nature (Lond) 389:385-389.
27. Morris YD, Moorefield CN, and Amin J (1999) Differential modulation of the γ-aminobutyric acid type C receptor by neuroactive steroids. Mol Pharmacol 56:752-759.
28. Morrow AL, Pace JR, Purdy RH, and Paul SM (1990) Characterization of steroid interactions with γ-aminobutyric acid receptor-gated chloride ion channels: evidence for multiple steroid recognition sites. Mol Pharmacol 37:263-270.
29. A receptors. Toxicology Lett 101:193-201.
30. Park-Chung M, Malayev A, Purdy RH, Gibbs TT, and Farb DH (1999) Sulfated and unsulfated steroids modulate gamma-aminobutyric acidA receptor function through distinct sites. Brain Res 830:72-87.
31. A receptor by depressant barbiturates and pregnane steroids. Br J Pharmacol 94:1257-1269.
32. A receptors. Neuropharmacology 32:59-63.
33. A receptors. Neuron 4:759-765.
34. Purdy RH, Morrow AL, Moore PH Jr, and Paul SM (1991) Stress-induced elevations of gamma-aminobutyric acid type A receptor-active steroids in the rat brain. Proc Natl Acad Sci USA 88:4553-4557.
35. C receptors of retinal neurons. Prog Brain Res 131:295-308.
36. Romeo E, Strohle A, Spalletta G, di Michele F, Hermann B, Holsboer F, Pasini A and Rupprecht R (1998) Effects of antidepressant treatment on neuroactive steroids in major depression. Am J Psychiatry 155:910-913.
37. A receptor desensitization. J Neurosci 20:3571-3579.
38. Shimada S, Cutting G, and Uhl GR (1992) γ-Aminobutyric acid A or C receptor? α-Aminobutyric acid rho 1 receptor RNA induces bicuculline-, barbiturate-, and benzodiazepine-insensitive γ-aminobutyric acid responses in Xenopus oocytes. Mol Pharmacol 41:683-687.
39. A receptor subtypes. Trends Pharmacol Sci 21:411-413.
40. Stoffel-Wagner B (2001) Neurosteroid metabolism in the human brain. Eur J Endocrinol 145:669-679.
41. Turner DM, Ransom RW, Yang JS, and Olsen RW (1989) Steroid anesthetics and naturally occurring analogs modulate the gamma-aminobutyric acid receptor complex at a site distinct from barbiturates. J Pharmacol Exp Ther 248:960-966.
42. A receptor single-channel kinetic properties of mouse spinal cord neurons in culture. J Physiol 456:215-245.
43. A receptor alpha subunit: effects on channel gating and regulation by ethanol. Br J Pharmacol 131:296-302.
44. Unwin N (1995) Acetylcholine receptor channel imaged in the open state. Nature (Lond) 373:37-43.
45. A receptors via two distinct and separable mechanisms. Nat Neurosci 3:1274-1281.
46. Weiss DS and Magleby KL (1989) Gating scheme for single GABA-activated Cl-channels determined from stability plots, dwell-time distributions and adjacent-interval durations. J Neurosci 9:1314-1324.
47. Wick MJ, Mihic SJ, Ueno S, Mascia MP, Trudell JR, Brozowski SJ, Ye Q, Harrison NL, and Harris RA (1998) Mutations of γ-aminobutyric acid and glycine receptors change alcohol cutoff: evidence for an alcohol receptor? Proc Natl Acad Sci USA 95:6504-6509.
48. A receptor states at potentiating and activating concentrations. J Neurosci 22:7417-7424.
49. + RNA from mammalian brain and retina. Mol Pharmacol 41:89-103.
50. Ye Q, Koltchine W, Mihic SJ, Mascia MP, Wick MJ, Finn SE, Harrison NL, and Harris RA (1998) Enhancement of glycine receptor function by ethanol is inversely correlated with molecular volume at position α267. J Biol Chem 273:3314-3319.
51. A receptor on the response to a neurosteroid. Eur J Pharmacol 225:321-330.