Subclassification and nomenclature of alpha- and beta-adrenoceptors.

@article{citeulike:1155469, abstract = {The subclassification of alpha- and beta-adrenoceptors has resulted in many opportunities for drug discovery. Important adrenoceptor targets include beta(2)-agonists as bronchodilators, beta(1) or beta(1)/beta(2) antagonists as antihypertensives, centrally acting alpha(2)-agonists for a variety of applications and alpha(1)-antagonists for hypertension and benign prostatic hyperplasia. The pharmacology and nomenclature of 9 adrenoceptors is now established, with alpha(1), alpha(2) and beta-adrenoceptors being divided into three subtypes each. It is unlikely that additional discrete adrenoceptor sequences will be identified; however the presence of "affinity states" can give rise to tissue specific differences in pharmacology for a specific subtype. Polymorphisms and splice variants of adrenoceptors continue to be identified; in some cases these modifications can affect pharmacological characteristics and could influence the efficacy of adrenoceptor-targeted therapy. Selective antagonists are now available of all 9 adrenoceptor subtypes. Although these will not all have therapeutic application, the availability of improved pharmacologic tools could lead to the identification of new adrenoceptor targets.}, address = {Dept of Urogenital Pharmacology, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, Pennsylvania, 19406-0939, USA. j\_paul\_hieble@gsk.com}, author = {Hieble, J. P. }, citeulike-article-id = {1155469}, issn = {1873-4294}, journal = {Curr Top Med Chem}, keywords = {agonist, b2ar, drug, genome, ligands, pharmacology, review}, number = {2}, pages = {129--134}, posted-at = {2007-03-12 14:33:19}, priority = {2}, title = {Subclassification and nomenclature of alpha- and beta-adrenoceptors.}, url = {http://view.ncbi.nlm.nih.gov/pubmed/17266601}, volume = {7}, year = {2007} }

TY - JOUR ID - citeulike:1155469 L3 - citeulike-article-id:1155469 TI - Subclassification and nomenclature of alpha- and beta-adrenoceptors. JF - Curr Top Med Chem VL - 7 IS - 2 SP - 129 EP - 134 AD - Dept of Urogenital Pharmacology, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, Pennsylvania, 19406-0939, USA. j_paul_hieble@gsk.com SN - 1873-4294 N2 - The subclassification of alpha- and beta-adrenoceptors has resulted in many opportunities for drug discovery. Important adrenoceptor targets include beta(2)-agonists as bronchodilators, beta(1) or beta(1)/beta(2) antagonists as antihypertensives, centrally acting alpha(2)-agonists for a variety of applications and alpha(1)-antagonists for hypertension and benign prostatic hyperplasia. The pharmacology and nomenclature of 9 adrenoceptors is now established, with alpha(1), alpha(2) and beta-adrenoceptors being divided into three subtypes each. It is unlikely that additional discrete adrenoceptor sequences will be identified; however the presence of "affinity states" can give rise to tissue specific differences in pharmacology for a specific subtype. Polymorphisms and splice variants of adrenoceptors continue to be identified; in some cases these modifications can affect pharmacological characteristics and could influence the efficacy of adrenoceptor-targeted therapy. Selective antagonists are now available of all 9 adrenoceptor subtypes. Although these will not all have therapeutic application, the availability of improved pharmacologic tools could lead to the identification of new adrenoceptor targets. KW - agonist KW - b2ar KW - drug KW - genome KW - ligands KW - pharmacology KW - review AU - Hieble, JP PY - 2007/// UR - http://view.ncbi.nlm.nih.gov/pubmed/17266601 ER -