메뉴 건너뛰기




Volumn 42, Issue 13, 1999, Pages 2403-2408

γ-aminobutyrate-A receptor modulation by 3-aryl-1-(arylsulfonyl)- 1,4,5,6-tetrahydropyridazines

Author keywords

[No Author keywords available]

Indexed keywords

3ALPHA HYDROXY 5ALPHA PREGNAN 20 ONE; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; PARTIAL AGONIST; PENTETRAZOLE;

EID: 0033168908     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm9805889     Document Type: Article
Times cited : (25)

References (33)
  • 1
    • 0026615116 scopus 로고
    • A receptors: Ligand-gated chloride ion channels modulated by multiple drug-binding sites
    • A receptors: ligand-gated chloride ion channels modulated by multiple drug-binding sites. Trends Pharmacol. Sci. 1992, 13, 446-450.
    • (1992) Trends Pharmacol. Sci. , vol.13 , pp. 446-450
    • Sieghart, W.1
  • 2
    • 77956845273 scopus 로고
    • Neuronal BZD receptors: New ligands, clones and pharmacology
    • (b) Gammill, R. B.; Carter, D. B. Neuronal BZD receptors: new ligands, clones and pharmacology. Annu. Rep. Med. Chem. 1993, 28, 19-27.
    • (1993) Annu. Rep. Med. Chem. , vol.28 , pp. 19-27
    • Gammill, R.B.1    Carter, D.B.2
  • 3
    • 0029788870 scopus 로고    scopus 로고
    • GABA physiology: Modulation by benzodiazepines and hormones
    • (c) Wilson, M. A. GABA physiology: Modulation by benzodiazepines and hormones. Crit. Rev. Neurobiol. 1996, 10, 1-37.
    • (1996) Crit. Rev. Neurobiol. , vol.10 , pp. 1-37
    • Wilson, M.A.1
  • 4
    • 0030884886 scopus 로고    scopus 로고
    • Interactions between steroid hormones and the nervous system
    • (a) Spindler, K.-D. Interactions between steroid hormones and the nervous system. Neurotoxicology 1997, 18, 745-754.
    • (1997) Neurotoxicology , vol.18 , pp. 745-754
    • Spindler, K.-D.1
  • 5
    • 0029050446 scopus 로고
    • Functional significance of steroid modulation of GABAergic neurotransmission: Analysis at the behavioral, cellular, and molecular levels
    • (b) McCarthy, M. M. Functional significance of steroid modulation of GABAergic neurotransmission: analysis at the behavioral, cellular, and molecular levels. Horm. Behav. 1995, 29, 131-140.
    • (1995) Horm. Behav. , vol.29 , pp. 131-140
    • McCarthy, M.M.1
  • 6
    • 0026579057 scopus 로고
    • Neuroactive steroids
    • (c) Paul, S. M.; Purdy, R. H. Neuroactive steroids. FASEB J. 1992, 6, 2311-2322.
    • (1992) FASEB J. , vol.6 , pp. 2311-2322
    • Paul, S.M.1    Purdy, R.H.2
  • 7
    • 0025353194 scopus 로고
    • Synthesis, metabolism, and pharmacological activity of 3α-hydroxy steroids which potentiate GABA-receptor-mediated chloride ion uptake in rat cerebral cortical synapto-neurosomes
    • (d) Purdy, R. H.; Morrow, A. L.; Blinn, J. R.; Paul, S. M. Synthesis, metabolism, and pharmacological activity of 3α-hydroxy steroids which potentiate GABA-receptor-mediated chloride ion uptake in rat cerebral cortical synapto-neurosomes. J. Med. Chem. 1990, 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
  • 8
    • 0021741846 scopus 로고
    • Modulation of the GABA receptor complex by a steroid anesthetic
    • (e) Harrison, N. L.; Simmonds, M. A. Modulation of the GABA receptor complex by a steroid anesthetic. Brain Res. 1984, 323, 287-292.
    • (1984) Brain Res. , vol.323 , pp. 287-292
    • Harrison, N.L.1    Simmonds, M.A.2
  • 9
    • 0022483382 scopus 로고
    • Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor
    • Washington, D.C.
    • (f) Majewska, M. D.; Harrison, N. L.; Schwartz, R. D.; Barker, J. L.; Paul, S. M. Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor. Science (Washington, D.C.) 1986, 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
  • 11
    • 0027142561 scopus 로고
    • A receptor function. 1. The effect of 6-methyl substitution on the electrophysiological activity of 7-substituted benz[e]indene-3-carbonitriles
    • A receptor function. 1. The effect of 6-methyl substitution on the electrophysiological activity of 7-substituted benz[e]indene-3-carbonitriles. J. Med. Chem. 1993, 36, 3956-3967.
    • (1993) J. Med. Chem. , vol.36 , pp. 3956-3967
    • Hu, Y.1    Zorumski, C.F.2    Covey, D.F.3
  • 12
    • 0029032435 scopus 로고
    • Neurosteroid analogues. 2. Total synthesis and electrophysiological evaluation of benz[e]indene analogues of the anesthetic steroid alphaxalone
    • (i) Hu, Y.; Zorumski, C. F.; Covey, D. F. Neurosteroid Analogues. 2. Total Synthesis and Electrophysiological Evaluation of Benz[e]indene Analogues of the Anesthetic Steroid Alphaxalone. J. Org. Chem. 1995, 60, 3619-3625.
    • (1995) J. Org. Chem. , vol.60 , pp. 3619-3625
    • Hu, Y.1    Zorumski, C.F.2    Covey, D.F.3
  • 13
    • 0028853824 scopus 로고
    • Neurosteroid analogues. 3. The synthesis and electrophysiological evaluation of benz[e]indene congeners of neuroactive steroids having the 5β-configuration
    • (j) Han, M.; Hu, Y.; Zorumski, C. F.; Covey, D. F. Neurosteroid Analogues. 3. The Synthesis and Electrophysiological Evaluation of Benz[e]indene Congeners of Neuroactive Steroids Having the 5β-Configuration. J. Med. Chem. 1995, 38, 4548-4556.
    • (1995) J. Med. Chem. , vol.38 , pp. 4548-4556
    • Han, M.1    Hu, Y.2    Zorumski, C.F.3    Covey, D.F.4
  • 21
    • 0030908224 scopus 로고    scopus 로고
    • Influence of gender and brain region on neurosteroid modulation of GABA responses in rats
    • (a) Wilson, M. A.; Biscardi, R. Influence of gender and brain region on neurosteroid modulation of GABA responses in rats. Life Sci. 1997, 60, 1679-1691.
    • (1997) Life Sci. , vol.60 , pp. 1679-1691
    • Wilson, M.A.1    Biscardi, R.2
  • 22
    • 0029555076 scopus 로고
    • Influence of the estrous cycle on the discrimination of apparent neuroactive steroid site subtypes on the γ-aminobutyric acidA receptor complex in the rat
    • (b) McCauley, L. D.; Gee, K. W. Influence of the estrous cycle on the discrimination of apparent neuroactive steroid site subtypes on the γ-aminobutyric acidA receptor complex in the rat. J. Pharmacol. Exp. Ther. 1995, 275, 1412-1417.
    • (1995) J. Pharmacol. Exp. Ther. , vol.275 , pp. 1412-1417
    • McCauley, L.D.1    Gee, K.W.2
  • 23
    • 0027332492 scopus 로고
    • A receptor complexes following acute treatment with anesthetically active steroids
    • A receptor complexes following acute treatment with anesthetically active steroids. Acta Endocrinol. 1993, 129, 480-485.
    • (1993) Acta Endocrinol. , vol.129 , pp. 480-485
    • Jussofie, A.1
  • 24
    • 0027585051 scopus 로고
    • Brain region-specific effects of neuroactive steroids on the affinity and density of the GABA-binding site
    • (b) Jussofie, A. Brain region-specific effects of neuroactive steroids on the affinity and density of the GABA-binding site. Biol. Chem. Hoppe-Seyler 1993, 374, 265-270.
