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搜索结果：“glucagon receptor”

“glucagon receptor”的搜索结果

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Tamoxifen Citrate

Catalog No. A10885
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Estrogen receptor 拮抗剂

Tamoxifen Citrate是哺乳动物甾醇异构酶的选择性和有效抑制剂。了解更多

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- Renu Sudhakar, .et al. Bazedoxifene, a Postmenopausal Drug, Acts as an Antimalarial and Inhibits Hemozoin Formation, Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Apalutamide (ARN-509)

Catalog No. A11923
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Androgen Receptor 抑制剂

Apalutamide (ARN-509)是一种具有潜在抗肿瘤活性的雄激素受体拮抗剂，IC50 为 16 nM。ARN-509与靶组织中的AR结合，从而阻止了雄激素诱导的受体激活，并促进了无法转运至细胞核的无活性复合物的形成。这防止了AR应答基因的结合和转录。了解更多

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- Frédérique Mittler, .et al. High-Content Monitoring of Drug Effects in a 3D Spheroid Model, Front Oncol, 2017, 7: 293 PMID: 29322028
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Naratriptan

Catalog No. A10624
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5-HT1 receptor

Naratriptan是一种选择性的5-HT1受体亚型激动剂。了解更多

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MRS 2578

Catalog No. A11486
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P2Y6 Receptor 拮抗剂

MRS 2578是P2Y6核苷酸受体的选择性拮抗剂。了解更多

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Laropiprant (MK0524)

Catalog No. A11483
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DP1 抑制剂

Laropiprant (MK0524)与烟酸合用可降低血液胆固醇。是一种有效的，选择性的 DP receptor 拮抗剂，Ki 值为 0.57 nM，对 TP 受体的 Ki 值为 2.95 nM。了解更多

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SB269970 HCl

Catalog No. A11925
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5-HT7 receptor 拮抗剂

SB269970 HCl是有效的选择性5-HT7受体拮抗剂。了解更多

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Memantine hydrochloride

Catalog No. A11708
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NMDA receptor 拮抗剂

Memantine hydrochloride是nmda受体的拮抗剂，与离子通道位点结合。它还是CYP2B6和CYP2D6抑制剂，作用于重组CYP2B6和CYP2D6，Ki分别为0.51 nM和94.9 μM。它被用于治疗帕金森综合征。了解更多

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Orphenadrine citrate

Catalog No. A11712
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NMDA receptor 拮抗剂

Orphenadrine柠檬酸盐是NMDA受体拮抗剂，Ki为6.0μM，还是HERG钾离子通道阻断剂。了解更多

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Metoprolol tartrate

Catalog No. A11713
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Beta1 receptor blocker

Metoprolol tartrate是一种选择性β1受体阻滞剂，用于治疗多种心血管系统疾病，尤其是高血压。了解更多

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Lafutidine

Catalog No. A11714
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H2 receptor 拮抗剂

Lafutidine是具有多峰作用机制的第二代H2受体拮抗剂。了解更多

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WIN 55,212-2 mesylate

Catalog No. A11932
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CB receptor 激动剂

WIN 55,212-2 mesylate是一种有效的cannabinoid receptor激动剂，在神经性疼痛的大鼠模型中具有有效的镇痛作用。它通过受体介导的信号激活p42和p44 MAP激酶。了解更多

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- Greish K, .et al. Synthetic cannabinoids nano-micelles for the management of triple negative breast cancer, J Control Release, 2018, Dec 10;291:184-195 PMID: 30367922
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Detomidine hydrochloride

Catalog No. A10298
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Adrenergic Receptor 激动剂

Detomidine hydrochloride是具有镇痛作用的镇静剂。α2-肾上腺素能激动剂产生剂量依赖性的镇静和镇痛作用，并通过激活α2儿茶酚胺受体介导，从而引起负反馈反应，从而减少兴奋性神经递质的产生。了解更多

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BML-190

Catalog No. A11938
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CB2 receptor ligand

BML-190是CB2受体的选择性反向激动剂。了解更多

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CGS 21680 HCl Hydrate

Catalog No. A11619
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Adenosine A2A Receptor 激动剂

