Drug intelligence / Profile preview

talipexole

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral, Intramuscular, Subcutaneous
01

Overview

Talipexole (B-HT 920) is a synthetic small molecule dopamine agonist that acts primarily at dopamine D2 receptors with agonist activity at both pre- and post-synaptic sites, as well as agonist activity at alpha-2 adrenoceptors and antagonist activity at 5-HT3 serotonin receptors. It is structurally characterized as an azepine derivative. Talipexole has been marketed under the brand name Domnin in Japan as an antiparkinsonian medication and has also been investigated for its effects on negative symptoms of schizophrenia. Its mechanism of action includes stimulation of dopaminergic signaling, inhibition of presynaptic dopamine release via autoreceptor activation, α2-adrenergic receptor agonism, and selective blockade of 5-HT3 serotonin channels. Talipexole was developed by Boehringer Ingelheim, introduced in Japan in 1996 and has not been approved in the US or Europe[1][3][4][5][6][7][8].

Brand names
Domnin
Other names
talipexole dihydrochloride6-allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride5,6,7,8-tetrahydro-6-(2-propenyl)-4H-thiazolo[4,5-d]azepine-2-amine dihydrochloride
02

Targets

ADRA2A (α2A)DRD2 (Dopamine D2 Receptor)HTR3A (5-hydroxytryptamine receptor 3A)

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