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A Miura Y Ukai T Matsuzaki N Taniguchi S Hayashi S Kano Y Kimura K Kimura H Enomoto 《Arzneimittel-Forschung》1986,36(9):1323-1328
The effects of methyl 2,6-dimethyl-4-(2-nitrophenyl)-5-(2-oxo-1,3,2-dioxaphosphorinan-2- yl)-1,4- dihydropyridine 3-carboxylate (DHP-218), a new dihydropyridine calcium antagonist, on vascular smooth muscles, cardiac muscles and [3H]-nitrendipine binding to the cardiac muscle and brain membranes were investigated in vitro. Vascular smooth muscles: Calcium-induced contraction of the rat aorta in high K+ solution was inhibited by DHP-218 with the pA2 value of 9.11. The IC50 value for the inhibitory effects of this compound in high K+-induced and phenylephrine-induced contraction was 6.3 nmol/l and 66 nmol/l, respectively. Vasodilatory effects of this drug on various blood vessels of rabbits contracted by high K+ appeared to a similar extent. The onset of the vasodilatory effect was very slow and the recovery rate of vasodilatory response after washout with the bathing solution containing high K+ or phenylephrine was also very slow. Cardiac muscles: Negative chronotropic and inotropic actions were observed at concentrations more than 30 and 100 nmol/l, respectively. Duration of the plateau phase of normal action potential was shortened and the amplitude and duration of slow action potential were reduced at concentrations more than 1 mumol/l. Very high vasculoselectivity was observed. Displacement of [3H]-nitrendipine binding: The pattern of displacement of [3H]-nitrendipine binding by DHP-218 was very similar to that of other 1,4-dihydropyridines but this compound was about 70 times less potent than nifedipine in [3H]-nitrendipine displacement capacity. These results indicate that DHP-218 has specific vasodilatory action due to calcium antagonism, but association and dissociation rates with tissue and receptors were different from those of nifedipine. 相似文献
3.
Michiko Oka Y. Itoh Shigeru Tatsumi F.-H. Ma Yojiro Ukai Yoshiaki Yoshikuni Kiyoshi Kimura 《Naunyn-Schmiedeberg's archives of pharmacology》1997,356(2):189-196
The effect of (+)-5-oxo-D-prolinepiperidinamide monohydrate (NS-105), a novel cognition enhancer, on adenylate cyclase activity
was investigated in cultured neurons of the mouse cerebral cortex. NS-105 (10–7 and 10–6 M) inhibited forskolin-stimulated cyclic AMP formation, an action that was dependent on pertussis toxin-sensitive G proteins.
Conversely, in pertussis toxin-pretreated neurons, NS-105 (10–7 –10–5 M) significantly enhanced the forskolin-stimulated cyclic AMP formation, and this action was completely reversed by cholera
toxin. A metabotropic glutamate receptor agonist (1S, 3R)-1-aminocyclopentane-1, 3-dicarboxylic acid (1S, 3R-ACPD) produced
similar bi-directional actions on the cyclic AMP formation. Both of these inhibitory and facilitatory actions of NS-105 and
1S, 3R-ACPD were blocked by L(+)-2-amino-3-phosphopropinoic acid (L-AP3). NS-105 (10–6 M) and 1S, 3R-ACPD (10–4 M) significantly enhanced isoproterenol- and adenosine-stimulated cyclic AMP formation. The enhancement of such Gs-coupled
receptor agonists-stimulated cyclic AMP formation was also produced by quisqualate but not by L(+)-2-amino-4-phosphonobutanoate
(L-AP4). The phosphoinositides hydrolysis was enhanced by 1S, 3R-ACPD (10–4 M) but not by NS-105 (10–6 M), however, 1S, 3R-ACPD-induced increase in phosphoinositides turnover was attenuated by NS-105. These findings suggest
that NS-105 stimulates metabotropic glutamate receptor subclasses that are coupled both negatively and positively to adenylate
cyclase, but it acts as an antagonist at the receptor subclasses that are linked to phosphoinositides hydrolysis.
Received: 3 February 1997 / Accepted: 25 April 1997 相似文献
4.
Sleep spindles are an EEG sign of light sleep under physiological conditions. We reported the simultaneous occurrence of sleep spindles and alpha activity in the waking EEG in 12 patients with a mean age of 59.0 years. Most of the patients were diagnosed as cerebrovascular disorders such as cerebral arteriosclerosis, transient ischemic attack and vascular dementia. The mean alpha frequency in the presence of WSA significantly decreased by 1.5 Hz. The frequency and spatial distribution of waking spindle activity were similar to those of sleep spindles. In our cases, at least the two factors of cerebrovascular involvement and older adults were considered to be primarily responsible for the intrusion of sleep spindles into wakefulness (presumably a state close to very light drowsiness) due possibly to the instability of sleep-waking cycle regulation. 相似文献
5.
