PNU 177864 hydrochloride

PNU-177864 hydrochloride is a potent, selective and orally active dopamine D3 receptor antagonist. PNU-177864 hydrochloride is structurally consistent with a cationic amphiphilic drug (CAD) and induces phospholipidosis in vivo. PNU-177864 hydrochloride antischizophrenic activity[1][2].

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

D3 Receptor

PNU-177864 (12.5-200 mg/kg; oral gavage; daily; for 2-4 weeks; Sprague-Dawley rats) treatment induces phospholipidosis in unusual target organs in dogs or rats including epididymis, pituitary, and hair follicles[1]. Animal Model: Male and female Sprague-Dawley rats (8-9-week-old)[1] Dosage: 12.5 mg/kg, 50 mg/kg (for 2 weeks), or 200 mg/kg; 8 mg/kg, 25 mg/kg, or 80 mg/kg (for 4 weeks) Administration: Oral gavage; daily; for 2-4 weeks Result: Induced phospholipidosis in unusual target organs in dogs or rats including epididymis, pituitary, and hair follicles.

[1]. Rudmann DG, et al. Epididymal and systemic phospholipidosis in rats and dogs treated with the dopamine D3 selective antagonist PNU-177864. Toxicol Pathol. 2004 May-Jun;32(3):326-32.

[2]. Vonderfecht SL, et al. Myopathy related to administration of a cationic amphiphilic drug and the use of multidose drug distribution analysis to predict its occurrence. Toxicol Pathol. 2004 May-Jun;32(3):318-25.