CGS 21680 HCl是一种特定的腺苷A2A亚型受体激动剂。了解更多

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- Qian Wang, .et al. cAMP-producing chemogenetic and adenosine A2a receptor activation inhibits the inwardly rectifying potassium current in striatal projection neurons, Neuropharmacology, 2019, 148: 229-243 PMID: 30659840
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TCN 201

Catalog No. A11947
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NMDA Receptor 拮抗剂

TCN 201是对NR1/NR2A相对于含NR1/NR2B的受体具有选择性的NMDA受体拮抗剂。了解更多

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Aminophylline

Catalog No. A10066
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Adenosine receptor 拮抗剂

Aminophylline是一种非选择性的腺苷受体拮抗剂和磷酸二酯酶抑制剂，能够逆转局部缺血引起的bradyasystole。了解更多

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Aniracetam

Catalog No. A10078
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AMPA Receptor 抑制剂

Aniracetam是一种安非他命，属于消旋体化学类别的促智药，据称比吡乙酰胺更有效。了解更多

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Bethanechol chloride

Catalog No. A10180
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Muscarinic receptor 激动剂

Bethanechol chloride是拟副交感神经的胆碱氨基甲酸酯，可选择性刺激毒蕈碱受体，而不会对烟碱样受体产生任何影响。了解更多

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Cimetidine

Catalog No. A10218
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H2-receptor 拮抗剂

Cimetidine是一种抑制胃酸产生的组胺H2受体拮抗剂。了解更多

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Clomipramine HCl

Catalog No. A10231
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5-HT Receptor 激动剂

Clomipramine HCl是下列转运蛋白的阻滞剂：5-羟色胺转运蛋白 (SERT)(Ki = 0.14 nM)，去甲肾上腺素转运蛋白（NET）(Ki = 54 nM)，多巴胺转运蛋白（DAT）(Ki = 3，020 nM)，甘氨酸转运蛋白（GlyT/LeuT）。了解更多

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Dyphylline

Catalog No. A10339
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Adenosine receptor 拮抗剂

Dyphylline是黄嘌呤衍生物，具有支气管扩张药和血管扩张药的作用。它充当腺苷受体拮抗剂和磷酸二酯酶抑制剂。了解更多

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GW842166X

Catalog No. A11253
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CB2 receptor 激动剂

GW842166X是一种选择性的非大麻类CB2受体激动剂，EC50为63 nM，对CB1受体没有显著的活性。了解更多

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Ki16198

Catalog No. A11966
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LPA Receptor 拮抗剂

Ki16198是有效的LPA受体拮抗剂，可抑制LPA1和LPA3诱导的肌醇磷酸生成，Ki分别为0.34μM和0.93μM。了解更多

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Ketanserin (Vulketan Gel)

Catalog No. A10497
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5-HT2A serotonin receptor 拮抗剂

Ketanserin (Vulketan Gel)是大鼠和人5-HT2A血清素受体拮抗剂，Ki为2.5 nM。了解更多

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Bepotastine Besilate

Catalog No. A11340
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Histamine Receptor 拮抗剂

Bepotastine Besilate是组胺H1受体激动剂。了解更多

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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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MK-0517 (Fosaprepitant)

Catalog No. A11756
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neurokinin-1 receptor 拮抗剂

MK-0517 (Fosaprepitant,L-758,298)是Aprepitant的水溶性磷酰基前药，它是NK1拮抗剂。了解更多

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Anamorelin HCl

Catalog No. A12345
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Anamorelin HCl目前正在开发中，是口服活性的饥饿素受体（ghrelin receptor）激动剂。用于治疗与恶病质/厌食症相关的非小肺癌。了解更多

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- Makito Miyake, .et al. Supplementary Oral Anamorelin Mitigates Anorexia and Skeletal Muscle Atrophy Induced by Gemcitabine Plus Cisplatin Systemic Chemotherapy in a Mouse Model, Cancers (Basel), 2020, Jul 17;12(7):E1942 PMID: 32709007
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Granisetron Hydrochloride

Catalog No. A10437
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5-HT3 receptor 拮抗剂