Shigeru Onodera Koji Saito Takafumi Saito Hitoshi Togashi Sumio Kawata Katsuaki Ukai Haruhide Shinzawa 《Nihon Shokakibyo Gakkai zasshi》2007,104(2):213-218
It is well known that long-term infection with Clonorchis sinensis often causes bile duct cancer, usually. It occurs in the intrahepatic bile duct. We encountered a rare case of clonorchiasis complicated with duodenal papillary cancer. The patient was a woman from China. Although clonorchiasis is rarely found in Japan, the promotion of international exchange may increase the number of visitors from endemic areas. Thus we must pay sufficient attention to this disease. Also, we reported that the microplate ELISA technique was useful in the diagnosis of clonorchiasis with high accuracy in this case. 相似文献
6.
7.
The effect of amlexanox given orally for 3 weeks was studied on the IgE-mediated experimental allergic rhinitis in the actively sensitized guinea pigs. The intranasal instillation of antigen (egg albumin) induced the increase of nasal vascular permeability (dye leakage), histamine content in nasal perfusate and nasal resistance in sensitized guinea pig. Amlexanox, 20 and 60 mg/kg/day given orally for 3 weeks significantly inhibited the increase of dye leakage into the nasal cavity, histamine content and nasal resistance in a dose-dependent manner. These results suggest that amlexanox given orally may be useful therapeutic agent for human allergic rhinitis. 相似文献
8.
The effects of naltrexone on the behavior in mice were investigated by using a multi-dimensional behavioral analyser. Within 15 min following observation, naltrexone preferentially suppressed the linear locomotion at the 10 and 30 mg/kg doses. The results suggest that naltrexone selectively disrupts the linear locomotion without affecting other behaviors in mice. 相似文献
9.
An expression of mRNA coding the calcium-activated Cl- channel-1 (CLCA1) in rabbit gastric parietal cells was examined to verify the possibility that the CLCA1 mediates housekeeping Cl- channels in the basolateral membrane. In whole-cell voltage-clamp experiments of rabbit parietal cells, A23187 (2 microM), a Ca2+ ionophore, activated the basolateral Cl- channels. The partial cDNA fragment of rabbit CLCA1 could be amplified from the total RNA of tracheal epithelium. A Northern blot analysis showed that rabbit CLCA1 mRNA of 3.4 kb is highly expressed in the tracheal epithelium, but not in the gastric parietal cells. Even in a more sensitive detection of rabbit CLCA1 mRNA by RT-PCR, no signal could be observed in the gastric parietal cells. These results suggest that the CLCA1 protein may not be a subunit of the housekeeping Ca2+ -dependent Cl- channel in the basolateral membrane of rabbit gastric parietal cells. 相似文献
10.
Katsuaki Ukai Kazuo Terashima Yutaka Imai Haruhide Shinzawa Yoshimi Okuyama Tsuneo Takahashi Makoto Ishikawa 《Pathology international》1990,40(9):623-634
In an effort to settle the conflicting views on the proliferation kinetics of Kupffer cells (Kc), we performed 2/3 partial hepatectomy on rats injected with Pelikan ink. Using an anti-rat macrophage monoclonal antibody, ED 2, we evaluated the numerical changes in total, carbon-positive ED 2+ cells and carbon-negative ED 2+ cells in the portal and central area. We also analyzed the ultrastructure and peroxidase cytochemistry of various types of cells observed during regeneration. The total numbers of ED 2+ cells in the remaining liver increased rapidly from day 2 to 5, and the number of dividing ED 2+ cells reached a maximum on day 2. Thus, the numerical increase in ED 2+ cells corresponded to the division phase. In contrast, the carbon-labeling experiment showed a continuous increase of carbon negative ED 2+ cells from day 2 to 7. In the central area where division was less frequent, the proportion of carbon-positive cells decreased markedly to 50% on day 7, as against 97% in control rats. These findings suggest the possibility of an influx of carbon-negative Kc in addition to cell division. Ultrastructurally, the presence of carbon-negative "small Kc" and "immature Kc" with morphological features different from those of carbon-positive Kc was demonstrated. Such carbon-negative Kc with a high nucleus-to-cytoplasm ratio and rather few phagosomes, were not observed in control rats. Furthermore, we demonstrated two types of possible precursor cell, i.e. "transitional" forms between monocytes and Kc, and "immature macrophages". The former showed peroxidase activity in some lysosomes as well as in the rough endoplasmic reticulum and nuclear envelope. Our result indicated that the proliferation kinetics of Kc depend upon both local proliferation and influx. 相似文献