15th Scientific Symposium of the Austrian Pharmacological Society (APHAR) [0.03%]
第十五届奥地利药理学协会（APhAr）科学研讨会
Elisabeth Moser,Pia Tschische,Wolfgang Platzer et al.
Elisabeth Moser et al.
Novel olanzapine analogues presenting a reduced H1 receptor affinity and retained 5HT2A/D2 binding affinity ratio [0.03%]
具有降低的H1受体亲和力和保留的5-HT2A/D2结合亲和力比的新一代奥氮平类似物
Somayeh Jafari,Marc E Bouillon,Xu-Feng Huang et al.
Somayeh Jafari et al.
Background: Olanzapine is an atypical antipsychotic drug with high clinical efficacy, but which can cause severe weight gain and metabolic disorders in treated patients. Blockade of the histamine 1 (H1) receptors is belie...
Lipid phosphate phosphatase inhibitors locally amplify lysophosphatidic acid LPA1 receptor signalling in rat brain cryosections without affecting global LPA degradation [0.03%]
脑切片中的脂质磷酸酶抑制剂可在局部放大甘油磷脂酸（LPA）LPA1受体信号转导而不影响整体LPA降解
Niina Aaltonen,Marko Lehtonen,Katri Varonen et al.
Niina Aaltonen et al.
Background: Lysophosphatidic acid (LPA) is a signalling phospholipid with multiple biological functions, mainly mediated through specific G protein-coupled receptors. Aberrant LPA signalling is being increasingly implicat...
The orthosteric agonist 2-chloro-5-hydroxyphenylglycine activates mGluR5 and mGluR1 with similar efficacy and potency [0.03%]
2-氯-5-羟基苯甘氨酸以相似的效力和效价活化mGluR5和mGluR1
Paul J Kammermeier
Paul J Kammermeier
Background: The efficacy, potency, and selectivity of the compound 2-Chloro-5-hydroxyphenylglycine (CHPG), a nominally selective agonist for metabotropic glutamate receptor 5 (mGluR5), were examined with select mGluRs by ...
Comparative Study
BMC pharmacology. 2012 May 29:12:6. DOI:10.1186/1471-2210-12-6 2012
Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity [0.03%]
长效κ阿片受体拮抗剂nor-BNI、GNTI和JDTic：小鼠药代动力学及亲脂性研究
Thomas A Munro,Loren M Berry,Ashlee Van&#x;t Veer et al.
Thomas A Munro et al.
Background: Nor-BNI, GNTI and JDTic induce κ opioid antagonism that is delayed by hours and can persist for months. Other effects are transient. It has been proposed that these drugs may be slowly absorbed or distributed...
5-hydroxytryptamine (5-HT) reduces total peripheral resistance during chronic infusion: direct arterial mesenteric relaxation is not involved [0.03%]
5-羟色胺（5-HT）在慢性输注期间通过减少总外周阻力来发挥作用：不涉及直接动脉肠系膜松弛作用
Robert Patrick Davis,Jill Pattison,Janice M Thompson et al.
Robert Patrick Davis et al.
Serotonin (5-hydroxytryptamine; 5-HT) delivered over 1 week results in a sustained fall in blood pressure in the sham and deoxycorticosterone acetate (DOCA)-salt rat. We hypothesized 5-HT lowers blood pressure through direct receptor-mediat...
Contrasting effects of linaclotide and lubiprostone on restitution of epithelial cell barrier properties and cellular homeostasis after exposure to cell stressors [0.03%]
利那洛肽和鲁比前列酮对细胞应激暴露后上皮细胞屏障特性和细胞稳态修复的不同影响
John Cuppoletti,Anthony T Blikslager,Jayati Chakrabarti et al.
John Cuppoletti et al.
Background: Linaclotide has been proposed as a treatment for the same gastrointestinal indications for which lubiprostone has been approved, chronic idiopathic constipation and irritable bowel syndrome with constipation. ...
Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor [0.03%]
沙格列汀与DPP4的强效性、选择性和长时间结合：与其他快速解离的DPP-4抑制剂相比，沙格列汀在体外和离体实验中维持对DPP4的抑制作用
Aiying Wang,Charles Dorso,Lisa Kopcho et al.
Aiying Wang et al.
Background: Dipeptidylpeptidase 4 (DPP4) inhibitors have clinical benefit in patients with type 2 diabetes mellitus by increasing levels of glucose-lowering incretin hormones, such as glucagon-like peptide -1 (GLP-1), a p...
Comparative Study
BMC pharmacology. 2012 Apr 4:12:2. DOI:10.1186/1471-2210-12-2 2012
Computational models for in-vitro anti-tubercular activity of molecules based on high-throughput chemical biology screening datasets [0.03%]
基于高通量化学生物学筛选数据集的体外抗结核分子计算模型
Vinita Periwal,Shireesha Kishtapuram;Open Source Drug Discovery Consortium;Vinod Scaria
Vinita Periwal
Background: The emergence of Multi-drug resistant tuberculosis in pandemic proportions throughout the world and the paucity of novel therapeutics for tuberculosis have re-iterated the need to accelerate the discovery of n...
The effect of formulation vehicles on the in vitro percutaneous permeation of ibuprofen [0.03%]
赋形剂对布洛芬体外透皮渗透的影响研究
Jessica Stahl,Mareike Wohlert,Manfred Kietzmann
Jessica Stahl
Background: The transdermal application of substances represents an elegant approach to overcome side effects related to injections or oral treatment. Due to benefits like a constant plasma level, no pain during applicati...