Cyproheptadine - Pharmacology

Pharmacology

Cyproheptadine is known to be an antagonist (or inverse agonist depending on the site in question) of the following receptors, listed in order of potency from greatest to least (K_i):

• H₁ (~0.05 nM) > 5-HT_2A (~2 nM) ≈ 5-HT_2B (~1.5 nM) ≈ 5-HT_2C (~2 nM) > mACh (M₁-M₅; ~7-12 nM) ≈ D₃ (~8 nM)

It also has weak but likely negligible affinity for the following sites (K_i):

• 5-HT_1A (~60-100 nM) ≈ α₁-adrenergic (?? nM) ≈ α₂-adrenergic (?? nM) > 5-HT₆ (~135-150 nM) ≈ 5-HT₇ (~125 nM) ≈ D₁ (~115 nM) ≈ D₂ (~115 nM) > 5-HT₃ (~250 nM) ≈ NET (~300 nM)

Additionally, cyproheptadine possesses calcium channel-blocking and local anesthetic properties.