Pharmacodynamics +<unk>  Site Ki (nM) Action Species Ref. H1 0.06 ↓ Human H2 H3 >10,000 Human H4 202 Human M1 12 ↓ Human M2 7 ↓ Human M3 12 ↓ Human M4 8 ↓ Human M5 11.8 ↓ Human 5-HT1A 59 ↓ Human 5-HT2A 1.67 ↓ Human 5-HT2B 1.54 ↓ Human 5-HT2C 2.23 ↓ Human 5-HT3 228 Mouse 5-HT6 142 Human 5-HT7 123 Human D1 117 Human D2 112 ↓ Human D3 8 Human 4,100 Rat 290 Rat<unk>  is a very potent antihistamine or inverse agonist of the H1 receptor. At higher concentrations, it also has anticholinergic, antiserotonergic, and antidopaminergic activities. Of the serotonin receptors, it is an especially potent antagonist of the 5-HT2 receptors. This is thought to underlie its effectiveness in the treatment of serotonin syndrome. However, it is possible that blockade of 5-HT1 receptors may also contribute to its effectiveness in serotonin syndrome.<unk>  has been reported to block 85% of 5-HT2 receptors in the human brain at a dose of 4 mg three times per day (12 mg/day total) and to block 95% of 5-HT2 receptors in the human brain at a dose of 6 mg three times per day (18 mg/day total) as measured with positron emission tomography (PET). The dose of<unk>  recommended to ensure blockade of the 5-HT2 receptors for serotonin syndrome is 20 to 30 mg. Besides its activity at neurotransmitter targets,<unk>  has been reported to possess weak antiandrogenic activity. Pharmacokinetics<unk>  is well-absorbed following oral ingestion, with peak plasma levels occurring after 1 to 3 hours. Its terminal half-life when taken orally is approximately 8 hours.
Cyproheptadine
Tripelennamine
Tianeptine
Apomorphine
Alosetron
Tropisetron
Palonosetron
Cilansetron