Biochemical and Biophysical Research Communications
Regular ArticleCloning, Expression and Characterization of Human α Adrenergic Receptors α1a, α1b and α1c
References (0)
Cited by (106)
Identification of 3,4-dihydro-2H-thiochromene 1,1-dioxide derivatives with a phenoxyethylamine group as highly potent and selective α<inf>1D</inf> adrenoceptor antagonists
2017, European Journal of Medicinal ChemistryCitation Excerpt :The α1 adrenergic receptors (α1 adrenoceptors, α1–ARs) are a part of the G protein-coupled receptor (GPCR) superfamily and are classified into three receptor subtypes, α1A, α1B and α1D-ARs [1–4].
Discovery of LASSBio-772, a 1,3-benzodioxole N-phenylpiperazine derivative with potent alpha 1A/D-Adrenergic receptor blocking properties
2011, European Journal of Medicinal ChemistryCitation Excerpt :After the initial identification of the two main groups of adrenoceptors (AR), i.e. alpha-AR and beta-AR, their functional role has been progressively elucidated and their subclassification has been refined into alpha 1, alpha 2, beta 1, beta 2 and beta 3 [2,3]. Alpha 1-AR subtypes, i.e. alpha 1A, alpha 1B, and alpha 1D [4–6], have distinct pharmacology and tissue expression [7–9], a fact relevant for the treatment of several diseases, such as hypertension and the obstructive symptoms of the lower urinary tract [10], including the secondary urinary obstruction produced by benign prostatic hyperplasia (BPH) [8,11–13]. Alternatively to surgical procedures, alpha 1-AR antagonists are efficient to relief the obstructive symptoms of BPH by decreasing the prostatic muscular tonus, mainly through the blockage of alpha 1A-AR [14].
α <inf>1D</inf> -Adrenergic receptors. Constitutive activity and reduced expression at the plasma membrane
2010, Methods in EnzymologyCitation Excerpt :Rat α1D-ARs were initially cloned by Lomasney et al. (1991) and afterward identified as the α1D subtype by Perez et al. (1991). The human ortholog was subsequently cloned and the gene located at chromosome 20 (Forray et al., 1994; Schwinn et al., 1995; Weinberg et al., 1994). The rat ortholog has 561 amino acids with a protein molecular weight of 59,364 Da whereas the human receptor has 572 amino acids and a protein molecular weight of 60,462 Da.
Receptor tyrosine kinases regulate α<inf>1D</inf>-adrenoceptor signaling properties: Phosphorylation and desensitization
2009, International Journal of Biochemistry and Cell BiologyThe antagonistic effect of antipsychotic drugs on a HEK293 cell line stably expressing human α<inf>1A1</inf>-adrenoceptors
2008, European Journal of Pharmacology