a full pharmacological analysis of the three turkey β-adrenoceptors and comparison with the human β-adrenoceptors一个完整的药理分析三个土耳其与人类β-adrenoceptorsβ-adrenoceptors和比较.pdfVIP

a full pharmacological analysis of the three turkey β-adrenoceptors and comparison with the human β-adrenoceptors一个完整的药理分析三个土耳其与人类β-adrenoceptorsβ-adrenoceptors和比较.pdf

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a full pharmacological analysis of the three turkey β-adrenoceptors and comparison with the human β-adrenoceptors一个完整的药理分析三个土耳其与人类β-adrenoceptorsβ-adrenoceptors和比较

A Full Pharmacological Analysis of the Three Turkey b- Adrenoceptors and Comparison with the Human b- Adrenoceptors Jillian G. Baker* Wellcome Trust Clinician Scientist Fellow, Institute of Cell Signalling, University of Nottingham, Nottingham, United Kingdom Abstract Background: There are three turkey b-adrenoceptors: the original turkey b-adrenoceptor from erythrocytes (tbtrunc, for which the X-ray crystal structure has recently been determined), tb3C and tb4C-receptors. This study examined the similarities and differences between these avian receptors and mammalian receptors with regards to binding characteristics and functional high and low affinity agonist conformations. Methodology/Principal Findings: Stable cell lines were constructed with each of the turkey b-adrenoceptors and 3H- CGP12177 whole cell binding, CRE-SPAP production and 3H-cAMP accumulation assays performed. It was confirmed that the three turkey b-adrenoceptors are distinct from each other in terms of amino acid sequence and binding characteristics. The greatest similarity of any of the turkey b-adrenoceptors to human b-adrenoceptors is between the turkey b3C-receptor and the human b2-adrenoceptor. There are pharmacologically distinct differences between the binding of ligands for the tbtrunc and tb4C and the human b-adrenoceptors (e.g. with CGP20712A and ICI118551). The tbtrunc and tb4C- adrenoceptors appear to exist in at least two different agonist conformations in a similar manner to that seen at both the human and rat b1-adrenoceptor and human b3-adrenoceptors. The tb3C-receptor, similar to the human b2-adrenoceptor, does not, at least so far, appear to exist in more than one agonist conformation. Conclusions/Significance: There are several similarities, but also se

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