tcsc0018442 5-HT1A modulator 1

5-HT1A modulator 1 displays very high affinities for the 5HT_1A, adrenergic α₁ and dopamine D₂ receptor with IC₅₀s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.

IC50 & Target: IC50: 2±0.3 nM (5-HT_1A receptor), 300±55 nM (5-HT_1B receptor), 500±75 nM (5-HT_2A receptor), 4000±440 nM (5-HT_2C receptor), 10±3 nM (Adrenergic α₁ receptor), 40±9 nM (Dopamine D₂ receptor)^[1]

In Vitro: 5-HT1A modulator 1 (Compound 24) also displays affinities for the 5HT_1B, 5-HT_2A and 5-HT_2C receptor with IC₅₀s of 300±55 nM, 500±75 nM, and 4000±440 nM, respectively^[1].

In Vivo: 5-HT1A modulator 1 (Compound 24) shows clear antagonist action at 5HT_2A receptor subtype in mice. The antagonism is nearly complete at the dose of 1 mg/kg ip for 5-HT1A modulator 1 (94% of antagonism, p<0.01). 5-HT1A modulator 1 completely blocks the stereotypies and the climbing at the dose of 1 mg/kg ip (100% of antagonism). 5-HT1A modulator 1 is also tested in rats, using the same paradigm. After oral administration, 5-HT1A modulator 1 significantly (p<0.05) reduces the hyperactivity by 50% at the doses of 2 and 4 mg/kg po, respectively 63% and 58% of antagonism for 5-HT1A modulator 1; the antagonism is complete (103% and 108%) at the respective doses of 8 and 16 mg/kg po for 5-HT1A modulator 1 (p<0.01)^[1].