3β-Hydroxypregnane Steroids Are Pregnenolone Sulfate-Like GABA A Receptor Antagonists

Journal of Neuroscience

Volumn 22, Issue 9, 2002, Pages 3366-3375

  Wang, Mingde ^a,b   He, Yejun ^a   Eisenman, Lawrence N ^a   Fields, Christopher ^a   Zeng, Chun Min ^a   Mathews, Jose ^a   Benz, Ann ^a   Fu, Tao ^a   Zorumski, Erik ^a   Steinbach, Joe Henry ^a   Covey, Douglas F ^a   Zorumski, Charles F ^a   Mennerick, Steven ^a  

^a WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b UMEÅ UNIVERSITY   (Sweden)

Author keywords

Anesthetic; GABAA receptors; Hippocampal culture; Inhibitory postsynaptic current; Neurosteroids; Pregnenolone sulfate

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; PREGNANE DERIVATIVE; PREGNENOLONE SULFATE; 4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID RECEPTOR BLOCKING AGENT; BENZODIAZEPINE RECEPTOR AFFECTING AGENT; FLUMAZENIL; HYDROXYSTEROID; LORAZEPAM; PREGNENOLONE; PROTEIN SUBUNIT;

ANIMAL TISSUE; ARTICLE; COMPETITIVE INHIBITION; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG ANTAGONISM; DRUG POTENTIATION; HORMONAL REGULATION; MEMBRANE CURRENT; NEUROTRANSMISSION; NEWBORN; NONHUMAN; PRIORITY JOURNAL; RAT; REDUCTION; AMINO ACID SUBSTITUTION; ANIMAL; CELL CULTURE; DOSE RESPONSE; DRUG EFFECT; GENETICS; METABOLISM; OOCYTE; PATCH CLAMP; SPRAGUE DAWLEY RAT; STRUCTURE ACTIVITY RELATION; SYNAPSE; XENOPUS LAEVIS;

AMINO ACID SUBSTITUTION; ANIMALS; CELLS, CULTURED; DOSE-RESPONSE RELATIONSHIP, DRUG; FLUMAZENIL; GABA ANTAGONISTS; GABA MODULATORS; GAMMA-AMINOBUTYRIC ACID; HYDROXYSTEROIDS; LORAZEPAM; OOCYTES; PATCH-CLAMP TECHNIQUES; PREGNANES; PREGNENOLONE; PROTEIN SUBUNITS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GABA-A; STRUCTURE-ACTIVITY RELATIONSHIP; SYNAPSES; XENOPUS LAEVIS;

EID: 0036584255     PISSN: 02706474     EISSN: None     Source Type: Journal    
DOI: 10.1523/jneurosci.22-09-03366.2002     Document Type: Article

References (36)

1. A receptors: mechanism and involvement of a residue in the M2 region of the a subunit. J Physiol (Lond) 532:673-684.
2. Barker JL, Harrison NL, Lange GD, Owen DG (1987) Potentiation of gamma-aminobutyric-acid-activated chloride conductance by a steroid anaesthetic in cultured rat spinal neurones. J Physiol (Lond) 386:485-501.
3. Bekkers JM, Stevens CF (1991) Excitatory and inhibitory autaptic currents in isolated hippocampal neurons maintained in cell culture. Proc Natl Acad Sci USA 88:7834-7838.
4. A receptors. Brain Res Brain Res Rev 37:91-97.
5. A receptor. Neuroscience 45:127-135.
6. Garrett KM, Gan J (1998) Enhancement of gamma-aminobutyric acidA receptor activity by alpha-chloralose. J Pharmacol Exp Ther 285:680-686.
7. Gasior M, Carter RB, Witkin JM (1999) Neuroactive steroids: potential therapeutic use in neurological and psychiatric disorders. Trends Pharmacol Sci 20:107-112.
8. A receptors. J Med Chem 39:4218-4232.
9. A channel responses to brief agonist pulses. Neuron 15:181-191.
10. Jones MV, Westbrook GL (1997) Shaping of IPSCs by endogenous calcineurin activity. J Neurosci 17:7626-7633.
11. Kokate TG, Svensson BE, Rogawski MA (1994) Anticonvulsant activity of neurosteroids: correlation with gamma-aminobutyric acid-evoked chloride current potentiation. J Pharmacol Exp Ther 270:1223-1229.
12. A receptors. In: Handbook of experimental pharmacology (Mohler H, ed), pp 117-140. Berlin: Springer.
13. A receptor in pituitary melanotrope cells. Eur J Pharmacol 331:303-311.
14. A receptor channels. Annu Rev Neurosci 17:569-602.
15. A receptors open? Neuron 12:61-71.
16. A receptor isoforms. Can J Physiol Pharmacol 76:909-920.
17. A receptor. Mechanism of action and physiological significance. Prog Neurobiol 38:379-395.
18. Majewska MD, Mienville JM, Vicini S (1988) Neurosteroid pregnenolone sulfate antagonizes electrophysiological responses to GABA in neurons. Neurosci Lett 90:279-284.
19. Mennerick S, Que J, Benz A, Zorumski CF (1995) Passive and synaptic properties of neurons grown in microcultures and in mass cultures. J Neurophysiol 73:320-332.
20. A receptors of a neuroactive steroid that negatively modulates glutamate neurotransmission and augments GABA neurotransmission. Mol Pharmacol 60:732-741.
21. A receptor-mediated currents via a reduction of channel opening frequency. Brain Res 489:190-194.
22. Park-Chung M, Wu FS, Purdy RH, Malayev AA, Gibbs TT, Farb DH (1997) Distinct sites for inverse modulation of N-methyl-D-aspartate receptors by sulfated steroids. Mol Pharmacol 52:1113-1123.
23. Park-Chung M, Malayev A, Purdy RH, Gibbs TT, Farb DH (1999) Sulfated and unsulfated steroids modulate gamma-aminobutyric acidA receptor function through distinct sites. Brain Res 830:72-87.
24. A receptor complex in avian CNS. Neurochem Res 22:221-225.
25. A receptor-mediated IPSCs by neuroactive steroids in a rat hypothalamohypophyseal coculture model. J Physiol (Lond) 500:475-485.
26. A receptor-complex. Neurosci Lett 135:273-275.
27. A receptors. Neuropharmacology 32:59-63.
28. A receptors. Neuron 4:759-765.
29. Robel P, Baulieu E-E (1994) Neurosteroids:biosynthesis and function. In: Neurobiology of steroids: methods in the neurosciences 22 (de Kloet R, Sutanto W, eds), pp 36-50. San Diego: Academic.
30. A receptor desensitization. J Neurosci 20:3571-3579.
31. Turner DM, Ransom RW, Yang JS, 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.
32. Wang MD, Backstrom T, Landgren S (2000) The inhibitory effects of allopregnanolone and pregnanolone on the population spike, evoked in the rat hippocampal CA1 stratum pyramidale in vitro, can be blocked selectively by epiallopregnanolone. Acta Physiol Scand 169:333-341.
33. Woodward RM, Polenzani L, Miledi R (1992) Effects of steroids on gamma-aminobutyric acid receptors expressed in Xenopus oocytes by poly(A)+ RNA from mammalian brain and retina. Mol Pharmacol 41:89-103.
34. A receptor on the response to a neurosteroid. Eur J Pharmacol 225:321-330.
35. A receptors. Chem Abstr 2001:640035.
36. Zorumski CF, Mennerick SJ, Covey DF (1998) Enantioselective modulation of GABAergic synaptic transmission by steroids and benz[e]indenes in hippocampal microcultures. Synapse 29:162-171.