    • (1993) Biol. Chem. Hoppe-Seyler , vol.374 , pp. 265-270
    • Jussofie, A.1
  • 25
    • 0028213983 scopus 로고
    • Allosteric effects of a GABA receptor-active steroid are altered by stress. Pharmacol
    • Deutsch, S. I.; Park, C. H.; Hitri, A. Allosteric effects of a GABA receptor-active steroid are altered by stress. Pharmacol. Biochem. Behav. 1994, 47, 913-917.
    • (1994) Biochem. Behav. , vol.47 , pp. 913-917
    • Deutsch, S.I.1    Park, C.H.2    Hitri, A.3
  • 27
    • 0028805303 scopus 로고
    • Nonsteroidal progesterone receptor ligands. 1. 3-Aryl-1-benzoyl-1,4,5,6-tetrahydropyridazines
    • (b) Combs, D. W.; Reese, K.; Phillips, A Nonsteroidal progesterone receptor ligands. 1. 3-Aryl-1-benzoyl-1,4,5,6-tetrahydropyridazines. J. Med. Chem. 1995, 38, 4878-4879.
    • (1995) J. Med. Chem. , vol.38 , pp. 4878-4879
    • Combs, D.W.1    Reese, K.2    Phillips, A.3
  • 28
    • 0028803378 scopus 로고
    • Nonsteroidal progesterone receptor ligands. 2. High-affinity ligands with selectivity for bone cell progesterone receptors
    • (c) Combs, D. W.; Reese, K; Cornelius, L. A. M.; Gunnet, J. W.; Cryan, E. V.; Granger, K. S.; Jordan, J. J.; Demarest, K. T. Nonsteroidal Progesterone Receptor Ligands. 2. High-Affinity Ligands with Selectivity for Bone Cell Progesterone Receptors. J. Med. Chem. 1995, 38, 4880-4884.
    • (1995) J. Med. Chem. , vol.38 , pp. 4880-4884
    • Combs, D.W.1    Reese, K.2    Cornelius, L.A.M.3    Gunnet, J.W.4    Cryan, E.V.5    Granger, K.S.6    Jordan, J.J.7    Demarest, K.T.8
  • 29
    • 0345155968 scopus 로고
    • Preparation of 1-arylsulfonyl, arylcarbonyl and 1-arylphosphonyl-3-phenyl-1,4,5,6-tetrahydropyridazine progestin agonists
    • PCT Int. Appl. WO 94 01,412
    • (d) Combs, D. W. Preparation of 1-arylsulfonyl, arylcarbonyl and 1-arylphosphonyl-3-phenyl-1,4,5,6-tetrahydropyridazine progestin agonists. PCT Int. Appl. WO 94 01,412; Chem. Abstr. 1995, 122, 31542.
    • (1995) Chem. Abstr. , vol.122 , pp. 31542
    • Combs, D.W.1
  • 30
    • 0029592604 scopus 로고
    • Characterization of a benzodiazepine receptor site with exceptionally high affinity for Ro 15-4513 in the rat CNS
    • Mehta, A. K.; Shank, R. P. Characterization of a benzodiazepine receptor site with exceptionally high affinity for Ro 15-4513 in the rat CNS. Brain Res. 1995, 704, 289-297.
    • (1995) Brain Res. , vol.704 , pp. 289-297
    • Mehta, A.K.1    Shank, R.P.2
  • 31
    • 0017332891 scopus 로고
    • A new rapid device for the rapid measurement of impaired motor function in mice
    • Coughenour, L. L.; McLean, J. R.; Parker, R. B. A New Rapid Device for the Rapid Measurement of Impaired Motor Function In Mice. Pharmacol. Biochem. Behav. 1977, 6, 351-353.
    • (1977) Pharmacol. Biochem. Behav. , vol.6 , pp. 351-353
    • Coughenour, L.L.1    McLean, J.R.2    Parker, R.B.3
  • 32
    • 0000311864 scopus 로고
    • Laboratory assay of clinically effective anti-epileptic drugs
    • Swinyard, E. A. Laboratory Assay of Clinically Effective Anti-epileptic Drugs. J. Am. Pharm. Assoc. 1949, 38, 201-204.
    • (1949) J. Am. Pharm. Assoc. , vol.38 , pp. 201-204
    • Swinyard, E.A.1
  • 33
    • 0345587912 scopus 로고    scopus 로고
    • note
    • 50 = 1.3 nM (manuscript in preparation). Formula presented


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.