查询词典 agonist

Meperidine is one of the most commonly used opioid for the relief of acute pain. However, this full opioid-agonist may also cause several adverse effects related to its pharmacological actions, including the less-recognized serotonin syndrome.

Meperidine是一个最普遍使用的吗啡类急性疼痛止痛剂，但是，此吗啡受体促动剂也可能导致若干药理学的不良反应，包括不易辨识的血清素症候群。

Results The pD2 value (the affinity to M-receptors of agonist) of Erycibele alkaloid's miosis is 3.60±0.15 and its IOP lowering action is 3.49±0.07. In the isolated iris contracting experiment, its pD2 value is 6.38±0.12. M3 receptor antagonist is the strongest antagonist in inhibiting the miosis, IOP lowering action and isolated iris pupillary contracting action of Erycibele alkaloid. 0.01% Erycibele alkaloid can cause the decrease of cAMP and the increase of cGMP in the aqueous humor.

结果 测定丁公藤碱缩瞳作用的pD2值为3.60±0.15，降眼压作用的pD2值为3.49±0.07，离体虹膜收缩作用的pD2值为6.38±0.12.M1～M3受体拮抗剂均可拮抗丁公藤碱的缩瞳作用、降眼压作用及离体虹膜收缩作用，其中以M3受体拮抗剂的拮抗作用最强。0.01％丁公藤碱可使房水环磷酸腺苷(cyclic adenosine monophosphate，cAMP)含量降低，环磷酸鸟苷(cyclic guanosine 3，5-monophosphate；cGMP)含量升高。

The effect of muscarinic receptors agonist-carbachol on conjunctival fibroblasts'proliferation was studied by Cell Proliferation ELISA.

Brdu酶联免疫吸附试验检测毒蕈碱受体激动剂carbachol对结膜成纤维细胞增殖的影响。

Beta 2 adrenergic agonist drugs as a class are widely used in obstetrics as tocolytics to inhibit or slow down labor and bronchodilators, but may act as functional and behavioral teratogens when given continuously in the mid to late second or early third trimesters.

2肾上腺素受体激动剂，这类药物被产科广泛用于抑制早产和支气管扩张，但如果在怀孕第二期的中段到晚段，以及第三期的早段给予的话，会对胎儿生理造成缺陷。

In our studies, the behavioral sensitization animal models, including rats and mice, induced by morphine, methamphetamine or cocaine were established to investigate the effects of L-type calcium channel antagonists, mood stablers (lithium salts, valproate, and carbamazepine), and a novel mu-receptor partial agonist the morphine on development, transfer, and expression of behavioral sensitization.

本课题建立吗啡，甲基苯丙胺以及可卡因诱导的大、小鼠行为敏化模型。探讨了L-型钙通道阻滞剂，情绪稳定剂（锂盐，丙戊酸钠和卡马西平），以及新型μ受体部分激动剂噻吩诺啡对行为敏化形成，转化以及表达的影响。

