Title: Cabergoline
CAS Registry Number: 81409-90-7
CAS Name: (8b)-N-[3-(Dimethylamino)propyl]-N-[(ethylamino)carbonyl]-6-(2-propenyl)ergoline-8-carboxamide
Additional Names: 1-ethyl-3-(3¢-dimethylaminopropyl)-3-(6¢-allylergoline-8¢b-carbonyl)urea; 1-[(6-allylergoline-8b-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea
Manufacturers' Codes: FCE-21336
Trademarks: Dostinex (Pharmacia & Upjohn)
Molecular Formula: C26H37N5O2
Molecular Weight: 451.60
Percent Composition: C 69.15%, H 8.26%, N 15.51%, O 7.09%
Literature References: Dopamine D2-receptor agonist. Prepn: P. Salvati et al., BE 888243; eidem, US 4526892 (1981, 1985 both to Farmitalia Carlo Erba). Prepn and bioactivity: E. Brambilla et al., Eur. J. Med. Chem. 24, 421 (1989). Clinical pharmacology: C. Ferrari et al., J. Clin. Endocrinol. Metab. 63, 941 (1986). Veterinary trial as abortifacient in dogs: K. Post et al., Theriogenology 29, 1233 (1988). Clinical evaluation to prevent puerperal lactation: G. B. Melis et al., Obstet. Gynecol. 71, 311 (1988); in hyperprolactinemic disorders: C. Ferrari et al., J. Clin. Endocrinol. Metab. 68, 1201 (1989). Clinical trial in Parkinson's disease: J. T. Hutton et al., Neurology 46, 1062 (1996).
Properties: White crystals from diethyl ether, mp 102-104°. Sol in ethyl alcohol, chloroform, DMF; slightly sol in 0.1 N HCl; very slightly sol in n-hexane. Insol in water. LD50 orally in male mice: >400 mg/kg (Brambilla).
Melting point: mp 102-104°
Toxicity data: Sol in ethyl alcohol, chloroform, DMF; slightly sol in 0.1 N HCl; very slightly sol in n-hexane. Insol in water. LD50 orally in male mice: >400 mg/kg (Brambilla)
Derivative Type: Diphosphate
CAS Registry Number: 85329-89-1
Molecular Formula: C26H37N5O2.2H3PO4
Molecular Weight: 647.59
Percent Composition: C 48.22%, H 6.69%, N 10.81%, O 24.71%, P 9.57%
Properties: mp 153-155°.
Melting point: mp 153-155°
Therap-Cat: Prolactin inhibitor; antiparkinsonian.
Therap-Cat-Vet: Prolactin inhibitor.
Keywords: Antiparkinsonian; Dopamine Receptor Agonist; Prolactin Inhibitor. |