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BF-1

Development stage: Preclinical
Lead developer: Biofrontera
Modality: Small Molecules

Overview

BF-1 is a highly selective, small molecule **5-HT2B (serotonin 2B) receptor antagonist** developed by **Biofrontera AG** for the prophylactic treatment of **migraine**. It was specifically designed to overcome the safety limitations of earlier, non-selective 5-HT2B antagonists, which were associated with monoaminergic side effects and valvular heart disease. BF-1 demonstrates high affinity (pKi 10.05) and potency (IC50 2.6 nM) for the 5-HT2B receptor. Its primary mechanism involves blocking neurogenic dural plasma protein extravasation, a process implicated in the development of migraine pain.

Targets

5-HT2C (5-hydroxytryptamine receptor 2C)HTR7 (5-hydroxytryptamine receptor 7)HTR2B (5-Hydroxytryptamine Receptor 2B)

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