ABSTRACT
Dopamine constitutes about 80 percent of the content of central catecholamines and has a crucial role in the etiology of several neuropsychiatric disorders, including Parkinson's disease, depression and schizophrenia. Several dopaminergic drugs are used to treat these pathologies, but many problems are attributed to these therapies. Within this context, the search for new more efficient dopaminergic agents with less adverse effects represents a vast research field. The aim of the present study was to report the structural design of two N-phenylpiperazine derivatives, compound 4: 1-[1-(4-chlorophenyl)-1H-4-pyrazolylmethyl]-4-phenylhexahydropyrazine and compound 5: 1-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4-ylmethyl]-4-phenylhexahydropyrazine, planned to be dopamine ligands, and their dopaminergic action profile. The two compounds were assayed (dose range of 15-40 mg/kg) in three experimental models: 1) blockade of amphetamine (30 mg/kg, ip)-induced stereotypy in rats; 2) the catalepsy test in mice, and 3) apomorphine (1 mg/kg, ip)-induced hypothermia in mice. Both derivatives induced cataleptic behavior (40 mg/kg, ip) and a hypothermic response (30 mg/kg, ip) which was not prevented by haloperidol (0.5 mg/kg, ip). Compound 5 (30 mg/kg, ip) also presented a synergistic hypothermic effect with apomorphine (1 mg/kg, ip). Only compound 4 (30 mg/kg, ip) significantly blocked the amphetamine-induced stereotypy in rats. The N-phenylpiperazine derivatives 4 and 5 seem to have a peculiar profile of action on dopaminergic functions. On the basis of the results of catalepsy and amphetamine-induced stereotypy, the compounds demonstrated an inhibitory effect on dopaminergic behaviors. However, their hypothermic effect is compatible with the stimulation of dopaminergic function which seems not to be mediated by D2/D3 receptors
Subject(s)
Animals , Male , Mice , Rats , Dopamine Antagonists , Psychotropic Drugs , Catalepsy , Dopamine Antagonists , Hypothermia , Psychotropic Drugs , Rats, Wistar , Stereotyped Behavior , Structure-Activity RelationshipABSTRACT
The aim of the present study was to assess the analgesic activity of the aerial parts of two Hypericum species native to Southern Brazil, H. caprifoliatum and H. polyanthemum. The antinociceptive effect of the H. polyanthemum cyclohexane extract (POL; 180 mg/kg) and of the H. caprifoliatum methanol (MET) and cyclohexane (CH) extracts (90 mg/kg) was evaluated in the hot-plate (ip and po) and writhing (po) tests using male Swiss CF1 mice weighing 22-27 g (N = 10 per group). All extracts displayed antinociceptive effects in the hot-plate test (MET ip = 48 percent, MET po = 39 percent, CH ip = 27 percent, CH po = 50 percent, POL ip = 74 percent, and POL po = 49 percent compared to control). Pretreatment with naloxone (2.5 mg/kg, sc) abolished the effects of CH and POL, and partially prevented the analgesia induced by MET administered by the ip (but not by the po) route. POL and CH (po) significantly reduced the number of writhes induced by acetic acid, while MET was ineffective in this regard. We conclude that the antinociceptive effects of the H. caprifoliatum (CH) and H. polyanthemum (POL) hexane extracts seem to be mediated by the opioid system. Moreover, the antinociceptive activity of the H. caprifoliatum MET extract seems to depend on at least two chemical substances (or groups of substances) with distinct pharmacokinetic profiles and mechanisms of action. Only the naloxone-insensitive component of MET activity showed good bioavailability following oral administration
Subject(s)
Animals , Male , Mice , Analgesics , Hypericum , Pain Threshold , Plant Extracts , Plants, Medicinal , Time FactorsABSTRACT
Os relatos encontrados na literatura científica sobre a composição química e atividades farmacológicas do gênero Pfaffia spp. são apresentados. Os estudos sobre esse gênero são ainda bastante escassos, sendo assim, o uso racional de espécies de Pfaffia, com finalidade terapêutica ainda depende de conhecimento aprofundado de suas propriedades farmacológicas e do desenvolvimento de tecnologias de produção e controle de qualidade.
This review summarizes available chemical and pharmacological data about Pfaffia genre. Scientific studies about these species are still lacking, and their therapeutical rational use depends on the availability of more informations about their pharmacological properties and the development of production and control quality technologies.
ABSTRACT
Neste trabalho é apresentada uma experiência no ensino de Farmacognosia, cuja base principal é o estudo dos aspectos farmacoterapêuticos de fitofármacos e fitoterápicos, visando o estabelecimento de seu uso racional. São apresentados dados sobre a comercialização e ações institucionais destinadas à normatização, padronização e utilização racional destes produtos no mundo, com propostas e condutas na prática farmacêutica para aquisição e dispensação adequada de fitoterápicos.
In this paper we present a pharmacognosy teaching experience which focuses mainly on the pharmacotherapeutic aspects of phytomedicines and drugs from natural sources aiming their rational use. World commercial data and institutional actions destined to provide normalization, standardization and rational use as well some propositions for the acquisition of these products and patient counseling are presented.