Tissue functions mediated by β3-adrenoceptors—findings and challenges

作者: Martin C. Michel , Peter Ochodnicky , Roger J. Summers

DOI: 10.1007/S00210-010-0529-2

关键词:

摘要: As β3-adrenoceptor agonists metamorphose from experimental tools into therapeutic drugs, it is vital to obtain a comprehensive picture of the cell and tissue functions mediated by this receptor subtype in humans. Human tissues with proven and/or high expression β3-adrenoceptors include urinary bladder, gall other parts gastrointestinal tract. While several have been proposed based on results obtained animals, their relevance humans remains uncertain. For instance, perform an important role thermogenesis lipolysis rodent brown white adipose tissue, respectively, but appears less significant. Moreover, use such as agonist BRL 37344 antagonist SR59230A demonstrate functional involvement may lead many cases misleading conclusions they can also interact β-adrenoceptor subtypes or even non-adrenoceptor targets. In conclusion, we propose that responses attributed stimulation need re-evaluation light development more selective tools. findings animals be extended order better understand potential additional indications side effects are beginning enter clinical medicine.

参考文章(71)
Ursula Ravens, Peter Molenaar, Torsten Christ, Alberto J. Kaumann, Evidence against beta-3-adrenoceptor-mediated increases in contractile force and L-type Ca2+ current ICa-L in human atrial myocardium at 37 degrees C Deutsche Gesellschaft fur Experimentelle und Klinische Pharmakologie und Toxikologie. ,(2010)
S B Liggett, R F Thomas, Lack of beta 3-adrenergic receptor mRNA expression in adipose and other metabolic tissues in the adult human. Molecular Pharmacology. ,vol. 43, pp. 343- 348 ,(1993)
Robert A. Ngala, Jacqueline O'Dowd, Steven J. Wang, Claire Stocker, Michael A. Cawthorne, Jonathan R.S. Arch, β2‐Adrenoceptors and non‐β‐adrenoceptors mediate effects of BRL37344 and clenbuterol on glucose uptake in soleus muscle: studies using knockout mice British Journal of Pharmacology. ,vol. 158, pp. 1676- 1682 ,(2009) , 10.1111/J.1476-5381.2009.00472.X
Bronwyn A. Evans, Masaaki Sato, Mohsin Sarwar, Dana S. Hutchinson, Roger J. Summers, Ligand-directed signalling at β-adrenoceptors British Journal of Pharmacology. ,vol. 159, pp. 1022- 1038 ,(2010) , 10.1111/J.1476-5381.2009.00602.X
M R Candelore, D E Macintyre, V S Susulic, B B Lowell, D S Fletcher, D Grujic, S Luell, Beta-3 Adrenergic Receptor Agonists Cause an Increase in Gastrointestinal Transit Time in Wild-type Mice, But Not in Mice Lacking the Beta-3 Adrenergic Receptor Journal of Pharmacology and Experimental Therapeutics. ,vol. 287, pp. 720- 724 ,(1998)
I Yamaguchi, H Kodama, K Kuratani, Enhancement of gastric mucosal blood flow by beta-3 adrenergic agonists prevents indomethacin-induced antral ulcer in the rat. Journal of Pharmacology and Experimental Therapeutics. ,vol. 270, pp. 559- 565 ,(1994)
Asami Mori, Tomoyo Miwa, Kenji Sakamoto, Tsutomu Nakahara, Kunio Ishii, Pharmacological evidence for the presence of functional β3-adrenoceptors in rat retinal blood vessels Naunyn-Schmiedeberg's Archives of Pharmacology. ,vol. 382, pp. 119- 126 ,(2010) , 10.1007/S00210-010-0526-5
Yoshitaka Tomiyama, Makoto Murakami, Yoshinobu Yamazaki, Masami Kojima, Masuo Akahane, Comparison between CL-316243- and CGP-12177A-induced relaxations in isolated canine ureter. Pharmacology. ,vol. 68, pp. 140- 146 ,(2003) , 10.1159/000070171
Carine Chavey, Marcus Mühlbauer, Carine Bossard, Ariane Freund, Sébastien Durand, Christian Jorgensen, Christian Jobin, Gwendal Lazennec, Interleukin-8 expression is regulated by histone deacetylases through the nuclear factor-kappaB pathway in breast cancer. Molecular Pharmacology. ,vol. 74, pp. 1359- 1366 ,(2008) , 10.1124/MOL.108.047332
Takahiro Horinouchi, Katsuo Koike, Agonistic activity of SR59230A at atypical β-adrenoceptors in guinea pig gastric fundus and duodenum European Journal of Pharmacology. ,vol. 416, pp. 165- 168 ,(2001) , 10.1016/S0014-2999(01)00854-8