Matches in SemOpenAlex for { <https://semopenalex.org/work/W196858819> ?p ?o ?g. }
- W196858819 endingPage "60" @default.
- W196858819 startingPage "37" @default.
- W196858819 abstract "Increasing numbers of compounds, previously classified as antagonists, were shown to inhibit this spontaneous or constitutive receptor activity, instead of leave it unaffected as expected for a formal antagonist. In addition, some other antagonists did not have any effect by themselves, but prevented the inhibition of constitutive activity induced by thought-to-be antagonists. These thought-to-be antagonists with negative efficacy are now known as “inverse agonists.” Inverse agonism at βAR has been evidenced for both subtypes in wild-type GPCRs systems and in engineered systems with high constitutive activity. It is important to mention that native systems are of particular importance for analyzing the in vivo relevance of constitutive activity because these systems have physiological expression levels of target receptors. Studies of inverse agonism of β blockers in physiological setting have also evidenced that pathophysiological conditions can affect pharmacodynamic properties of these ligands. To date, hundreds of clinically well-known drugs have been tested and classified for this property. Prominent examples include the beta-blockers propranolol, alprenolol, pindolol, and timolol used for treating hypertension, angina pectoris, and arrhythmia that act on the β2ARs, metoprolol, and bisoprolol used for treating hypertension, coronary heart disease, and arrhythmias by acting on β1ARs. Inverse agonists seem to be useful in the treatment of chronic disease characterized by harmful effects resulting from β1AR and β2AR overactivation, such as heart failure and asthma, respectively." @default.
- W196858819 created "2016-06-24" @default.
- W196858819 creator A5001379512 @default.
- W196858819 creator A5039686693 @default.
- W196858819 creator A5045403820 @default.
- W196858819 date "2010-01-01" @default.
- W196858819 modified "2023-10-10" @default.
- W196858819 title "Measurement of Inverse Agonism in β-Adrenoceptors" @default.
- W196858819 cites W1489775551 @default.
- W196858819 cites W1491114612 @default.
- W196858819 cites W1539231406 @default.
- W196858819 cites W157937727 @default.
- W196858819 cites W1586466064 @default.
- W196858819 cites W1769585641 @default.
- W196858819 cites W1855952875 @default.
- W196858819 cites W1931989857 @default.
- W196858819 cites W1963763914 @default.
- W196858819 cites W1964191104 @default.
- W196858819 cites W1965835906 @default.
- W196858819 cites W1967099995 @default.
- W196858819 cites W1968125885 @default.
- W196858819 cites W1968604533 @default.
- W196858819 cites W1969931674 @default.
- W196858819 cites W1970006678 @default.
- W196858819 cites W1980017048 @default.
- W196858819 cites W1980358526 @default.
- W196858819 cites W1981047025 @default.
- W196858819 cites W1981731045 @default.
- W196858819 cites W1985826042 @default.
- W196858819 cites W1990813403 @default.
- W196858819 cites W1991138299 @default.
- W196858819 cites W1991398722 @default.
- W196858819 cites W1992540995 @default.
- W196858819 cites W1994969848 @default.
- W196858819 cites W1999921744 @default.
- W196858819 cites W2001033076 @default.
- W196858819 cites W2001438720 @default.
- W196858819 cites W2002896923 @default.
- W196858819 cites W2004328970 @default.
- W196858819 cites W2008985170 @default.
- W196858819 cites W2009068572 @default.
- W196858819 cites W2013576776 @default.
- W196858819 cites W2013644228 @default.
- W196858819 cites W2015912619 @default.
- W196858819 cites W2016449014 @default.
- W196858819 cites W2016736407 @default.
- W196858819 cites W2021294213 @default.
- W196858819 cites W2021301705 @default.
- W196858819 cites W2023724239 @default.
- W196858819 cites W2024712635 @default.
- W196858819 cites W2034315036 @default.
- W196858819 cites W2035098682 @default.
- W196858819 cites W2040933762 @default.
- W196858819 cites W2042845128 @default.
- W196858819 cites W2044190119 @default.
- W196858819 cites W2046610430 @default.
- W196858819 cites W2046787882 @default.
- W196858819 cites W2048731323 @default.
- W196858819 cites W2051197841 @default.
- W196858819 cites W2054046898 @default.
- W196858819 cites W2055440970 @default.
- W196858819 cites W2056216587 @default.
- W196858819 cites W2057803818 @default.
- W196858819 cites W2058089380 @default.
- W196858819 cites W2060259870 @default.
- W196858819 cites W2064746296 @default.
- W196858819 cites W2065812771 @default.
- W196858819 cites W2066564095 @default.
- W196858819 cites W2067693762 @default.
- W196858819 cites W2068031204 @default.
- W196858819 cites W2068315807 @default.
- W196858819 cites W2068769204 @default.
- W196858819 cites W2071691692 @default.
- W196858819 cites W2071841509 @default.
- W196858819 cites W2072289094 @default.
- W196858819 cites W2072372524 @default.
- W196858819 cites W2076685644 @default.
- W196858819 cites W2076983520 @default.
- W196858819 cites W2077425788 @default.
- W196858819 cites W2077706015 @default.
- W196858819 cites W2078721878 @default.
- W196858819 cites W2081423064 @default.
- W196858819 cites W2083220635 @default.
- W196858819 cites W2083810814 @default.
- W196858819 cites W2087047630 @default.
- W196858819 cites W2088844067 @default.
- W196858819 cites W2092754405 @default.
- W196858819 cites W2093638860 @default.
- W196858819 cites W2096028625 @default.
- W196858819 cites W2099062455 @default.
- W196858819 cites W2104483434 @default.
- W196858819 cites W2111331556 @default.
- W196858819 cites W2117031715 @default.
- W196858819 cites W2120062223 @default.
- W196858819 cites W2121279599 @default.
- W196858819 cites W2123495845 @default.
- W196858819 cites W2127160263 @default.
- W196858819 cites W2128827219 @default.