Chronic treatment with the neuroactive steroid ganaxolone in the rat induces anticonvulsant tolerance to diazepam but not to itself

Journal of Pharmacology and Experimental Therapeutics

Volumn 295, Issue 3, 2000, Pages 1241-1248

  Reddy, Doodipala S ^a   Rogawski, Michael A ^a  

^a NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3ALPHA HYDROXY 5ALPHA PREGNAN 20 ONE; 4 AMINOBUTYRIC ACID A RECEPTOR; DIAZEPAM; GANAXOLONE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTICONVULSANT ACTIVITY; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG CROSS TOLERANCE; DRUG EXPOSURE; DRUG POTENCY; DRUG TOLERANCE; FEMALE; LONG TERM EXPOSURE; NONHUMAN; PRIORITY JOURNAL; RAT; SEIZURE;

ANIMALS; ANTICONVULSANTS; DIAZEPAM; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG TOLERANCE; FEMALE; MOTOR ACTIVITY; PREGNANOLONE; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GABA-A;

EID: 0033714804     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (61)

1. International Union of Pharmacology. XV. Subtypes of γ-aminobutyric acid(A) receptors: Classification on the basis of subunit structure and receptor function
2. Ovarian steroids modify the behavioral and neurochemical responses of the central benzodiazepine receptor
3. Benzodiazepine agonist and inverse agonist actions on GABA(A) receptor-operated chloride channels. II. Chronic effects of ethanol
4. Characterization of the anticonvulsant properties of ganaxolone (CCD 1042; 3α-hydroxy-3β-methyl-5α-pregnan-20-one), a selective, high-affinity, steroid modulator of the γ-aminobutyric acid(A) receptor
5. Role of brain allopregnanolone in the plasticity of γ-aminobutyric acid type A receptor in rat brain during pregnancy and after delivery
6. Withdrawal from the endogenous steroid progesterone results in GABA(A) currents insensitive to benzodiazepine modulation in rat CA1 hippocampus
7. Simultaneous analysis of families of sigmoidal curves: Application to bioassay, radioligand assay, and physiological dose-response curves
8. Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition
9. Profile of acute tolerance to three sedative anxiolytics
10. The influence of estrus cycle on neurosteroid potency at the γ-aminobutyric acid(A) receptor complex
11. Allopregnanolone synthesis in cerebellar granule cells: Roles in regulation of GABA(A) receptor expression and function during progesterone treatment and withdrawal
12. γ-Aminobutyric acid(A) receptor regulation: Chronic treatment with pregnanolone uncouples allosteric interactions between steroid and benzodiazepine recognition sites
13. γ-Aminobutyric acid(A) receptor regulation: Heterologous uncoupling of modulatory site interactions induced by chronic steroid, barbiturate, benzodiazepine, or GABA treatment in culture
14. Biochemical and electrophysiological mechanisms underlying benzodiazepine tolerance and dependence
15. Anticonvulsant and behavioral effects of neuroactive steroids alone and in conjunction with diazepam
16. Acute and chronic effects of the synthetic neuroactive steroid, ganaxolone, against the convulsive and lethal effects of pentylenetrazol in seizure-kindled mice: Comparison with diazepam and valproate
17. Time course for development of anticonvulsant tolerance and GABAergic subsensitivity after chronic diazepam
18. Pharmacokinetics of benzodiazepines and of their metabolites
19. Tolerance to the anticonvulsant effect of benzodiazepines
20. Intermittent progesterone therapy and frequency of complex partial seizures in women with menstrual disorders
21. Progesterone therapy in women with complex partial and secondary generalized seizures
22. Psychoneuroendocrine aspects of tempolimbic epilepsy. Part II: Epilepsy and reproductive steroids
23. Chronic treatment with diazepam or abecarnil differentially affects the expression of GABA(A) receptor subunit mRNAs in the rat cortex
24. 2-subunit gene
