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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

383.51

C₂₁H₂₅N₃O₂S

142477-34-7

Solid

White to off-white

O=C1SC2=CC(CCN3CCN(C4=CC=CC=C4OC)CC3)=CC=C2N1C

Room temperature in continental US; may vary elsewhere.

• [1]. Taverne T, et al. Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. J Med Chem. 1998 Jun 4;41(12):2010-8.  [Content Brief]