Title: Rolipram
CAS Registry Number: 61413-54-5
CAS Name: 4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone
Manufacturers' Codes: ZK-62711
Molecular Formula: C16H21NO3
Molecular Weight: 275.34
Percent Composition: C 69.79%, H 7.69%, N 5.09%, O 17.43%
Literature References: Prototypical selective phosphodiesterase 4 (PDE4) inhibitor. Prepn: BE 826923; R. Schmiechen et al., US 4193926 (1975, 1980 both to Schering AG). Selective enzyme inhibition and enhancement of cAMP accumulation in rat brain tissue: U. Schwabe et al., Mol. Pharmacol. 12, 900 (1976). Antidepressant mechanism of action study: H. Wachtel, Neuropharmacology 22, 267 (1983). Receptor binding study: H. H. Schneider et al., Eur. J. Pharmacol. 127, 105 (1986). Pharmacokinetics: W. Krause, G. Kühne, Xenobiotica 18, 561 (1988). Clinical evaluation in severe depression: F. Eckmann et al., Curr. Ther. Res. 43, 291 (1988). Pharmacology and efficacy in exptl autoimmune encephalomyelitis: N. Sommer et al., Nat. Med. 1, 244 (1995).
Properties: Crystals from ethyl acetate, mp 132°.
Melting point: mp 132°
Use: Pharmacological tool for characterization of phosphodiesterase isoenzymes.
Therap-Cat: Antidepressant. |