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1.
Richard B. Rothman Uwe K. Schumacher Candace B. Pert 《Journal of neurochemistry》1984,43(4):1197-1199
Abstract: (β-FNA, the β -fumaramate methyl ester of naltrexone, has been shown to antagonize irreversibly the actions of morphine on the guinea pig ileum and mouse vas deferens bioassays but does not affect the actions of δ-receptor ligands on the mouse vas deferens bioassay, suggesting that the compound does not irreversibly bind to the S receptor. In this paper we examine the effect of (β -FNA on the binding of the prototypic δ agonists, Leuenkephalin and d -Ala2 - d -Leu5 -enkephalin, its metabolically stable analogue, and show that treatment of membranes with β -FNA does lead to alterations in the in vitro properties of δ receptors. 相似文献
2.
Terry W. Moody Duncan P. Taylor Candace B. Pert 《Journal of cellular biochemistry》1981,15(2):153-159
The effect of nucleotides on central nervous system neuropeptide receptor binding was investigated. The guanine nucleotides, guanosine-5′-triphosphate and guanylyl-5′-imidodiphosphate, significantly inhibited the binding of radiolabeled vasoactive intestinal polypeptide but not that of [Tyr4]bombesin to rat brain membranes. Vasoactive intestinal polypeptide binding was inhibited by guanine nucleotides in a dose-dependent manner. Using a 20 μM dose, 60% of the specific vasoactive intestinal polypeptide binding was inhibited by guanylyl-5′-imidodiphosphate, which was more potent than guanosine-5′-triphosphate, whereas other nucleotides were not effective. This reduction in binding was a consequence of lower affinity of the receptor for vasoactive intestinal polypeptide, which in turn resulted from an increased rate of dissociation. 相似文献
3.
Single unit recording and micropressure ejection techniques were used to investigate the actions of opiates on dopaminergic and non-dopaminergic neurons in the rat substantia nigra. Systemic administration of morphine, 1 to 4 mg/kg, led to a naloxone-reversible increase in firing rate of all zona compacta dopaminergic (ZC) neurons examined (n=10). In a specifically defined subpopulation of non-dopaminergic nigral zona reticulata (ZR) neurons, systemically administered morphine led to a naloxone reversible decrease in activity (n=9). D-Ala2-d-leu5 (DADL)-enkephalin, when applied directly onto ZC neurons by micropressure ejection techniques, had no effect on their firing rate. In contrast, micropressure ejection of DADL enkephalin onto ZR neurons produced a decrease in firing rate which was blocked by systemically administered naloxone. Morphine sulfate applied by pressure ejection onto both ZC and ZR neurons produced mixed results which were not always blocked by naloxone. These results suggest that one of the mechanisms by which opiates increase dopaminergic neurotransmission is through disinhibition of dopaminergic neurons in the substantia nigra. 相似文献
4.
Visualization and solubilization of rat brain opiate receptors with a “κ” ligand selectivity pattern 总被引:2,自引:0,他引:2
Remi Quirion Wayne D. Bowen Miles Herkenham Candace B. Pert 《Cellular and molecular neurobiology》1982,2(4):333-346
1. Specific binding of [3H]ethylketocyclazocine (EkappaC), a prototype kappa-opiate agonist, to slide-mounted rat striatal sections is increased in the presence of 100 mM NaCl at 4 degrees C. 2. Under similar incubation conditions, binding of mu and delta prototype opiates is reduced to almost undetectable levels. 3. Correlation (P less than 0.01) of the ligand selectivity pattern of [3H]EKC displacement with the potencies of various opiate drugs in inhibiting the contractions of the rabbit vas deferens, a kappa-opiate receptor bioassay, suggests that the binding site under study represents the pharmacologically relevant kappa-opiate receptor. 4. Visualization of these kappa-opiate receptors with tritium-sensitive film reveals a striking, highly discrete brain distribution pattern (e.g., striatal patches, habenular stripe) which is similar to that of [3H]dihydromorphine and [3H]naloxone. 5. Soluble [3H]EKC binding sites obtained from rat membranes also possess a kappa-like ligand selectivity pattern, with bremazocine being a potent displacer while mu and delta ligands are almost inactive. 6. A possible explanation of these data is that the "kappa"-opiate binding site in rat brain is one transitional state of an opiate receptor capable of assuming distinct conformations with characteristic ligand selectivity patterns. Other possibilities such as pre and post-synaptic locations should also be considered. 相似文献
5.
Comparisons were made between the efficacy of naloxone to reverse analgesia induced by electrical stimulation (SPA) of the periaqueductal gray matter and analgesia induced by microinjections of morphine into the same brain region. Naloxone at 1 or 10 mg/kg was ineffective in antagonizing SPA during the first two minutes post-stimulation. Although some antagonism did appear 3–5 minutes after stimulation, the effect was neither consistent nor dose-dependent. Morphine, on the other hand, was antagonized in a dose-dependent and complete fashion by naloxone. The assumption that similar mechanisms underlie both opiate and electrical stimulation induced analgesia is discussed. 相似文献
6.
7.
Anna CC Aguiar Ananda C Cunha Isabela Penna Ceravolo Regina A Correia Gon?alves Arildo JB Oliveira Antoniana Ursine Krettli 《Memórias do Instituto Oswaldo Cruz》2015,110(7):906-913
Several species of Aspidosperma plants are used to treat diseases in
the tropics, including Aspidosperma ramiflorum, which acts against
leishmaniasis, an activity that is experimentally confirmed. The species, known as
guatambu-yellow, yellow peroba,
coffee-peroba andmatiambu, grows in the Atlantic
Forest of Brazil in the South to the Southeast regions. Through a guided
biofractionation of A. ramiflorum extracts, the plant activity
against Plasmodium falciparum was evaluated in vitro for toxicity
towards human hepatoma G2 cells, normal monkey kidney cells and nonimmortalised human
monocytes isolated from peripheral blood. Six of the seven extracts tested were
active at low doses (half-maximal drug inhibitory concentration < 3.8 µg/mL); the
aqueous extract was inactive. Overall, the plant extracts and the purified compounds
displayed low toxicity in vitro. A nonsoluble extract fraction and one purified
alkaloid isositsirikine (compound 5) displayed high selectivity indexes (SI) (= 56
and 113, respectively), whereas compounds 2 and 3 were toxic (SI < 10). The
structure, activity and low toxicity of isositsirikine in vitro are described here
for the first time in A. ramiflorum, but only the neutral and
precipitate plant fractions were tested for activity, which caused up to 53%
parasitaemia inhibition of Plasmodium berghei in mice with
blood-induced malaria. This plant species is likely to be useful in the further
development of an antimalarial drug, but its pharmacological evaluation is still
required. 相似文献
8.
Unilateral amygdala electrodes were implanted in male Sprague-Dawley rats stimulated once daily with a 200 μamp pulse of 500 millisecond duration to produce kindling. Forty-six percent (12 of 26) of the animals that eventually developed after-discharges demonstrated rhythmic oscillations in after-discharge duration. The presence or absence of generalized bilateral clonic seizures also showed rhythmic oscillations in close association with after-discharge duration. It is suggested that during kindling some animals, independent of electrode placement, develop rhythmic oscillations in excitability of the amygdala. This model may represent a means of experimentally eliciting or uncovering neuronal substrates which show regular alterations in excitability and may be relevant to the oscillations in mood and behavior observed in the affective disorders. 相似文献
9.
10.
Danilo E Xavier Renata C Picão Raquel Girardello Lorena CC Fehlberg Ana C Gales 《BMC microbiology》2010,10(1):217