Neuroactive steroids and human recombinant ρ1 GABAC receptors

Journal of Pharmacology and Experimental Therapeutics

Volumn 323, Issue 1, 2007, Pages 236-247

  Li, Wenjun ^a   Jin, Xiaochun ^a   Covey, Douglas F ^a   Steinbach, Joe Henry ^a  

^a WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

(3ALPHA,5ALPHA,17ALPHA) 3 HYDROXYANDROSTANE 17 CARBONITRILE; (3ALPHA,5ALPHA,17BETA) 3 HYDROXYANDROSTANE 17 CARBONITRILE; (3ALPHA,5BETA,17ALPHA) 3 HYDROXYANDROSTANE 17 CARBONITRILE; 17ALPHA ESTRADIOL; 3ALPHA HYDROXY 5ALPHA PREGNAN 20 ONE; 3BETA HYDROXY 5BETA PREGNAN 20 ONE; 4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID C RECEPTOR; ALLOPREGNANOLONE SULFATE; ANDROSTERONE; ANDROSTERONE SULFATE; COMPLEMENTARY DNA; COMPLEMENTARY RNA; ELTANOLONE; EPIALLOPREGNANOLONE; EPIALLOPREGNANOLONE SULFATE; EPIPREGNANOLONE SULFATE; EPIPREGNENOLONE; ESTRADIOL; ETHINYLESTRADIOL; ETIOCHOLANOLONE; PICROTOXIN; PRASTERONE SULFATE; PREGNANOLONE SULFATE; PREGNENOLONE; PREGNENOLONE SULFATE; RECOMBINANT PROTEIN; STEROID; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL CELL; ARTICLE; DRUG BINDING SITE; DRUG MECHANISM; DRUG STRUCTURE; ENANTIOMER; MEMBRANE POTENTIAL; MUTATION; NEUROTRANSMISSION; NONHUMAN; NUCLEOTIDE SEQUENCE; OOCYTE; PRIORITY JOURNAL; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; SULFATION; XENOPUS LAEVIS;

ANIMALS; GABA ANTAGONISTS; HUMANS; MOLECULAR STRUCTURE; MUTATION; OOCYTES; PATCH-CLAMP TECHNIQUES; RECEPTORS, GABA; RECOMBINANT PROTEINS; STEREOISOMERISM; STEROIDS; STRUCTURE-ACTIVITY RELATIONSHIP; XENOPUS LAEVIS;

EID: 34548848044     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.107.127365     Document Type: Article

References (48)

