Raseglurant (
INN
Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...
) (code name ADX-10059) is a
negative allosteric modulator
In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimulus. Some of them, like benzodiazepines, are drugs. The site that an allosteric modulator binds t ...
of the
mGlu5 receptor and
derivative
In mathematics, the derivative of a function of a real variable measures the sensitivity to change of the function value (output value) with respect to a change in its argument (input value). Derivatives are a fundamental tool of calculus. F ...
of
MPEP which was under development by
Addex Therapeutics for the treatment of
migraine
Migraine (, ) is a common neurological disorder characterized by recurrent headaches. Typically, the associated headache affects one side of the head, is pulsating in nature, may be moderate to severe in intensity, and could last from a few hou ...
,
gastroesophageal reflux disease
Gastroesophageal reflux disease (GERD) or gastro-oesophageal reflux disease (GORD) is one of the upper gastrointestinal chronic diseases where stomach content persistently and regularly flows up into the esophagus, resulting in symptoms and/ ...
, and
dental anxiety
Dental fear, or dentophobia, is a normal emotional reaction to one or more specific threatening stimuli in the dental situation. However, dental anxiety is indicative of a state of apprehension that something dreadful is going to happen in relatio ...
.
It reached
phase II clinical trial
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietar ...
s for all of the aforementioned indications before being discontinued due to the observation of possible predictive signs of
hepatotoxicity
Hepatotoxicity (from ''hepatic toxicity'') implies chemical-driven liver damage. Drug-induced liver injury is a cause of acute and chronic liver disease caused specifically by medications and the most common reason for a drug to be withdrawn fro ...
in patients with long-term use.
See also
*
Basimglurant
Basimglurant (INN) (developmental code names RG-7090, RO-4917523) is a negative allosteric modulator of the mGlu5 receptor which is under development by Roche and Chugai Pharmaceutical for the treatment of treatment-resistant depression (as an ...
*
Dipraglurant
Dipraglurant (INN) (code name ADX-48621) is a negative allosteric modulator of the mGlu5 receptor which is under development by Addex Therapeutics for the treatment of Parkinson's disease levodopa-induced dyskinesia (PD-LID). As of 2014, it is i ...
*
Fenobam
Fenobam is an imidazole derivative developed by McNeil Laboratories in the late 1970s as a novel anxiolytic drug with an at-the-time-unidentified molecular target in the brain. Subsequently, it was determined that fenobam acts as a potent and s ...
*
Mavoglurant
Mavoglurant (developmental code name AFQ-056) is an experimental drug candidate for the treatment of fragile X syndrome and other conditions which has been discontinued. It exerts its effect as an antagonist of the metabotropic glutamate recepto ...
References
External links
Development of ADX10059 Ended for Long-term Use - Addex Therapeutics
MGlu5 receptor antagonists
Fluoroarenes
Aminopyridines
Alkyne derivatives
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