Abstract：
:It is generally accepted that seven-transmembrane receptors have the capacity to regulate cellular signaling systems in the absence of occupancy by a ligand (i.e. the receptors display constitutive activity). Drugs can increase (agonists), decrease (inverse agonists) or not change (antagonists) receptor activity towards a cellular effector. Moreover, some drugs (protean ligands) have multiple pharmacological properties (e.g. agonism towards one response and inverse agonism towards another response coupled to the same receptor and measured from the same cells, simultaneously). In this article, we describe response-dependent constitutive activity and ligand pharmacology for 5-HT2A and 5-HT2C receptors in vitro. Moreover, we provide evidence that 5-HT2A and 5-HT2C receptor constitutive activity is physiologically relevant in vivo and suggest that strong consideration should be given to the impact of constitutive receptor activity on disease and the therapeutic potential of inverse agonism.
journal_name
Trends Pharmacol Scijournal_title
Trends in pharmacological sciencesauthors
Berg KA,Harvey JA,Spampinato U,Clarke WPdoi
10.1016/j.tips.2005.10.008subject
Has Abstractpub_date
2005-12-01 00:00:00pages
625-30issue
12eissn
0165-6147issn
1873-3735pii
S0165-6147(05)00274-9journal_volume
26pub_type
杂志文章,评审abstract：:Urinary incontinence and other urinary storage symptoms are frequent in the general population but available treatments have limited efficacy and tolerability. Rho kinase (ROCK) has a central role in the regulation of smooth muscle contraction, including that of the urinary bladder. Recent experimental evidence indica...
journal_title：Trends in pharmacological sciences
pub_type： 杂志文章,评审
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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doi：10.1016/j.tips.2007.02.009
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journal_title：Trends in pharmacological sciences
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doi：10.1016/j.tips.2006.09.002
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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