Assay Requirements and Technologies

The first requirement of an in vitro safety profiling assay is to be as predictive as possible of an adverse event, given all the limitations of in vitro assays and the other important parameters to consider in combination, such as physicochemical 

Serotonin 5-HT 2B receptor HTR2B Agonism Cardiac valvulopathy, fibroblast mitogenesis, hypertension. Antagonism No side effects clearly defined, but cardiac effects cannot be excluded, especially at embryonic stage. 

Adenosine 2a receptor ADORA2A Agonism Inhibition of platelet aggregation, anti-inflammation and neuroprotective effects, coronary vasodilation, decreased blood pressure, increased plasma renin activity and sleep induction. Antagonism Increased platelet aggregation, hypertension, nervousness (tremor, agitation), arousal, insomnia, cerebral and coronary vasodilation (in microvessels only). 

Adenosine 3 receptor ADORA3 Agonism Immunosuppression, hypotension, anti-ischaemic (cardioprotective), pro-ischaemic (cerebral), cell necrosis, cell proliferation and angiogenesis. Antagonism might cause myocardial ischaemia, proinflammatory effects, hypertension and interfere with the regulation of cell growth. 

Adrenergic Alpha lA receptor ADRAIA Agonism Smooth muscle contraction (prostate in particular, effects on the lower urinary tract) and cardiac positive ionotropy, arrhythmia. Antagonism Orthostatic hypotension and other blood pressure related adverse effects and impact on various aspects of sexual function. 

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