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The rat homologue of the bovine alpha 1c-adrenergic receptor shows the pharmacological properties of the classical alpha 1A subtype.

Authors: Laz, TM  Forray, C  Smith, KE  Bard, JA  Vaysse, PJ  Branchek, TA  Weinshank, RL 
Citation: Laz TM, etal., Mol Pharmacol 1994 Sep;46(3):414-22.
Pubmed: (View Article at PubMed) PMID:7935320

The cDNA for the rat alpha 1c-adrenergic receptor (AR) has been cloned using a probe derived from the bovine alpha 1c-AR sequence. Clone rB7a has a 2.6-kilobase insert with a 1390-base pair open reading frame and encodes a receptor of 466 amino acids. The cloned receptor has 91% amino acid identity with the bovine alpha 1c-AR. The rat alpha 1c-AR mRNA was detected in tissues known to be enriched for the alpha 1A-AR subtype, including vas deferens, heart, kidney, and hippocampus. Rat alpha 1c-AR mRNA was absent from liver and spleen when assayed by Northern blot analyses and RNase protection assays. In COS-7 cells transfected with cDNAs encoding the three rat alpha 1-ARs, WB-4101 and benoxathian had similar binding affinities for the alpha 1a/d-AR and the alpha 1c-AR and 10-fold lower affinities for the alpha 1b-AR. The affinity of 5-methylurapidil was found to be 10- and 30-fold higher at the alpha 1c-AR than at the alpha 1a/d- and alpha 1b-ARs, respectively. (S)-(+)-Niguldipine was found to have high affinity for the rat alpha 1c-AR, with 42- and 22-fold lower affinity at the alpha 1a/d- and alpha 1b-ARs, respectively. Treatment of intact transfected COS-7 cells with chlorethylclonidine resulted in the inactivation of 19% of the alpha 1c-ARs, in contrast to 72% and 85% inactivation of the alpha 1a/d- and alpha 1b-ARs, respectively. Similarly to the other two alpha 1-ARs, the rat alpha 1c-AR is coupled to the activation of phospholipase C. Our data suggest that the rat alpha 1c-AR cDNA encodes an alpha 1-AR with the pharmacological properties previously defined for the alpha 1A subtype found in tissues.


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CRRD Object Information
CRRD ID: 69745
Created: 2002-01-08
Species: All species
Last Modified: 2002-01-08
Status: ACTIVE


RGD is funded by grant HL64541 from the National Heart, Lung, and Blood Institute on behalf of the NIH.