binospirone

Binospirone (ORG GC 94) is a tetracyclic compound developed by Organon as a potential treatment for migraine and other essential headaches. It is chemically related to the antidepressant mianserin (Org GB 94). Pharmacologically, binospirone acts as a partial agonist at serotonin (5-HT) receptors, exhibiting a biphasic action in certain vascular beds where it can both potentiate and inhibit 5-HT responses. This mechanism is thought to correct deficiencies in central serotonin concentrations or turnover, similar to other anti-migraine agents like ergotamine and pizotifen. While it reached clinical evaluation in the late 1970s and early 1980s, its development appears to have been discontinued.

Other names

binospirone mesylate