N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers

Bioorganic and Medicinal Chemistry Letters

Volumn 9, Issue 6, 1999, Pages 907-912

  Hu, Lain Yen ^a   Ryder, Todd R ^a   Rafferty, Michael F ^a   Cody, Wayne L ^a   Lotarski, Susan M ^a   Miljanich, George P ^b   Millerman, Elizabeth ^b   Rock, David M ^a   Song, Yuntao ^a   Stoehr, Sally J ^a   Taylor, Charles P ^a   Weber, Mark L ^a   Szoke, Balazs G ^b   Vartanian, Mark G ^a  

^a PFIZER INC   (United States)

^b ELAN PHARMACEUTICALS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CALCIUM CHANNEL BLOCKING AGENT; PD 151307; PD 167341; UNCLASSIFIED DRUG;

ARTICLE; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; STRUCTURE ACTIVITY RELATION;

ANIMALS; CALCIUM CHANNEL BLOCKERS; DIAMINES; DIPEPTIDES; DISEASE MODELS, ANIMAL; MICE; MICE, INBRED DBA; MODELS, CHEMICAL; SEIZURES;

EID: 0033594206     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00100-6     Document Type: Article

References (16)

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10. +2 channel blocker (nitrendipine). PD 151307 was run in parallel as a standard in each assay.
11. 2O (120 mL) and treated with formaldehyde (80 mL, 37% solution) and Raney Nickel. The reaction mixture was stirred for 21 h, acetone was added and the product was precipitated and collected (77%). ss
12. 3) Calcd: C 74.41, H 9.18, N 7.66; Found: C 74.73, H 9.42, N 7.3 2.
13. Compound and showed % protection from the Tonic phase at the dose of mg/kg. The protocol for audiogenic seizure mouse studies by DBA/2 mice: (a) De Sarro, G. B.; Meldrum, B. S.; Nistico, G. Br. J. Pharmacol. 1988, 93, 247.
14. +2 channel blocker, ω-conotoxin GVIA, is active in the DBA/2 model. Jackson, H. C.; Scheideier, M. A. Phychopharmacology 1996, 126, 85.
15. + channel blockers are active in the DBA/2 model. Meldrum, B. S. Neurology 1994, 44, S14.
16. + channel currents.