Detail of "58-28-6"

Reference

On the selective inhibition of serotonin uptake in vivo by ORG 6582

On the selective inhibition of serotonin uptake in vivo by ORG 6582. Sugrue, Michael F.; Goodlet, Ian; Mireylees, Stewardt E. (Dep. Pharmacol., Organon Lab. Ltd., Newhouse/Lanarkshire, Scot.). Eur. J. Pharmacol., 40(1), 121-30 (English) 1976. CODEN: EJPHAZ. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) In vivo blockade of serotonin (5-HT) [50-67-9] uptake was studied by investigating the effect of drug pretreatment on the ability of p-chloroamphetamine to lower rat brain 5-HT levels. Org 6582 (I) [59905-71-4] was .apprx.2-fold more potent than fluoxetine-HCl [56296-78-7], 5-fold more potent than chlorimipramine-HCl [17321-77-6],and 14-fold more potent than desipramine-HCl [58-28-6] in blocking the ability of p-chloroamphetamine to lower rat brain 5-HT content. I also had a longer duration of action than either fluoxetine or chlorimipramine. Although I did not effect amine steady state levels, it did decrease rat brain 5-HT turnover and lower rat brain levels of 5-hydroxyindoleacetic acid [54-16-0]. In contrast to both desipramine and chlorimipramine, I was devoid of effect on the ability of 1-metaraminol and 6-hydroxydopamine to lower rat heart noradrenaline (NA) levels. The ability of intraventricularly administered 6-hydroxydopamine to lower rat brain NA levels was unaltered by I pretreatment. The corresponding i.p. ED50 values for desipramine and chlorimipramine were 7.3 and 28.8 mg/kg, resp. Like desipramine and chlorimipramine, I had no effect on the ability of intraventricular 6-hydroxydopamine to lower rat brain I content. I had no effect on steady state levels or on the turnover of NA and dopamine in the rat brain. Apparently, I is a potent long acting selective inhibitor of 5-HT uptake in vivo.

Ultrastructural effects of parachlorophenylalanine, 5-hydroxytryptamine and the imipramine group on the nerve processes of the small intestine

Ultrastructural effects of parachlorophenylalanine, 5-hydroxytryptamine and the imipramine group on the nerve processes of the small intestine. Feher, Erzsebet; Csanyi, Karoly (1st Dep. Anat., Semmelweis Univ. Med. Sch., Budapest, Hung.). Acta Anat., 100(1), 61-7 (English) 1978. CODEN: ACATA5. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Section cross-reference(s): 13 Intraluminal treatment of isolated cat ileum with desipramine-HCl [58-28-6] (30 mg/kg/day), imipramine [50-49-7] (30mg/kg/day), or 4-chloro-DL-phenylalanine [7424-00-2] (100 mg/kg/day) selectively decreased granulated vesicles in small intestinal nerve fibers. However, 5-hydroxytryptamine creatinine sulfate [971-74-4] complex with water (500 mg/kg/day) increased the granular vesicles; yellow fluorescent neurons and processes were obsd. in the myenteric and submucous plexuses. Thus, the serotonergic nature of certain nerve fibers was demonstrated.