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Volumn 287, Issue 1, 1998, Pages 198-207

Substituted 3β-phenylethynyl derivatives of 3α-hydroxy-5α-pregnan- 20-one: Remarkably potent neuroactive steroid modulators of γ-aminobutyric acid(A) receptors

Author keywords

[No Author keywords available]

Indexed keywords

3ALPHA HYDROXY 5ALPHA PREGNAN 20 ONE; 3ALPHA,21 DIHYDROXY 5ALPHA PREGNAN 20 ONE; 3BETA (4 ACETYLPHENYLETHYNYL) 3ALPHA HYDROXY 5ALPHA PREGNAN 20 ONE; 4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; FLUNITRAZEPAM; MUSCIMOL; NEUROSTEROID; PENTETRAZOLE; PROGESTERONE DERIVATIVE; TERT BUTYLBICYCLOPHOSPHOROTHIOATE; UNCLASSIFIED DRUG; BENZODIAZEPINE RECEPTOR AFFECTING AGENT; ELTANOLONE; FUSED HETEROCYCLIC RINGS; RECOMBINANT PROTEIN; TERT-BUTYLBICYCLOPHOSPHOROTHIONATE;

EID: 17944397975     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article
Times cited : (22)

References (36)
  • 2
    • 0029859637 scopus 로고    scopus 로고
    • In vitro and in vivo activity of 16,17-dehyro-epipregnanolones: 17,20-bond torsional energy analysis and D-ring conformation
    • Bolger MB, Wieland S, Hawkinson JE, Xia H, Upasani R and Lan NC (1996) In vitro and in vivo activity of 16,17-dehyro-epipregnanolones: 17,20-bond torsional energy analysis and D-ring conformation. Phamaceut Res 13:1486-1492.
    • (1996) Phamaceut Res , vol.13 , pp. 1486-1492
    • Bolger, M.B.1    Wieland, S.2    Hawkinson, J.E.3    Xia, H.4    Upasani, R.5    Lan, N.C.6
  • 7
    • 0030838076 scopus 로고    scopus 로고
    • Anticonvulsant and behavioral effects of neuroactive steroids alone and in conjunction with diazepam
    • 1997
    • Gasior M, Carter RB, Goldberg SR and Witkin JM (1997) Anticonvulsant and behavioral effects of neuroactive steroids alone and in conjunction with diazepam. J Pharmacol Exp Ther 282:543-553 1997.
    • (1997) J Pharmacol Exp Ther , vol.282 , pp. 543-553
    • Gasior, M.1    Carter, R.B.2    Goldberg, S.R.3    Witkin, J.M.4
  • 9
    • 0028801074 scopus 로고
    • A receptor complex: The pharmacological properties and therapeutic potential of epalons
    • A receptor complex: The pharmacological properties and therapeutic potential of epalons. Crit Rev Neurobiol 9:207-227.
    • (1995) Crit Rev Neurobiol , vol.9 , pp. 207-227
    • Gee, K.W.1    McCauley, L.D.2    Lan, N.C.3
  • 10
    • 0028981625 scopus 로고
    • 3H]muscimol binding to the GABAA receptor complex in rat cortex
    • 3H]muscimol binding to the GABAA receptor complex in rat cortex. Eur J Pharmacol 288:157-162.
    • (1995) Eur J Pharmacol , vol.288 , pp. 157-162
    • Goodnough, D.B.1    Hawkinson, J.E.2
  • 12
    • 0021741846 scopus 로고
    • Modulation of the GABA receptor complex by a steroid anaesthetic
    • Harrison NL and Simmonds MA (1984) Modulation of the GABA receptor complex by a steroid anaesthetic. Brain Res 323:287-292.
    • (1984) Brain Res , vol.323 , pp. 287-292
    • Harrison, N.L.1    Simmonds, M.A.2
  • 15
    • 0028171991 scopus 로고
    • The neuroactive steroid 3α-hydroxy-5β-pregnan-20-one is a two-component modulator of ligand binding to the GABAA receptor
    • Hawkinson JE, Kimbrough CL, McCauley LD, Bolger MB, Lan NC and Gee KW (1994b) The neuroactive steroid 3α-hydroxy-5β-pregnan-20-one is a two-component modulator of ligand binding to the GABAA receptor. Eur J Pharmacol 269:157-163.
    • (1994) Eur J Pharmacol , vol.269 , pp. 157-163
    • Hawkinson, J.E.1    Kimbrough, C.L.2    McCauley, L.D.3    Bolger, M.B.4    Lan, N.C.5    Gee, K.W.6
  • 16
    • 26444528699 scopus 로고    scopus 로고
    • (1995) Process for synthesis of steroidal allylic tert alcohols. US Patent 5,449,795
    • Hogenkamp DJ (1995) Process for synthesis of steroidal allylic tert alcohols. US Patent 5,449,795.
    • Hogenkamp, D.J.1
  • 18
    • 0027497889 scopus 로고
    • FISH ordering of reference markers and of the gene for the alpha 5 subunit of the gamma-aminobutyric acid receptor (GABRA5) within the Angelman and Prader-Willi syndrome chromosomal regions
    • Knoll JHM, Sinnett D, Wagstaff J, Glatt K, Wilcox AS, Whiting PM, Wingrove P, Sikela JM and Lalande M (1993) FISH ordering of reference markers and of the gene for the alpha 5 subunit of the gamma-aminobutyric acid receptor (GABRA5) within the Angelman and Prader-Willi syndrome chromosomal regions. Hum Mol Genet 2:183-189.
