Literature DB >> 10406647

Multiple parallel synthesis of N,N-dialkyldipeptidylamines as N-type calcium channel blockers.

T R Ryder1, L Y Hu, M F Rafferty, E Millerman, B G Szoke, K Tarczy-Hornoch.   

Abstract

Selective N-type Voltage Sensitive Calcium Channel (VSCC) blockers have shown utility in several models of stroke and pain. A series of N,N-dialkyldipeptidylamines with potent functional activity at N-type VSCC's has been identified. Multiple parallel synthesis of a focused array of thirty compounds using polymer-supported quenching reagents and preliminary pharmacology are presented. Eighteen compounds were identified with an IC50 below 1 microM in an in vitro functional assay.

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Year:  1999        PMID: 10406647     DOI: 10.1016/s0960-894x(99)00284-x

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  Calcium channel blockers and pain therapy.

Authors:  B Cox
Journal:  Curr Rev Pain       Date:  2000

2.  Molecular modelling and QSAR analysis of some structurally diverse N-type calcium channel blockers.

Authors:  Jignesh Mungalpara; Ashish Pandey; Vaibhav Jain; C Gopi Mohan
Journal:  J Mol Model       Date:  2009-10-04       Impact factor: 1.810

Review 3.  Targeting voltage-gated calcium channels in neurological and psychiatric diseases.

Authors:  Gerald W Zamponi
Journal:  Nat Rev Drug Discov       Date:  2015-11-06       Impact factor: 84.694

Review 4.  The Physiology, Pathology, and Pharmacology of Voltage-Gated Calcium Channels and Their Future Therapeutic Potential.

Authors:  Gerald W Zamponi; Joerg Striessnig; Alexandra Koschak; Annette C Dolphin
Journal:  Pharmacol Rev       Date:  2015-10       Impact factor: 25.468

5.  Acute visceral pain relief mediated by A3AR agonists in rats: involvement of N-type voltage-gated calcium channels.

Authors:  Elena Lucarini; Elisabetta Coppi; Laura Micheli; Carmen Parisio; Alessia Vona; Federica Cherchi; Anna M Pugliese; Felicita Pedata; Paola Failli; Seph Palomino; Jared Wahl; Tally M Largent-Milnes; Todd W Vanderah; Dilip K Tosh; Kenneth A Jacobson; Daniela Salvemini; Carla Ghelardini; Lorenzo Di Cesare Mannelli
Journal:  Pain       Date:  2020-09-01       Impact factor: 7.926

  5 in total

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