Literature DB >> 1356555

A68930 is a potent, full agonist at dopamine1 (D1) receptors in renal epithelial LLC-PK1 cells.

A Grenader1, D P Healy.   

Abstract

The selective dopamine1 (D1) receptor agonists SK&F 82526 (fenoldopam) and A68930 and the mixed D1/D2 agonist SK&F 85174 were tested for their ability to stimulate adenosine 3':5'-cyclic monophosphate (cyclic AMP) accumulation in the porcine renal epithelial cell line, LLC-PK1. SK&F 82526 and SK&F 85174 were potent stimulators of cyclic AMP accumulation (EC50s 21.4 and 14.5 nM, respectively), but only partial agonists (intrinsic activities 31% and 46% of dopamine respectively). In contrast, A68930 was a potent, full agonist (EC50 12.7 nM, intrinsic activity 102% of dopamine). The stimulatory effects of A68930 and dopamine on cyclic AMP accumulation were not additive, and the stimulation of cyclic AMP accumulation by A68930 was blocked by the D1-selective antagonist, SCH 23390. These properties of A68930 suggest that it may be a useful D1-selective agonist to study renal D1 receptor mechanisms in vitro and in vivo.

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Year:  1992        PMID: 1356555      PMCID: PMC1907500          DOI: 10.1111/j.1476-5381.1992.tb14320.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  9 in total

Review 1.  Multiple receptors for dopamine.

Authors:  J W Kebabian; D B Calne
Journal:  Nature       Date:  1979-01-11       Impact factor: 49.962

2.  Autoradiographic localization of dopamine DA1 receptors in rat kidney with [3H]Sch 23390.

Authors:  T Huo; D P Healy
Journal:  Am J Physiol       Date:  1989-09

3.  Locally formed dopamine stimulates cAMP accumulation in LLC-PK1 cells via a DA1 dopamine receptor.

Authors:  A Grenader; D P Healy
Journal:  Am J Physiol       Date:  1991-06

Review 4.  The dopamine receptor in adult and maturing kidney.

Authors:  R A Felder; C C Felder; G M Eisner; P A Jose
Journal:  Am J Physiol       Date:  1989-09

5.  Evidence from functional and autoradiographic studies for the presence of tubular dopamine-1 receptors and their involvement in the renal effects of fenoldopam.

Authors:  S S Hedge; A Ricci; F Amenta; M F Lokhandwala
Journal:  J Pharmacol Exp Ther       Date:  1989-12       Impact factor: 4.030

6.  A68930: a potent agonist selective for the dopamine D1 receptor.

Authors:  M P DeNinno; R Schoenleber; R MacKenzie; D R Britton; K E Asin; C Briggs; J M Trugman; M Ackerman; L Artman; L Bednarz
Journal:  Eur J Pharmacol       Date:  1991-06-25       Impact factor: 4.432

7.  Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells.

Authors:  A Grenader; D P Healy
Journal:  J Pharmacol Exp Ther       Date:  1991-07-01       Impact factor: 4.030

8.  Role of kidney dopamine in the natriuretic response to volume expansion in rats.

Authors:  S S Hegde; A L Jadhav; M F Lokhandwala
Journal:  Hypertension       Date:  1989-06       Impact factor: 10.190

Review 9.  Clinical experience with intravenous fenoldopam.

Authors:  T L Holcslaw; T R Beck
Journal:  Am J Hypertens       Date:  1990-06       Impact factor: 2.689

  9 in total
  3 in total

1.  The effects of clozapine on behavioural responses to the selective 'D1-like' dopamine receptor agonist, A 68930, and to the selective 'D2-like' agonist, RU 24213.

Authors:  S A Daly; J L Waddington
Journal:  Br J Pharmacol       Date:  1994-11       Impact factor: 8.739

2.  The dopamine D1 receptor is expressed and facilitates relaxation in airway smooth muscle.

Authors:  Kentaro Mizuta; Yi Zhang; Dingbang Xu; Fumiko Mizuta; Frank D'Ovidio; Eiji Masaki; Charles W Emala
Journal:  Respir Res       Date:  2013-09-02

3.  The dopamine D1 receptor is expressed and induces CREB phosphorylation and MUC5AC expression in human airway epithelium.

Authors:  Nao Matsuyama; Sumire Shibata; Atsuko Matoba; Tada-Aki Kudo; Jennifer Danielsson; Atsushi Kohjitani; Eiji Masaki; Charles W Emala; Kentaro Mizuta
Journal:  Respir Res       Date:  2018-04-02
  3 in total

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