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Volumn 6, Issue 14, 1996, Pages 1623-1628

SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonist

Author keywords

[No Author keywords available]

Indexed keywords

2 BENZHYDRYL 3 (2 METHOXYBENZYLAMINO) 1 AZABICYCLO[2.2.2]OCTANE; 2 BENZYL 1 (3,5 DIMETHYLBENZOYL) 4 (4 QUINOLINYLMETHYLAMINO)PIPERIDINE; NEUROKININ 1 RECEPTOR; PIPERIDINE DERIVATIVE; TACHYKININ RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

EID: 0030598679     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(96)00287-9     Document Type: Article
Times cited : (39)

References (29)
  • 12
    • 0012014057 scopus 로고
    • Approaches towards the design and synthesis of nonpeptidic substance-P antagonists
    • Testa, B.; Kyburz, E.; Fuhrer, W.; Giger, R., Ed.; Verlag Helvetica Chimica Acta, Basel
    • (7) Schilling, W.; Bittiger, H.; Brugger, F.; Criscione, L.; Hauser, K.; Ofner, S.; Olpe, H.-R.; Vassout, A.; Veenstra, S. "Approaches Towards the Design and Synthesis of Nonpeptidic Substance-P Antagonists", in Perspectives in Medicinal Chemistry, pp. 207-220, Testa, B.; Kyburz, E.; Fuhrer, W.; Giger, R., Ed.; Verlag Helvetica Chimica Acta, Basel, 1993.
    • (1993) Perspectives in Medicinal Chemistry , pp. 207-220
    • Schilling, W.1    Bittiger, H.2    Brugger, F.3    Criscione, L.4    Hauser, K.5    Ofner, S.6    Olpe, H.-R.7    Vassout, A.8    Veenstra, S.9
  • 15
    • 85030205467 scopus 로고    scopus 로고
    • note
    • 1H-NMR. The mixture could only be separated chromatographically after hydrogenolysis.
  • 16
    • 0003020201 scopus 로고
    • 3H-Substance P binding sites
    • Skrabanek, P.; Powell, D., Ed.; Boole Press Ltd., Dublin
    • 3H-Substance P binding sites", in Substance P - Dublin, pp 198-199, Skrabanek, P.; Powell, D., Ed.; Boole Press Ltd., Dublin, 1983.
    • (1983) Substance P - Dublin , pp. 198-199
    • Bittiger, H.1    Heid, J.2
  • 17
    • 85030199689 scopus 로고    scopus 로고
    • note
    • (12) Intermediates 33 can also be prepared according to Ref. [9].
  • 18
    • 85030200793 scopus 로고    scopus 로고
    • note
    • 20 = +27.8 ± 0.5° (c = 2.08, MeOH).
  • 19
    • 85030199708 scopus 로고    scopus 로고
    • note
    • (14) Dialkylation was also observed (mono: di = 2:1).
  • 20
    • 85030204075 scopus 로고    scopus 로고
    • note
    • 2 insertion.
  • 21
    • 85030209174 scopus 로고    scopus 로고
    • note
    • H = 1.13)
  • 27
    • 85030208949 scopus 로고    scopus 로고
    • note
    • 3H-SP radioligand binding, gerbil midbrain in nM units.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.