ArticleBritish journal of pharmacology1999
Microphysiometric analysis of human alpha1a-adrenoceptor expressed in Chinese hamster ovary cells.
Article in British journal of pharmacology, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 24 citations in OpenAlex.
- Systemic Absorption of Cyclopentolate and Adverse Events After Retinopathy of Prematurity Exams.Current eye research · 2016Trial
- Adrenoceptors: Receptors, Ligands and Their Clinical Uses, Molecular Pharmacology and Assays.Handbook of experimental pharmacology · 2024Review
- The human endogenous metabolome as a pharmacology baseline for drug discovery.Drug discovery today · 2019Review
- Mirabegron relaxes urethral smooth muscle by a dual mechanism involving β3 -adrenoceptor activation and α1 -adrenoceptor blockade.British journal of pharmacology · 2016Article
- Phenotype pharmacology of lower urinary tract α(1)-adrenoceptors.British journal of pharmacology · 2012Review
- Adrenergic control of cardiac gap junction function and expression.Naunyn-Schmiedeberg's archives of pharmacology · 2011Review
- Identification of the alpha1L-adrenoceptor in rat cerebral cortex and possible relationship between alpha1L- and alpha1A-adrenoceptors.British journal of pharmacology · 2008Article
- Alpha-1-adrenoceptor subtype selective regulation of connexin 43 expression in rat cardiomyocytes.Naunyn-Schmiedeberg's archives of pharmacology · 2008Article
- Pharmacological characterization of unique prazosin-binding sites in human kidney.Naunyn-Schmiedeberg's archives of pharmacology · 2003Article
- Rapid acid extrusion response triggered by alpha(1) adrenoceptor in CHO cells.The Journal of physiology · 2001Article
- Inverse agonism and neutral antagonism at a constitutively active alpha-1a adrenoceptor.British journal of pharmacology · 2000Article
- Splice isoforms of alpha(1a)-adrenoceptor in rabbit.British journal of pharmacology · 2000Article
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. The human recombinant alpha1a-adrenoceptor (AR) has been stably expressed in Chinese hamster ovary cells. Four stable clones, aH4, aH5, aH6 and aH7, expressing 30, 370, 940 and 2900 fmol AR mg(-1) protein, respectively, have been employed to characterize this AR subtype using radioligand binding and microphysiometry to measure extracellular acidification rates. 2. Noradrenaline (NA) gave concentration-dependent responses in microphysiometry with increasing extracellular acidification rates. The potency of NA increased as the receptor density increased; pEC50 values of NA for the clones aH4, aH5, aH6 and aH7 were 6.9, 7.5, 7.8 and 8.1, respectively. This increase of potency according to receptor density indicates the presence of spare receptor for NA. Methoxamine, phenylephrine, oxymetazoline and clonidine also gave concentration-dependent responses with various intrinsic activities. 3. Antagonists shifted concentration-response curves for NA rightward in a concentration-dependent manner. Schild analysis revealed that the affinity profile of this AR subtype to antagonists in the clone aH7 had a typical pattern for the alpha1a-AR; high affinity for prazosin and WB 4101, and low affinity for BMY7378 (pA2=9.5, 9.8 and 7.3, respectively). This profile is similar in the case of the clone aH4. These affinities were in good agreement with those obtained in binding experiments. 4. These results have demonstrated that (1) classical receptor theory can be applied in microphysiometry, and (2) microphysiometry is a useful tool to investigate the pharmacological characterization of alpha1a-AR.
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