Literature DB >> 10476867

Synthesis and dopamine receptor modulating activity of unsubstituted and substituted triproline analogues of L-prolyl-L-leucyl-glycinamide (PLG).

P W Baures1, A Pradhan, W H Ojala, W B Gleason, R K Mishra, R L Johnson.   

Abstract

Triprolines Pro-Pro-Pro-NH2 (4), Pro-Pro-D-Pro-NH2 (5), Pro-Pro(trans-3-Me)-D-Pro-NH2 (6), and Pro-Pro(cis-3-Me)-D-Pro-NH2 (7) were made as conformationally constrained analogues of Pro-Leu-Gly-NH2. Triprolines 4-6 produced significant increases in the high- and low-affinity state ratio (RH/RL) of the dopamine receptor, but only 4 was found to increase apomorphine induced rotations in 6-hydroxydopamine-lesioned rats.

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Year:  1999        PMID： 10476867     DOI： 10.1016/s0960-894x(99)00386-8

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


  6 in total

1.  Allosteric modulation of the dopamine D2 receptor by Pro-Leu-Gly-NH2 peptidomimetics constrained in either a polyproline II helix or a type II beta-turn conformation.

Authors:  Bhooma Raghavan; Kevin J Skoblenick; Swapna Bhagwanth; Niran Argintaru; Ram K Mishra; Rodney L Johnson
Journal:  J Med Chem       Date:  2009-04-09       Impact factor: 7.446

2.  Transformation of Pro-Leu-Gly-NH2 peptidomimetic positive allosteric modulators of the dopamine D2 receptor into negative modulators.

Authors:  Swapna Bhagwanth; Satyendra Mishra; Ritesh Daya; Jordan Mah; Ram K Mishra; Rodney L Johnson
Journal:  ACS Chem Neurosci       Date:  2012-01-13       Impact factor: 4.418

3.  Allosteric modulation of the dopamine receptor by conformationally constrained type VI beta-turn peptidomimetics of Pro-Leu-Gly-NH2.

Authors:  Ashish P Vartak; Kevin Skoblenick; Nancy Thomas; Ram K Mishra; Rodney L Johnson
Journal:  J Med Chem       Date:  2007-12-01       Impact factor: 7.446

4.  A Novel Cosegregating DCTN1 Splice Site Variant in a Family with Bipolar Disorder May Hold the Key to Understanding the Etiology.

Authors:  André Hallen; Arthur J L Cooper
Journal:  Genes (Basel)       Date:  2020-04-18       Impact factor: 4.096

5.  Development of peptidomimetic ligands of Pro-Leu-Gly-NH(2) as allosteric modulators of the dopamine D(2) receptor.

Authors:  Swapna Bhagwanth; Ram K Mishra; Rodney L Johnson
Journal:  Beilstein J Org Chem       Date:  2013-01-30       Impact factor: 2.883

6.  Effects of the dopamine D2 allosteric modulator, PAOPA, on the expression of GRK2, arrestin-3, ERK1/2, and on receptor internalization.

Authors:  Dipannita Basu; Yuxin Tian; Jayant Bhandari; Jian Ru Jiang; Patricia Hui; Rodney L Johnson; Ram K Mishra
Journal:  PLoS One       Date:  2013-08-06       Impact factor: 3.240
  6 in total

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