Zomepirac sodium inhibited the reflex hypertension caused by an injection of bradykinin into the splenic artery of anaesthetized dogs, but not that by injection of bradykinin plus PGE1. In the rat acetic acid writhing test, the potency ratio of intraperitoneal (ED50 = 0.41 microgram/kg) to intravenous (ED50 = 33.5 micrograms/kg) anti-writhing activity of zomepirac sodium was 79.2 (37.1-173), th...

We have studied the in vitro biological activities and mechanisms of action of 1,25-dihydroxyvitamin D3 (1,25D3) and nine potent 1,25D3 analogs on proliferation and differentiation of myeloid leukemia cell lines (HL-60, retinoic acid-resistant HL-60 [RA-res HL-60], NB4 and Kasumi-1). The common novel structural motiff for almost all the analogs included removal of C-19 (19-nor); each also had u...

In this study, A2780 human ovarian carcinoma cells were grown in folinic acid in contrast to folic acid, and the molecular and biochemical properties of cisplatin-resistant A2780 cells were analyzed for changes in the dTMP synthase cycle. At concentrations of folinic acid that were optimal for cell growth (10(-8) M), the ED50 for cisplatin was 2.5 and 43 microM in the A2780S and A2780DDP cells,...

Apomorphine, at doses greater than or equal to 10 mg/kg (intraperitoneally), produced two patterns of stereotypy. In rats from one supplier it induced predominantly gnawing while in those from another predominantly climbing, suggesting that the response to the drug is influenced by genetic and/or experimental factors. At lower doses, apomorphine induced climbing in both groups (ED50 = 1.4 mg/kg...

The effects of NPY(13-36) on cardiorespiratory responses elicited by microinjections of L-glutamate into the nucleus tractus solitarius (NTS) have been studied in anaesthetized (alpha-chloralose + urethane) Sprague-Dawley rats. NPY(13-36) in doses ranging from 50 to 500 fmol produces a significant increase in mean arterial pressure (MAP) without significant effects on heart rate (HR) and respir...

Ganaxolone (3alpha-hydroxy-3beta-methyl-5alpha-pregnan-20-one), a synthetic analog of the endogenous neurosteroid allopregnanolone and a positive allosteric modulator of GABAA receptors, may represent a new treatment approach for epilepsy. Here we demonstrate that pretreatment with ganaxolone (1.25-20 mg/kg, s.c.) causes a dose-dependent suppression of behavioral and electrographic seizures in ...

considerable interest has been focused on the triazole structure, which has been known to possess a broad spectrum of biological activities such as antitumor, anti-inflammatory, antimicrobial, antiviral, and anticonvulsant activities. before this, several heterocyclic compounds containing triazole were synthesized that had shown considerable anticonvulsant activity. as part of our continuous re...

Depression affects more than 300 million people worldwide, represents one of the leading causes of disability worldwide. Treatment is based on the use of tricyclic antidepressant, selective serotonin reuptake inhibitors, between others; that although are clinically effective has a delayed onset activity and produce important side effects. Medicinal plants are presented as a source of study in t...

Depression affects more than 300 million people worldwide, represents one of the leading causes of disability worldwide. Treatment is based on the use of tricyclic antidepressant, selective serotonin reuptake inhibitors, between others; that although are clinically effective has a delayed onset activity and produce important side effects. Medicinal plants are presented as a source of study in t...