DuP 734 是一种 sigma 受体拮抗剂，DuP 734 是一种有效的选择性 sigma 和 5-HT2 受体配体，对 D2 受体的亲和力弱。DuP 734 具有抗精神病活性，而没有抗精神病剂常见的副作用。

DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics.

Solid

Sigma receptor; 5-HT2 receptor; D2 receptor

DuP 734 potently blocks mescaline-induced scratching (ED 50 =0.35 mg/kg, p.o.) and aggressive activity (ED 50 =1.9 mg/kg, p.o.) and is relatively much weaker as an apomorphine antagonist (ED 50 =12 mg/kg, p.o.).
Administration of DuP 734 potently antagonizes the binding of [H]DuP 734 and [H](+)-SKF 10,047 to brain sigma receptors in vivo with ID 50 values of 0.02 and 0.07 mg/kg (0.07 and 0.25μmol/kg), respectively.
Following intravenous dosing, the disposition of DuP 734 in mice, rats, beagle dogs and cynomolgus monkeys is characterized by high total body systemic plasma clearance (46 to 87 mL/min/kg) and large steady-state volume of distribution (3.6 to 6.8 L/kg). The terminal elimination half-life ranged from 50 to 83 min.

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

[1]. L Cook, et al. DuP 734 [1-(cyclopropylmethyl)-4-(2(4-fluorophenyl)-2- Oxoethyl)piperidine HBr], a Potential Antipsychotic Agent: Preclinical Behavioral Effects. J Pharmacol Exp Ther. 1992 Dec;263(3):1159-66.
[2]. M Watanabe, et al. [H]1-(cyclopropylmethyl)-4-(2-(4-fluorophenyl)-2-oxoethyl) Piperidine HBr (DuP 734). A Selective Ligand for Sigma Receptors in Mouse Brain in Vivo. J Pharmacol Exp Ther. 1993 Sep;266(3):1541-8.

In Vitro: DMSO : 250 mg/mL (701.71 mM; Need ultrasonic)H₂O : ≥ 100 mg/mL (280.69 mM)