Abstract

A novel alpha 1-adrenergic receptor subtype has been cloned from a bovine brain cDNA library. The deduced amino acid sequence is that of a 466-residue polypeptide. The structure is similar to that of the other adrenergic receptors as well as the larger family of G protein-coupled receptors that have a presumed seven-membrane-spanning domain topography. The greatest sequence identity of this receptor protein is with the previously cloned hamster alpha 1B-adrenergic receptor being approximately 72% within the presumed membrane-spanning domains. Localization on different human chromosomes provides evidence that the bovine cDNA is distinct from the hamster alpha 1B-adrenergic receptor. The bovine cDNA clone expressed in COS7 cells revealed 10-fold higher affinity for the alpha 1-adrenergic antagonists WB4101 and phentolamine and the agonist oxymetazoline as compared with the alpha 1B receptor, results similar to pharmacologic binding properties described for the alpha 1A receptor. Despite these similarities in pharmacological profiles, the bovine alpha 1-adrenergic receptor is sensitive to inhibition by the alkylating agent chloroethylclonidine unlike the alpha 1A-adrenergic receptor subtype. In addition, a lack of expression in tissues where the alpha 1A subtype exists suggests that this receptor may actually represent a novel alpha 1-adrenergic receptor subtype not previously appreciated by pharmacological criteria.

Highlights

  • A novel al-adrenergic receptor subtype has been cloned from a bovine brain cDNA library

  • The bovine cDNA clone expressed in COS7 cells revealed lo-fold higher affinity for the al-adrenergic antagonists WB4101 and phentolamine and the agonist oxymetazoline as compared with the

  • We present the cloning, sequencing, and expression of another oc,adrenergic receptor subtype from bovine brain. This receptor shows the pharmacological properties proposed for the cYIA-adrenergic receptor subtype, but on the basis of a lack of expression in tissues where the alA subtype exists and its sensitivity to CEC’, it may represent a novel a!,adrenergic receptor subtype not previously appreciated by pharmacological criteria

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Summary

Introduction

A novel al-adrenergic receptor subtype has been cloned from a bovine brain cDNA library. The bovine cDNA clone expressed in COS7 cells revealed lo-fold higher affinity for the al-adrenergic antagonists WB4101 and phentolamine and the agonist oxymetazoline as compared with the We present the cloning, sequencing, and expression of another oc,-adrenergic receptor subtype from bovine brain This receptor shows the pharmacological properties proposed for the cYIA-adrenergic receptor subtype, but on the basis of a lack of expression in tissues where the alA subtype exists and its sensitivity to CEC’, it may represent a novel a!,-adrenergic receptor subtype not previously appreciated by pharmacological criteria

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