    • (1993) Hum Mol Genet , vol.2 , pp. 183-189
    • Knoll, J.H.M.1    Sinnett, D.2    Wagstaff, J.3    Glatt, K.4    Wilcox, A.S.5    Whiting, P.M.6    Wingrove, P.7    Sikela, J.M.8    Lalande, M.9
  • 19
    • 0028149787 scopus 로고
    • Anticonvulsant activity of neurosteroids: Correlation with γ-aminobutyric acid-evoked chloride current potentiation
    • 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.
    • (1994) J Pharmacol Exp Ther , vol.270 , pp. 1223-1229
    • Kokate, T.G.1    Svensson, B.E.2    Rogawski, M.A.3
  • 21
    • 0029671013 scopus 로고    scopus 로고
    • A-receptor-mediated effects of progesterone, its ring-A-reduced metabolites and synthetic neuroactive steroids on neurogenic oedema in the rat meninges
    • A-receptor-mediated effects of progesterone, its ring-A-reduced metabolites and synthetic neuroactive steroids on neurogenic oedema in the rat meninges. Br J Pharmacol 117:99-104.
    • (1996) Br J Pharmacol , vol.117 , pp. 99-104
    • Limmroth, V.1    Lee, W.S.2    Moskowitz, M.A.3
  • 22
    • 84951384024 scopus 로고
    • A simplified method of evaluating dose-effect experiments
    • Litchfield JT and Wilcoxon F (1949) A simplified method of evaluating dose-effect experiments. J Pharmacol Exp Ther 96:99-105.
    • (1949) J Pharmacol Exp Ther , vol.96 , pp. 99-105
    • Litchfield, J.T.1    Wilcoxon, F.2
  • 23
    • 0022483382 scopus 로고
    • Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor
    • Majewska MD, Harrison NL, Schwartz RD, Barker JL and Paul SM (1986) Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor. Science 232:1004-1007.
    • (1986) Science , vol.232 , pp. 1004-1007
    • Majewska, M.D.1    Harrison, N.L.2    Schwartz, R.D.3    Barker, J.L.4    Paul, S.M.5
  • 24
    • 0016806065 scopus 로고
    • Structure-activity relationships in steroidal anaesthetics
    • Phillips GH (1975) Structure-activity relationships in steroidal anaesthetics. J Steroid Biochem 6:607-613.
    • (1975) J Steroid Biochem , vol.6 , pp. 607-613
    • Phillips, G.H.1
  • 25
    • 0025353194 scopus 로고
    • Synthesis, metabolism and pharmacological activity of 3α-hydroxy steroids which potentiate GABA-receptor-mediated chloride ion uptake in rat cerebral cortical synaptoneurosomes
    • Purdy RH, Morrow AL, Blinn JR and Paul SM (1990) Synthesis, metabolism and pharmacological activity of 3α-hydroxy steroids which potentiate GABA-receptor-mediated chloride ion uptake in rat cerebral cortical synaptoneurosomes. J Med Chem 33:1572-1581.
    • (1990) J Med Chem , vol.33 , pp. 1572-1581
    • Purdy, R.H.1    Morrow, A.L.2    Blinn, J.R.3    Paul, S.M.4
  • 29
    • 0028986669 scopus 로고
    • Comparative behavioral characterization of the neuroactive steroids 3α-OH, 5α-pregnan-20-one and 3α-OH, 5β-pregnan-20-one in rodents
    • Wieland S, Belluzi JD, Stein L and Lan NC (1995) Comparative behavioral characterization of the neuroactive steroids 3α-OH, 5α-pregnan-20-one and 3α-OH, 5β-pregnan-20-one in rodents. Psychopharmacology 118:65-71.
    • (1995) Psychopharmacology , vol.118 , pp. 65-71
    • Wieland, S.1    Belluzi, J.D.2    Stein, L.3    Lan, N.C.4
  • 32
    • 0028916586 scopus 로고
    • In vitro pharmacology of ACEA-1021 and ACEA-1031: Systemically active quinoxalinediones with high affinity and selectivity for N-methyl-D-aspartate receptor glycine sites
    • Woodward RM, Huettner JE, Guastella J, Keana JFW and Weber E (1995) In vitro pharmacology of ACEA-1021 and ACEA-1031: Systemically active quinoxalinediones with high affinity and selectivity for N-methyl-D-aspartate receptor glycine sites. Mol Pharmacol 47:568-581.
    • (1995) Mol Pharmacol , vol.47 , pp. 568-581
    • Woodward, R.M.1    Huettner, J.E.2    Guastella, J.3    Keana, J.F.W.4    Weber, E.5
  • 34
    • 0028972886 scopus 로고
    • A receptor α4 subunit: Identification of a unique diazepam-insensitive binding site
    • A receptor α4 subunit: Identification of a unique diazepam-insensitive binding site. Eur J Pharmacol 291:319-325.
    • (1995) Eur J Pharmacol , vol.291 , pp. 319-325
    • Yang, W.1    Drewe, J.A.2    Lan, N.C.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.