Literature DB >> 11212124

Nipecotic and iso-nipecotic amides as potent and selective somatostatin subtype-2 receptor agonists.

C Zhou1, L Guo, G Morriello, A Pasternak, Y Pan, S P Rohrer, E T Birzin, S E Huskey, T Jacks, K D Schleim, K Cheng, J M Schaeffer, A A Patchett, L Yang.   

Abstract

N-Substituted nipecotic and iso-nipecotic amides of beta-methylTrpLys tert-butyl ester were found to be novel, selective and potent agonists of the somatostatin subtype-2 receptor in vitro. For example iso-nipecotic amide 8a showed high hsst2 binding affinity (Ki = 0.5 nM) and good selectivity (h5/h2 = 832).

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Year:  2001        PMID: 11212124     DOI: 10.1016/s0960-894x(00)00687-9

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


  2 in total

1.  Beta(2)/beta(3)-di- and alpha/beta(3)-tetrapeptide derivatives as potent agonists at somatostatin sst(4) receptors.

Authors:  Caroline Nunn; Magnus Rueping; Daniel Langenegger; Edi Schuepbach; Thierry Kimmerlin; Peter Micuch; Konstanze Hurth; Dieter Seebach; Daniel Hoyer
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2003-01-24       Impact factor: 3.000

2.  Understanding the influence of lipid bilayers and ligand molecules in determining the conformational dynamics of somatostatin receptor 2.

Authors:  Santhosh Kumar Nagarajan; Sathya Babu; Seema A Kulkarni; Aanand Vadivelu; Panneer Devaraju; Honglae Sohn; Thirumurthy Madhavan
Journal:  Sci Rep       Date:  2021-04-07       Impact factor: 4.379

  2 in total

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