1. A receptors: mechanism and involvement of a residue in the M2 region of the alpha subunit. J Physiol 532:673-684.
2. A receptors. J Physiol 558:59-74.
3. A receptor. Mol Pharmacol 71:461-472.
4. Alakuijala A, Alakuijala J, and Pasternack M (2006) Evidence for a functional role of GABA receptors in the rat mature hippocampus. Eur J Neurosci 23:514-520.
5. Belelli D, Herd MB, Mitchell EA, Peden DR, Vardy AW, Gentet L, and Lambert JJ (2006) Neuroactive steroids and inhibitory neurotransmission: mechanisms of action and physiological relevance. Neuroscience 138:821-829.
6. 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 U S A 94:11031-11036.
7. 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.
8. Bormann J (2000) The 'ABC' of GABA receptors. Trends Pharmacol Sci 21:16-19.
9. Carland JE, Moore AM, Hanrahan JR, Mewett KN, Duke RK, Johnston GA, and Chebib M (2004) Mutations of the 2′ proline in the M2 domain of the human GABAC rho1 subunit alter agonist responses. Neuropharmacology 46:770-781.
10. A receptor-mediated current. J Physiol 550:679-691.
11. C receptors. Vision Res 38:1431-1441.
12. Ffrench-Constant RH, Rocheleau TA, Steichen JC, and Chalmers AE (1993) A point mutation in a Drosophila GABA receptor confers insecticide resistance. Nature 363:449-451.
13. Gee KW, Bolger MB, Brinton RE, Coirini H, and McEwen BS (1988) Steroid modulation of the chloride ionophore in rat brain: structure-activity requirements, regional dependence and mechanism of action. J Pharmacol Exp Ther 246:803-812.
14. C receptors in short-term memory formation in young chicks. Neuroscience 131:567-576.
15. Goutman JD and Calvo DJ (2004) Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABA rho 1 receptor. Br J Pharmacol 141:717-727.
16. A channel that abolish block by picrotoxin. Receptors Channels 3:13-20.
17. A receptor. J Neurosci 21:RC136.
18. C receptors: relatively simple transmitter-gated ion channels? Trends Pharmacol Sci 17:319-323.
19. C receptors as drug targets. Curr Drug Targets CNS Neurol Disord 2:260-268.
20. A receptors. Mol Pharmacol 69:2015-2026.
21. C receptor as the mechanism of steroid action. Mol Pharmacol 69:1779-1782.
22. C receptor-mediated inhibition in the retina. Vision Res 44:3289-3296.
23. Mascia MP, Trudell JR, and Harris RA (2000) Specific binding sites for alcohols and anesthetics on ligand-gated ion channels. Proc Natl Acad Sci U S A 97:9305-9310.
24. Mennerick S, He Y, Jiang X, Manion BD, Wang M, Shute A, Benz A, Evers AS, Covey DF, and Zorumski CF (2004) Selective antagonism of 5′-reduced neurosteroid effects at GABAA receptors. Mol Pharmacol 65:1191-1197.
25. Mennerick S, Zeng CM, Benz A, Shen W, Izumi Y, Evers AS, Covey DF, and Zorumski CF (2001) Effects on gamma-aminobutyric acid (GABA)-A receptors of a neuroactive steroid that negatively modulates glutamate neurotransmission and augments GABA neurotransmission. Mol Pharmacol 60:732-741.
26. C receptor subunits in native central neurons. J Neurosci 24:7241-7250.
27. Morris K, 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. Morris KD and Amin J (2004) Insight into the mechanism of action of neuroactive steroids. Mol Pharmacol 66:56-69.
29. Neher E and Steinbach JH (1978) Local anaesthetics transiently block currents through single acetylcholine-receptor channels. J Physiol 277:153-176.
30. A receptor pharmacology of enantiomers of dehydroepiandrosterone sulfate, pregnenolone sulfate, and (3alpha,5beta)-3- hydroxypregnan-20-one sulfate. J Med Chem 41:2604-2613.
31. Pan Y and Qian H (2005) Interactions between rho and gamma2 subunits of the GABA receptor. J Neurochem 94:482-490.
32. A gamma2S, glycine alpha1 and glycine alpha2 receptor subunits in vitro. Eur J Neurosci 12:3137-3145.
33. Paradiso K, Sabey K, Evers AS, Zorumski CF, Covey DF, and Steinbach JH (2000) Steroid inhibition of rat neuronal nicotinic alpha 4 beta 2 receptors expressed in HEK 293 cells. Mol Pharmacol 58:341-351.
34. Paradiso K, Zhang J, and Steinbach JH (2001) The C terminus of the human nicotinic alpha4beta2 receptor forms a binding site required for potentiation by an estrogenic steroid. J Neurosci 21:6561-6568.
35. Phillipps GH (1975) Structure-activity relationships in steroidal anaesthetics. J Steroid Biochem 6:607-613.
36. Pribilla I, Takagi T, Langosch D, Bormann J, and Betz H (1992) The atypical M2 segment of the beta subunit confers picrotoxinin resistance to inhibitory glycine receptor channels. EMBO J 11:4305-4311.
37. C receptors. Mol Pharmacol 67:470-479.
38. Rundström N, Schmieden V, Betz H, Bormann J, and Langosch D (1994) Cyanotriphenylborate: subtype-specific blocker of glycine receptor chloride channels. Proc Natl Acad Sci U S A 91:8950-8954.
39. Sabey K, Paradiso K, Zhang J, and Steinbach JH (1999) Ligand binding and activation of rat nicotinic α4β2 receptors stably expressed in HEK293 cells. Mol Pharmacol 55:58-66.
40. A receptor desensitization. J Neurosci 20:3571-3579.
41. Steinbach JH, Bracamontes J, Yu L, Zhang PN, and Covey DF (2000) Subunit-specific action of an anticonvulsant thiobutyrolactone on recombinant glycine receptors involves a residue in the M2 membrane-spanning region. Mol Pharmacol 58:11-17.
42. 2+ current in adult rat sensory neurons by a steroid that lacks γ-aminobutyric acidmodulatory activity. Mol Pharmacol 54:918-927.
43. A receptor antagonists. J Neurosci 22:3366-3375.
44. Wang TL, Hackam AS, Guggino WB, and Cutting GR (1995) A single amino acid in gamma-aminobutyric acid rho1 receptors affects competitive and noncompetitive components of picrotoxin inhibition. Proc Natl Acad Sci U S A 92:11751-11755.
45. Woodward RM, Polenzani L, and Miledi R (1992) Effects of steroids on γ-aminobutyric acid receptors expressed in Xenopus oocytes by poly(A)- RNA from mammalian brain and retina. Mol Pharmacol 41:89-103.
46. C receptors: a comparison of native versus recombinant receptors. Trends Pharmacol Sci 22:121-132.
47. Zhang D, Pan ZH, Zhang X, Brideau AD, and Lipton SA (1995) Cloning of a gamma-aminobutyric acid type C receptor subunit in rat retina with a methionine residue critical for picrotoxinin channel block. Proc Natl Acad Sci U S A 92:11756-11760.
48. Zheng W, Xie W, Zhang J, Strong JA, Wang L, Yu L, Xu M, and Lu L (2003) Function of gamma-aminobutyric acid receptor/channel rho 1 subunits in spinal cord. J Biol Chem 278:48321-48329.