Structurally diverse amphiphiles exhibit biphasic modulation of GABA A receptors: Similarities and differences with neurosteroid actions

British Journal of Pharmacology

Volumn 160, Issue 1, 2010, Pages 130-141

  Chisari, M ^a   Shu, H J ^a   Taylor, A ^a   Steinbach, J H ^a   Zorumski, C F ^a   Mennerick, S ^a  

^a WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Amphiphiles; Current modulation; GABA A receptors; Neurosteroid

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; AMPHOPHILE; CAPSAICIN; DOCOSAHEXAENOIC ACID; DODECYL SULFATE SODIUM; NEUROSTEROID; TRITON X 100;

ANIMAL CELL; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG BINDING SITE; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG SPECIFICITY; DRUG STRUCTURE; ELECTRIC CURRENT; ELECTRIC POTENTIAL; FEMALE; NEUROMODULATION; NONHUMAN; OOCYTE; PRIORITY JOURNAL; PROTEIN QUATERNARY STRUCTURE; XENOPUS LAEVIS;

ANIMALS; CAPSAICIN; DOCOSAHEXAENOIC ACIDS; DRUG INTERACTIONS; FEMALE; GABA MODULATORS; GLUCOSIDES; MUTATION; NEUROTRANSMITTER AGENTS; OCTOXYNOL; OOCYTES; RECEPTORS, GABA-A; SODIUM DODECYL SULFATE; STRUCTURE-ACTIVITY RELATIONSHIP; SURFACE-ACTIVE AGENTS; XENOPUS LAEVIS;

EID: 77950925086     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2010.00679.x     Document Type: Article

References (36)

1. Adams PR (1976). Drug blockade of open end-plate channels. J Physiol (Lond) 260 : 531 552.
2. A receptors: mechanism and involvement of a residue in the M2 region of the α subunit. J Physiol (Lond) 532 : 673 684.
3. A receptor. J Neurosci 25 : 11605 11613.
4. A receptor α1 subunit M1 domain reveal unexpected complexity for modulation by neuroactive steroids. Mol Pharmacol 74 : 614 627.
5. Alexander SPH, Mathie A, Peters JA (2009). Guide to Receptors and Channels (GRAC), 4th edn. Br J Pharmacol 158 (Suppl. 1 S1 S254.
6. Baulieu EE, Robel P, Schumacher M (2001). Neurosteroids: beginning of the story. Int Rev Neurobiol 46 : 1 32.
7. A receptor. Nat Rev Neurosci 6 : 565 575.
8. A receptor modulation: evidence for a low affinity interaction. J Neurophysiol 102 : 1254 1264.
9. A and glutamate receptors: relation to in vivo effects. Br J Pharmacol 118 : 378 384.
10. A receptor-mediated current. J Physiol 550 : 679 691.
11. Gasior M, Carter RB, Witkin JM (1999). Neuroactive steroids: potential therapeutic use in neurological and psychiatric disorders. Trends Pharmacol Sci 20 : 107 112.
12. 2P channels: focus on TREK1. Nat Rev Neurosci 8 : 251 261.
13. A receptors through two discrete transmembrane sites. Nature 444 : 486 489.
14. Huettner JE, Bean BP (1988). Block of N-methyl-D-aspartate-activated current by the anticonvulsant MK-801: selective binding to open channels. Proc Natl Acad Sci USA 85 : 1307 1311.
15. Inoue M, Akaike N (1988). Blockade of gamma-aminobutyric acid-gated chloride current in frog sensory neurons by picrotoxin. Neurosci Res 5 : 380 394.
16. 3 receptors in N1E-115 neuroblastoma cells. Br J Pharmacol 117 : 1507 1515.
17. A receptor by the marine cembranoid eupalmerin acetate. Br J Pharmacol 153 : 598 608.
18. C receptor as the mechanism of steroid action. Mol Pharmacol 69 : 1779 1782.
19. Lundbaek JA, Birn P, Girshman J, Hansen AJ, Andersen OS (1996). Membrane stiffness and channel function. Biochem 35 : 3825 3830.
20. Majewska MD, Mienville JM, Vicini S (1988). Neurosteroid pregnenolone sulfate antagonizes electrophysiological responses to GABA in neurons. Neurosci Lett 90 : 279 284.
21. A receptors of a neuroactive steroid that negatively modulates glutamate neurotransmission and augments GABA neurotransmission. Mol Pharmacol 60 : 732 741.
22. Neher E, Steinbach JH (1978). Local anesthetics transiently block currents through single acetylcholine-receptor channels. J Physiology 277 : 153 176.
23. Newland CF, Cull-Candy SG (1992). On the mechanism of action of picrotoxin on GABA receptor channels in dissociated sympathetic neurones of the rat. J Physiol (Lond) 447 : 191 213.
24. A receptor pharmacology of enantiomers of dehydroepiandrosterone sulfate, pregnenolone sulfate, and (3α,5β)-3- hydroxypregnan-20-one sulfate. J Med Chem 41 : 2604 2613.
25. A receptor function through distinct sites. Brain Res 830 : 72 87.
26. + channel. EMBO J 17 : 4283 4290.
27. A receptor gating depends on extracellular pH. Neuroreport 16 : 1951 1954.
28. A receptor function is regulated by lipid bilayer elasticity. Biochemistry 45 : 13118 13129.
29. A receptors in Xenopus oocytes. Biochim Biophys Acta 1788 : 1073 1080.
30. Twede VD, Covey DF, Tartaglia AL, Bamber BA (2007). The neurosteroids dehydroepiandrosterone sulfate and pregnenolone sulfate inhibit the UNC-49 GABA receptor through a common set of residues. Mol Pharmacol 72 : 1322 1329.
31. A receptor antagonists. J Neurosci 22 : 3366 3375.
32. Wood SC, Forman SA, Miller KW (1991). Short chain and long chain alkanols have different sites of action on nicotinic acetylcholine receptor channels from Torpedo. Mol Pharmacol 39 : 332 338.
33. Yang L, Sonner JM (2008). Anesthetic-like modulation of receptor function by surfactants: a test of the interfacial theory of anesthesia. Anesth Analg 107 : 868 874.
34. Yoon KW, Covey DF, Rothman SM (1993). Multiple mechanisms of picrotoxin block of GABA-induced currents in rat hippocampal neurons. J Physiol (Lond) 464 : 423 439.
35. Zorumski CF, Mennerick S, Isenberg KE, Covey DF (2000). Potential clinical uses of neuroactive steroids. Idrugs 3 : 1053 1063.
36. Zuo Y, Aistrup GL, Marszalec W, Gillespie A, Chavez-Noriega LE, Yeh JZ et al. (2001). Dual action of n-alcohols on neuronal nicotinic acetylcholine receptors. Mol Pharmacol 60 : 700 711.