The effects and mechanism of GABAergic neurons, NOergic neurons, opioid peptide and cyclic adenosine monophosphate in the nucleus reticularis thalami on sleep-wakefulness cycle of rats and the effects and mechanism of the 5-HTergic nerve fibers project from the nucleus raphes dorsalis to RT on sleep-wakefulness cycle of rats were investigated with the methods of brain stereotaxic, nucleus spile, microinjection and polysomngraphy.1. The effects of GABAergic neurons in RT on sleep-wakefulness cycle of rats1.1 Microinjection of 3-mercaptopropionic acid (3-MP, a kind of glutamate decarboxylase inhibitor) into RT. On the day of microinjection, sleep only decreased a litter. On the second day, sleep marked decreased and wakefulness marked increased. On the third and fourth day, sleep and wakefulness stages resumed to normal.1.2 Microinjection of gamma-amino butyric acid (GABA 1.0μg) into RT enhanced sleep and reduced wakefulness compared with control; while microinjection of L-glutamate (L-Glu, 0.2μg) decreased sleep and increased wakefulness; microinjection of bicuculline (BIC, 1.0μg), a GABAA receptor antagonist, enhanced wakefulness and reduced sleep; microinjection of baclofen (BAC, 1.0μg), GABAB receptor agonist, had the same effects as GABA.2. The effects of NOergic neurons in RT on sleep-wakefulness cycle of rats2.1 Microinjection of L-arginine (L-Arg, 0.5μg) into RT decreased sleep compared with control, but there were on statistaical difference between L-Arg group and control; while microinjection of sodium nitroprusside (SNP, 0.2μg), a NO donor into RT, sleep marked decreased and wakefulness marked increased. Microinjection of nitric oxide synthase inhibitor, N-nitro-L-arginine (L-NNA, 2.0μg) into RT enhanced sleep and reduced wakefulness.2.2 After simultaneous microinjection of L-NNA (2.0μg) and SNP (0.2μg) into RT, SNP abolished the sleep-promoting effect of L-NNA compared with L-NNA group; after simultaneous microinjection of L-NNA (2.0μg) and L-Arg(0.5μg) into RT, we found that L-NNA could not blocked the wakefulness-promoting effect of L-Arg.3. The effects of opioid peptide in RT on sleep-wakefulness cycle of rats3.1 Microinjection of morphine sulfate (MOR, 1.0μg) into RT increased wakefulness and decreased sleep compared with control; while microinjection of naloxone hydrochloride (NAL, 1.0μg), the antagonist of opiate receptors, into RT, enhanced sleep and reduced wakefulness.3.2 After simultaneous microinjection of MOR (1.0μg) and NAL (1.0μg) into RT, the wakefulness-promoting effect of MOR and the sleep-promoting effect of NAL were not observed compared with control.4. The effects of cAMP in RT on sleep-wakefulness cycle of rats Microinjection of cAMP (1.0μg) into RT increased sleep and decreased wakefulness compared with control; microinjection of methylene blue (MB,1.0μg) into RT enhanced sleep and reduced wakefulness compared with control.5. The effects of the 5-HTergic nerve fibers project from DRN to RT on sleep-wakefulness cycle of rats5.1 When L-Glu (0.2μg) was microinjected into DRN and normal sodium (NS,1.0μg) was microinjected into bilateral RT. We found that sleep was decreased and wakefulness was increased compared with control; when L-Glu (0.2μg) was microinjected into DRN and methysergide (MS,1.0μg), a non-selective 5-HT antagonist, was microinjected into bilateral RT, We found that sleep was enhanced and wakefulness was reduced compared with L-Glu group.5.2 When p-chlorophenylalanine (PCPA, 10μg) was microinjected into DRN and NS (1.0μg) was microinjected into bilateral RT, We found that sleep was increased and wakefulness was decreased compared with control; microinjection of 5-hydroxytryptaphan (5-HTP, 1.0μg), which can convert to 5-HT by the enzyme tryptophane hydroxylase and enhance 5-HT into bilateral RT, could block the effect of microinjection of PCPA into DRN on sleep-wakefulness cycle.

