13-06268. Monatepil [Archived]
Nomenclature
CAS number: 103377-41-9
N-(6,11-Dihydrodibenzo[b,e]thiepin-11-yl)-4-(4-fluorophenyl)-1-piperazinebutanamide; 11-[4-[4-(4-fluorophenyl)-1-piperazinyl]butyrylamino]-6,11-dihydrodibenzo[b,e]thiepin. C28H30FN3OS; mol wt 475.62.
C 70.71%, H 6.36%, F 3.99%, N 8.83%, O 3.36%, S 6.74%.
Description and references
Tricyclic calcium channel blocker with α1-adrenoceptor antagonist activity. Prepn: H. Uno et al., WO 8601203; eidem, US 4749703 (1986, 1988 both to Dainippon); M. Kurokawa et al., J. Med. Chem. 34, 927 (1991). HPLC determn in plasma: M. Kurono et al., J. Chromatogr. 532, 175 (1990). Review of pharmacology: H. Takeuchi et al., Cardiovasc. Drug Rev. 12, 254-269 (1994). Series of articles on pharmacology and clinical effect in hypertension and hyperlipidemia: Am. J. Hypertens. 7 (No. 10, pt. 2), 131S-166S (1994).
Properties
Crystals from chloroform + n-hexane, mp 194-194.5°.Derivative
Maleate.Nomenclature
CAS number: 103379-03-9
AD-2615; AJ-2615. C28H30FN3OS.C4H4O4; mol wt 591.69.
C 64.96%, H 5.79%, F 3.21%, N 7.10%, O 13.52%, S 5.42%.
Properties
Colorless crystals from ethanol, mp 149-150°. Sol in acetic acid, dimethylformaldehyde, methanol; sparingly sol in ethanol, chloroform, acetic anhydride, acetone. Practically insol in water, ether. LD50 in mice (g/kg): >1 i.p.; >4 orally (Uno).Therapeutic Category
Antihypertensive.
Keywords
α-Adrenergic Blocker; Antihypertensive; Calcium Channel Blocker
Status
This monograph has been retired and is no longer subject to revision or update.