NLX-112 (also known as befiradol or F13640) is a highly selective 5-HT1A receptor full agonist with >1000-fold selectivity compared to other types of receptors. It has been investigated for the treatment of Parkinson′s disease patients who exhibit L-DOPA-induced dyskinesia
Serotonin 5-HT1A receptor full agonist
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L-DOPA is the gold-standard treatment for Parkinson's disease (PD), but induces troublesome dyskinesia after prolonged treatment. This is associated with the 'false neurotransmitter' conversion of L-DOPA to dopamine by serotonin neurons projecting from the raphe to the dorsal striatum. Reducing
The Journal of pharmacy and pharmacology, 69(9), 1178-1190 (2017-06-15)
NLX-112 (befiradol, F13640) is a selective serotonin 5-HT1A receptor agonist. Although it has been tested in vivo, little has been reported on its in vitro signal transduction profile. NLX-112 was tested on G-protein activation, inhibition of adenylyl cyclase, ERK1/2 phosphorylation (pERK)
Although l-DOPA alleviates the motor symptoms of Parkinson's disease (PD), it elicits troublesome l-DOPA-induced dyskinesia (LID) in a majority of PD patients after prolonged treatment. This is likely due to conversion of l-DOPA to dopamine as a 'false neurotransmitter' from
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