本研究采用脑立体定位、核团插管、微量注射、多导睡眠描记等方法，研究丘脑网状核(nucleus reticularis thalami，RT)中γ-氨基丁酸(gamma-amino butyric acid ，GABA)能神经元、一氧化氮(nitrogen monoxidum，NO)能神经元、阿片肽类神经递质、环一磷酸腺苷(cyclic adenosine monophosphate，cAMP)及中缝背核(nucleus raphes dorsalis，DRN)至RT的5-羟色胺(5-hydroxytryptamine，5-HT)能神经纤维投射对大鼠睡眠-觉醒周期的影响及其作用机制。1 RT内GABA能神经元对大鼠睡眠-觉醒周期的影响1.1大鼠RT内微量注射GABA合成关键酶抑制剂3-巯基丙酸(3-MP，5μg)，注射当天睡眠时间略有减少，第二日睡眠时间显著减少，觉醒时间明显增多，第三、四日睡眠和觉醒时间逐渐恢复至正常。1.2大鼠RT内微量注射GABA受体激动剂GABA( 1.0μg)后，与生理盐水组比较，睡眠时间增加，觉醒时间减少；而RT内微量注射L-谷氨酸(glutamic acid， L-Glu， 0.2μg)后，睡眠时间减少，觉醒时间增加；RT内微量注射GABAA受体阻断剂荷包牡丹碱(bicuculline，BIC，1.0μg)后，睡眠时间减少，觉醒时间增加；RT内微量注射GABAB受体激动剂氯苯氨丁酸(baclofen，BAC，1.0μg)后，产生了与GABA相似的促睡眠效果。2 RT内NO能神经元对大鼠睡眠-觉醒周期的影响2.1大鼠RT内微量注射NO的前体L-精氨酸(L-Arg，0.5μg)后，与生理盐水组对比，睡眠时间略有减少，但无显著性意义；而RT内微量注射NO的供体硝普钠(Sodium Nitroprusside，SNP，0.2μg)后可明显增加觉醒时间，缩短睡眠时间；微量注射一氧化氮合酶抑制剂L-硝基精氨酸(L-arginine，L-NNA，2.0μg)后，引起睡眠时间增多，觉醒时间减少。2.2大鼠RT内同时微量注射L-NNA(2.0μg)和SNP(0.2μg)后与L-NNA组比较发现SNP逆转了L-NNA的促睡眠作用；RT内同时微量注射L-NNA(2.0μg)和L-Arg(0.5μg)后，与L-NNA(2.0μg)组比较发现L-Arg可以增加觉醒而缩短睡眠，其促觉醒作用未能被NOS的抑制剂L-NNA所逆转。3 RT内阿片肽对大鼠睡眠-觉醒周期的影响3.1大鼠RT内微量注射硫酸吗啡(morphine sulfate，MOR，1.0μg)后与生理盐水组对比，睡眠时间减少而觉醒时间增加； RT内微量注射阿片肽受体拮抗剂盐酸纳洛酮(naloxone hydrochloride，NAL，1.0μg)后与生理盐水组比较，睡眠时间增加而觉醒时间减少。3.2大鼠RT内同时微量注射MOR(1.0μg)和NAL(1.0μg)后，与生理盐水组对比，原有的MOR促觉醒效果和NAL的促睡眠效果都没有表现。4 RT内环一磷酸腺苷信使对大鼠睡眠-觉醒周期的影响大鼠RT内微量注射cAMP(1.0μg)后与NS(1.0μg)组比较，睡眠时间增多而觉醒时间减少；RT内微量注射亚甲蓝(methylene blue，MB，1.0μg)后，与NS组比较，睡眠时间增多而觉醒时间减少。5中缝背核投射到丘脑网状核的5-羟色胺能神经纤维对大鼠睡眠-觉醒周期的影响5.1大鼠DRN内微量注射L-Glu(0.2μg)，同时在双侧RT内微量注射NS (1.0μg)后，与对照组(DRN和双侧RT注射NS， 0.2μg)比较，睡眠时间减少，觉醒时间增多；大鼠DRN内微量注射L-Glu(0.2μg)，同时在双侧RT内微量注射二甲基麦角新碱(methysergide， MS， 1.0μg )后，与对照组(DRN注射L-Glu 0.2μg，双侧RT注射NS 1.0μg)比较，睡眠时间增多，觉醒时间减少。5.2大鼠DRN内微量注射对氯苯丙氨酸(p-chlorophenylalanine，PCPA，10μg)，同时在双侧RT内微量注射NS (1.0μg)后，与对照组(DRN和双侧RT注射NS， 1.0μg)比较，睡眠时间增多，觉醒时间减少；大鼠DRN内微量注射PCPA(10μg)，产生睡眠增多效应后，在双侧RT内微量注射5-羟色胺酸(5-hydroxytryptaphan ， 5-HTP， 1.0μg )后，与对照组(DRN注射PCPA 10μg，双侧RT注射NS 1.0μg)比较，睡眠时间减少，觉醒时间增多。

AIM To investigate the effects of low-dose pethidine, a μ-opioid receptor agonist on cigarette smoke-induced acute airway smooth muscle constriction and inflammatory reaction in guinea pigs.

目的 研究小剂量阿片受体激动剂哌替啶对香烟烟雾吸入引起的豚鼠急性气道收缩反应和炎性反应的影响。

Caffeine (the agonist of RyR1) and ruthenium red (the antagonist of RyR1) had no effect on the E value either.

激动剂咖啡因，抑制剂钌红也不改变RyR1的E值。

The concentration-response curve of GABA was shifted downward by hypotonic without any change of the threshold value.The values of two curves were very close(33.02μM and 29.41μM). Hypotonic decreased the maximal amplitude of IGABA by(31.38±2.13)%.③This inhibitory effect was reversed by ruthenium red, a nonselective TRPV4 receptor antagonist, and was increased by 4ɑ-PDD, a selectively TRPV4 receptor agonist.

低渗透压+GABA的量效曲线较单独的IGABA量效曲线明显下移，而两者的阈值和最大反应浓度基本不变，分别为10μM和1000μM；两条曲线的EC50值非常接近，分别为29.41μM和33.02μM；预加低渗透压后最大反应浓度时，IGABA的幅值减少了(31.38±2.13)%。

This inhibitory effect was increased by 4ɑ-PDD, a selective TRPV4 receptor agonist, and was reversed by ruthenium red, a nonselective TRPV4 receptor antagonist, suggesting that the inhibition is mediated via TRPV4 receptor.

4低渗透压对IATP的抑制作用可被TRPV4(transient receptor potential vanilloid 4)受体激动剂4ɑ-PDD(4ɑ-phorbol 12，13-didecanoate)增强，并可被TRPV4受体非特异性阻断剂钌红(ruthemium red， RR)阻断。

In the United States, chronic alcoholism and hepatitis C are the most common ones.

在美国，慢性酒精中毒，肝炎是最常见的。

If you have any questions, you can contact me anytime.

如果有任何问题，你可以随时联系我。