Granisetron Hydrochloride是血清素5-ht3受体拮抗剂。了解更多

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Rupatadine Fumarate

Catalog No. A12356
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PAFR 抑制剂/H1 receptor 抑制剂

Rupatadine Fumarate是PAFR和组胺(H1)受体的抑制剂，Ki分别为550和102 nM。了解更多

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Rupatadine

Catalog No. A11222
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PAFR 抑制剂/H1 receptor 抑制剂

Rupatadine是PAFR和组胺（H1）受体的抑制剂，Ki分别为550和102 nM。了解更多

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SDZ 220-581

Catalog No. A12426
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NMDA receptor 拮抗剂

SDZ 220-581是一种竞争性NMDA受体拮抗剂（pKi = 7.7）。了解更多

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Almotriptan malate (Axert)

Catalog No. A11799
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5-HT Receptor 激动剂

Almotriptan malate (Axert)是一种选择性的5-羟色胺1B/1D（5-HT1B/1D）受体激动剂，用于治疗成人偏头痛。了解更多

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- Li Li, .et al. Delineating a serotonin 1B receptor circuit for appetite suppression in mice, J Exp Med, 2022, Aug 1;219(8):e20212307 PMID: 35796804
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Aripiprazole (Abilify)

Catalog No. A11801
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5-HT1A receptor 激动剂

Aripiprazole (Abilify)是人5-HT1A受体部分激动剂，Ki为4.2 nM。了解更多

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- Jaime Osuna-Luque, .et al. Behavioral Mechanisms That Depend on Dopamine and Serotonin in Caenorhabditis elegans Interact With the Antipsychotics Risperidone and Aripiprazole, J Exp Neurosci, 2018, 12: 1179069518798628 PMID: 30245571
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Prednisone (Adasone)

Catalog No. A10752
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Glucocorticoid Receptor 激动剂

Prednisone (Adasone)可降低粘膜TNF-a的产生，肠道通透性和NF-kB表达水平。了解更多

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Carvedilol

Catalog No. A11843
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β2-adrenergic receptor

Carvedilol是具有抗氧化特性的β1和β2肾上腺素能受体（AR）激动剂。了解更多

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Loxiglumide (CR1505)

Catalog No. A11769
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CCK-A receptor 拮抗剂

Loxiglumide (CR1505)是一种胆囊收缩素拮抗剂。了解更多

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Salmeterol

Catalog No. A11788
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beta2-adrenergic receptor 激动剂

Salmeterol是一种长效β2-肾上腺素能受体激动剂。了解更多

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MK-2894

Catalog No. A11497
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EP4 receptor 拮抗剂

MK-2894是一种高度有效和选择性的第二代EP4拮抗剂。了解更多

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MK-4305 (Suvorexant)

Catalog No. A11500
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OX receptor 拮抗剂

Suvorexant (MK-4305)是OX1R和OX2R的有效，选择性和口服可生物利用的拮抗剂，目前正在临床研究中作为失眠的新疗法。了解更多

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- Richard L Spinieli, .et al. Orexin contributes to eupnea within a critical period of postnatal development, Am J Physiol Regul Integr Comp Physiol, 2021, Oct 1;321(4):R558-R571 PMID: 34405704
- Jacob W Clark, .et al. Manipulation of REM sleep via orexin and GABAA receptor modulators differentially affects fear extinction in mice: effect of stable versus disrupted circadian rhythm, Sleep, 2021, Mar 15;zsab068 PMID: 33720375
- Zhang B, .et al. Hypothalamic orexin and mechanistic target of rapamycin activation mediate sleep dysfunction in a mouse model of tuberous sclerosis complex, Neurobiol Dis, 2019, Oct 9;134:104615 PMID: 31605778
- Obara K, .et al. Assessment of Inhibitory Effects of Hypnotics on Acetylcholine-Induced Contractions in Isolated Rat Urinary Bladder Smooth Muscle, Biol Pharm Bull, 2019, 42(2):280-288 PMID: 30713259
- James B Jaggard, .et al. Hypocretin underlies the evolution of sleep loss in the Mexican cavefish, eLife, 2018, 7: e32637 PMID: 29405117
- Skillman B, .et al. Quantification of suvorexant in blood using liquid chromatography-quadrupole/time of flight (LC-Q/TOF) mass spectrometry, J Chromatogr B Analyt Technol Biomed Life Sci, 2018, Aug 1;1091:87-95 PMID: 29859493
- Clark L, .et al. On the use of Pichia pastoris for isotopic labeling of human GPCRs for NMR studies, J Biomol NMR, 2018, Aug;71(4):203-211 PMID: 30121871
- Sullinger S, .et al. Identification of Suvorexant in Urine Using Liquid Chromatography-Quadrupole/Time-of-Flight Mass Spectrometry (LC-Q/TOF-MS), J Anal Toxicol, 2017, Apr 1;41(3):224-229 PMID: 28035034
- Carson M, .et al. Quantification of suvorexant in urine using gas chromatography/mass spectrometry, J Chromatogr B Analyt Technol Biomed Life Sci, 2017, Jan 1;1040:289-294 PMID: 27825624
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SB-277011