25. Modifications of γ-aminobutyric acid(A) receptor subunit expression in rat neocortex during tolerance to diazepam
26. The quantitative measurement of motor incoordination in naive mice using an accelerating rotarod
27. CYP3A4 drug interactions: Correlation of 10 in vitro probe substrates
28. Influence of menstrual cycle and gender on alprazolam pharmacokinetics
29. Finasteride, a 5α-reductase inhibitor, blocks the anticonvulsant activity of progesterone in mice
30. Anticonvulsant activity of neurosteroids: Correlation with γ-aminobutyric acid-evoked chloride current potentiation
31. Lack of anticonvulsant tolerance to the neuroactive steroid pregnanolone in mice
32. Acute tolerance to triazolam during continuous and step infusions: Estimation of the effect offset rate constant
33. The selective interaction of neurosteroids with the GABA(A) receptors
34. Long-term studies on anticonvulsant tolerance and withdrawal characteristics of benzodiazepine receptor ligands in different seizure models in mice. I. Comparison of diazepam, clonazepam, clobazam and abecarnil
35. Development of tolerance to the anticonvulsant effect of diazepam in amygdala kindled rats
36. Modulation of GABA(A) receptor function by neuroactive steroids: Evidence for heterogeneity of steroid sensitivity of recombinant GABA(A) receptor isoforms
37. Development of tolerance in mice to the sedative effects of the neuroactive steroid minaxolone following chronic exposure
38. Which GABA(A)-receptor subtypes really occur in the brain?
39. Ganaxolone: A novel positive allosteric modulator of the GABA(A) receptor complex for the treatment of epilepsy
40. Initial human experience with ganaxolone, a neuroactive steroid with antiepileptic activity
41. Allopregnanolone concentrations and premenstrual syndrome
42. Allopregnanolone concentration in hippocampus of prepubertal rats and female rats throughout estrous cycle
43. The entry, distribution, and elimination of drugs
44. Neurosteroids act on recombinant human GABA(A) receptors
45. Controlled sedation with alphaxolone-alphadalone
46. Neurosteroid coadministration prevents development of tolerance and augments recovery from benzodiazepine withdrawal anxiety and hyperactivity in mice
47. Enhanced anticonvulsant activity of ganaxolone following neurosteroid withdrawal in a rat model of catamenial epilepsy
48. γ-Aminobutyric acid(A) receptor regulation in culture: Altered allosteric interactions following prolonged exposure to benzodiazepines, barbiturates, and methylxanthines
49. Anticonvulsant tolerance and withdrawal characteristics of benzodiazepine receptor ligands in different seizure models in mice. Comparison of diazepam, bretazenil and abecarnil
50. Benzodiazepines. Diazepam
51. Effects of subunit types of the cloned GABA(A) receptor on the response to a neurosteroid
52. GABA(A) receptor α4-subunit suppression prevents withdrawal properties of an endogenous steroid
53. Withdrawal from 3α-OH-5α-pregnan-20-one using a pseudopregnancy model alters the kinetics of hippocampal GABA(A)-gated current and increases the GABA(A) receptor α4 subunit in association with increased anxiety
54. Reduced benzodiazepine sensitivity in patients with premenstrual syndrome: A pilot study
55. General principles. Experimental selection, quantification, and evaluation of antiepileptic drugs
56. Anxiolytic and anticonvulsant activity of a synthetic neuroactive steroid Co3-0593
57. Role of cDNA-expressed human cytochromes P450 in the metabolism of diazepam
58. Chronic neurusteroid treatment attenuates single cell GABA(A) response and its potentiation by modulators in cortical neurons
59. Chronic neurosteroid treatment decreases the efficacy of benzodiazepine ligands and neurosteroids at the γ-aminobutyric acid(A) receptor complex in mammalian cortical neurons
60. Chronic neurosteroid treatment produces functional heterologous uncoupling at the γ-aminobutyric acid type A/benzodiazepine receptor complex in mammalian cortical neurons