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Volumn 9, Issue 10, 1999, Pages 1379-1384

N-substituted-3-arylpyrrolidines: Potent and selective ligands at serotonin 1A receptor

Author keywords

[No Author keywords available]

Indexed keywords

LIGAND; N [(N SACCHARINO)BUTYL]PYRROLIDINE; PYRROLIDINE DERIVATIVE; SEROTONIN 1A RECEPTOR; UNCLASSIFIED DRUG;

EID: 0033577775     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00201-2     Document Type: Article
Times cited : (18)

References (19)
  • 3
    • 0000629984 scopus 로고
    • serotonin (5-HT) receptors. Sammes PG, Taylor JB, editors. Oxford: Pergamon Press
    • Hibert MF, Mir AK, Fozard JR: serotonin (5-HT) receptors. In: Sammes PG, Taylor JB, editors. Comprehensive Medicinal Chemistry, Vol. 3. Oxford: Pergamon Press, 1990:567-600.
    • (1990) Comprehensive Medicinal Chemistry , vol.3 , pp. 567-600
    • Hibert, M.F.1    Mir, A.K.2    Fozard, J.R.3
  • 4
    • 0028319235 scopus 로고
    • note
    • 50, 3 nM) have been reported as a patent (DE 19615232). We thank the referee who called our attention to this information. Other N-substituted-3-arylpyrrolidine derivatives with different pharmacological behavior have been reported from Abbott laboratories, see: (a) Zelle RE, Hancock AA, Buchner SA, Basha FZ, Tietje K, DeBernardis JF, Meyer MD. Bioorg. Med. Chem. Lett. 1994:4;1319-1322.
    • (1994) Bioorg. Med. Chem. Lett. , vol.4 , pp. 1319-1322
    • Zelle, R.E.1    Hancock, A.A.2    Buchner, S.A.3    Basha, F.Z.4    Tietje, K.5    DeBernardis, J.F.6    Meyer, M.D.7
  • 7
    • 0031552095 scopus 로고    scopus 로고
    • Also, a Swedish group has reported different 3-arylpyrrolidine derivatives as potential DA receptor antagonists, see
    • (c) Hancock AA, Buckner SA, Giardina WJ, Brune ME, Lee JY, Morse PA, Oheim KW, Stanisic DS, Warner RB, Kerkman DJ, DeBernardis JF. J. Pharmacol. Exp. Ther. 1995:272;1160-1169). Also, a Swedish group has reported different 3-arylpyrrolidine derivatives as potential DA receptor antagonists, see: Sonesson C, Wikström H, Smith MW, Svensson K, Carlsson A, Waters N. Bioorg. Med. Chem. Lett. 1997:7;231-246..
    • (1997) Bioorg. Med. Chem. Lett. , vol.7 , pp. 231-246
    • Sonesson, C.1    Wikström, H.2    Smith, M.W.3    Svensson, K.4    Carlsson, A.5    Waters, N.6
  • 9
    • 0029055877 scopus 로고
    • Other synthetic methods have been appeared during our study, see: (a) Denmark SE, Marcin LR. J. Org. Chem. 1995:60;3221-3235.
    • (1995) J. Org. Chem. , vol.60 , pp. 3221-3235
    • Denmark, S.E.1    Marcin, L.R.2
  • 13
    • 0013542176 scopus 로고    scopus 로고
    • note
    • 2O, the organic phase was washed with brine, dried over magnesium sulfate, and concentrated in vacuo. Purification of the residue by column chromatography on silica gel (eluent: 10% ethyl acetate in hexanes) afforded the product 3a in 78% yield (685 mg).
  • 15
    • 0013511497 scopus 로고    scopus 로고
    • note
    • 3, 75 MHz): δ 170.8, 146.1, 140.1, 136.9, 130.1, 128.8, 128.5, 127.7, 127.4, 126.5, 125.8, 62.7, 60.6, 55.0, 49.2, 43.8, 43.5, 33.8, 26.8, 26.0, 25.0.
  • 16
    • 0013477016 scopus 로고    scopus 로고
    • note
    • All the compounds tested were racemic. The binding study for enantiopure (R)-6c and (S)-6c, synthesized in a different approach, indicated that the (S)-isomer was about twice potent than the (R)-isomer: Unpublished results.
  • 17
    • 0013511192 scopus 로고    scopus 로고
    • note
    • 2 of rat striatum. Specific binding was measured by subtracting nonspecific binding out of total binding. Nonspecific binding was measured in the presence of specified concentrations of each non-labeled ligands under the same condition as that for measuring total binding.
  • 18
    • 0001875379 scopus 로고    scopus 로고
    • Drugs and the treatment of psychiatric disorders
    • Hardman JG, Limbird LE, Molinoff PB, Ruddon RW, Gilman AG, editors. New York: McGraw-Hill
    • Baldessarini RJ: Drugs and the treatment of psychiatric disorders. In: Hardman JG, Limbird LE, Molinoff PB, Ruddon RW, Gilman AG, editors. The Pharmacological Basis of Therapeutics, 9th Ed. New York: McGraw-Hill, 1996:399-430.
    • (1996) The Pharmacological Basis of Therapeutics, 9th Ed. , pp. 399-430
    • Baldessarini, R.J.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.