Catalog No. A11559
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dopamine D3 receptor 拮抗剂

SB-277011是一种用作有效和选择性多巴胺D3受体拮抗剂的药物，其对D3的选择性约为D2的80-100倍，并且缺乏任何部分激动剂活性。了解更多

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Sitaxsentan sodium (TBC-11251)

Catalog No. A11564
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ETA receptor 拮抗剂

Sitaxsentan sodium (TBC-11251)是一种选择性内皮素受体A拮抗剂，IC50和Ki分别为1.4 nM和0.43 nM。了解更多

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Tolvaptan

Catalog No. A11594
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vasopressin receptor 2 拮抗剂

Tolvaptan是一种选择性的竞争性精氨酸加压素受体2拮抗剂，IC50为1.28μM。了解更多

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GW 501516

Catalog No. A11437
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PPARδ receptor 激动剂

GW501516是一种合成pparδ特异性激动剂，对pparδ (ki=1.1 nm)显示出高亲和力，其选择性超过pparα和pparγ的1000倍。了解更多

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Eletriptan hydrobromide

Catalog No. A11418
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5-HT1B/1D receptor 激动剂

Eletriptan hydrobromide是一种选择性SR-1B/SR-1D激动剂。了解更多

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- Li Li, .et al. Delineating a serotonin 1B receptor circuit for appetite suppression in mice, J Exp Med, 2022, Aug 1;219(8):e20212307 PMID: 35796804
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Vortioxetine (Lu AA21004) hydrobromide

Catalog No. A12602
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5-HT Receptor modulator

Vortioxetine (Lu AA21004) hydrobromide是一种口服多峰血清素能药物，可抑制5-HT（1A），5-HT（1B），5-HT（3A），5-HT（7）和SERT，IC50为15 nM，33 nM，3.7 nM，19 nM和1.6 nM。了解更多

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MPEP

Catalog No. A12589
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mGlu5 receptor 拮抗剂

MPEP是mGlu5受体亚型（IC50 = 36 nM）的有效且高度选择性的非竞争性拮抗剂，并且是mGlu4受体的正构构调节剂。了解更多

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SB-408124

Catalog No. A11567
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OX Receptor 拮抗剂

SB-408124是一种选择性的非肽orexin OX1受体拮抗剂(人OX1和OX2受体的Kb值分别为21.7和1405 nM)。体内口服后阻断orexin-A诱导的修饰。了解更多

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MK-0679 (Verlukast)

Catalog No. A11607
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LTD4 receptor 拮抗剂

MK-0679 (Verlukast)是有效的白三烯D4拮抗剂。了解更多

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NBI-42902

Catalog No. A12375
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GnRH receptor 抑制剂

NBI-42902是人促性腺激素释放激素受体的新型非肽拮抗剂。了解更多

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SCH 442416

Catalog No. A12695
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A2A Receptor 拮抗剂

SCH 442416是一种选择性的腺苷A2A受体拮抗剂。以高亲和力结合人和大鼠A2A受体（Ki值分别为0.048和0.5 nM）。在体外对hA2A的选择性比hA1高> 23000倍，并且对hA2B和hA3受体的亲和力最小（IC50> 10μM）。了解更多

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