Reference

Antidepressant biochemical profile of the novel bicyclic compound Wy-45,030, an ethylcyclohexanol derivative

Antidepressant biochemical profile of the novel bicyclic compound Wy-45,030, an ethylcyclohexanol derivative. Muth, Eric A.; Haskins, John T.; Moyer, John A.; Husbands, George E. M.; Nielsen, Susan T.; Sigg, Ernest B. (Dep. Exp. Ther., Wyeth Lab., Inc., Philadelphia, PA 19101, USA). Biochem. Pharmacol., 35(24), 4493-7 (English) 1986. CODEN: BCPCA6. ISSN: 0006-2952. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The novel bicyclic compd. Wy-45030 [1-2-(dimethylamino)-1-(4-methoxyphenyl)ethylcyclohexanol hydrochloride] (I) [99300-78-4] exhibited a neurochem. profile predictive of antidepressant activity. Like the tricyclic antidepressants, it inhibited rat brain imipramine receptor binding and synaptosomal monoamine uptake (dopamine as well as norepinephrine and serotonin). It did not inhibit monoamine oxidase. Unlike the tricyclic antidepressants, it was not antimuscarinic in the guinea pig ileum, nor did it have any appreciable affinity for brain a-1 adrenergic or histamine-1 binding sites. Wy-45030 was also without affinity for a-2 or b adrenergic, benzodiazepine, serotonin-1, serotonin-2, dopamine-2, and opiate receptors. Such a profile is predictive of antidepressant activity devoid of the side effects common to tricyclic therapy.

Determination of venlafaxine in human plasma by HPLC and its pharmacokinetics

All Rights Reserved. Determination of venlafaxine in human plasma by HPLC and its pharmacokinetics. Shi, Haoqiang; Zhuang, Qingqi; Cai, Weimin (Medical College, Shanghai Jiaotong University, Shanghai 200025, Peop. Rep. China). Zhongguo Yiyao Gongye Zazhi, 36(11), 694-696 (Chinese) 2005 Zhongguo Yiyao Gongye Zazhi Bianjibu. 99300-78-4 and 93413-69-5 are also occured in this study. CODEN: ZYGZEA. ISSN: 1001-8255. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) An HPLC method with fluorescence detection for detn. of venlafaxine in human plasma was established. After extd. by liq.-liq. extn., a C8 column was used with the mobile phase of acetonitrile-phosphate buffer soln. (, pH 5.5) at the flow rate of 1.5 mL/min. The excitation and emission wavelengths were 276 and 598 nm, resp. The calibration curve was linear in the concn. range of 5-2,000 ng/mL. The extn. recovery was 96.9%-104.3%. The RSDs of intra- and inter-day were less than 8%. A single dose of 150 mg venlafaxine hydrochloride sustained-release capsules was given to ten volunteers. The pharmacokinetics parameters Cmax, Tmax, AUC0?￥ and t1/2 were (168±12.3) ng/mL, (6.1±1.8) h, (4,510±1,462) ng×h×mL-1, and (5.7±0.7) h, resp. .