Sidharta, Patricia N. van Giersbergen, Paul L.M. Dingemanse, Jasper
Published in
Pharmacology
Purpose: To investigate the multiple-dose pharmacokinetics (PK), pharmacodynamics (PD), and tolerability of palosuran, a selective, potent antagonist of the human UT receptor. Methods: This was a double-blind, randomized, placebo-controlled study. Three dose levels were investigated for PKs, PDs, and safety in sequential groups of 8 subjects each. ...
Lee, Hyung Gon Song, Ji A Han, Dong Soo Woo, Kyeong Wan Yoon, Myung Ha
Published in
Pharmacology
This study examined the effects of intrathecal areca nut on spinal nerve-ligated and chemotherapy-induced neuropathic pain (NP), and investigated the relevance of spinal 5-hydroxytryptamine (5-HT) and α2-adrenergic receptors to those effects. For drug administration, intrathecal catheters were inserted into the subarachnoid space of male Sprague-Da...
Wei, Can Liu, Zhengfang Li, Luchao Zhang, Yanbin Fang, Zhiqing Fan, Yidong
Published in
Pharmacology
Background: Trametes robiniophila Murr (Huaier) has been used as an adjuvant therapy of tumor in traditional Chinese medicine for many years, but the underlying mechanisms are largely unknown. In the present study, we tested the inhibitory effect of Huaier extract on renal cancer 786-O cells and explored the possible mechanisms. Methods: 786-O cell...
Brown, Andrew J. Castellano-Pellicena, Irene Haslam, Carl P. Nichols, Paula L. Dowell, Simon J.
Published in
Pharmacology
Background/Aims: CID16020046 blocks the effect of the lipid lysophosphatidylinositol (LPI) at its receptor, GPR55. CID16020046 and another antagonist, ML193, have been used to investigate GPR55-mediated effects of LPI on cells, tissues, and in vivo. Here we describe the structure-activity relationship of CID16020046. Methods: Yeast or human cells w...
Chiu, Kuan-Ming Lin, Tzu-Yu Lee, Ming-Yi Lu, Cheng-Wei Wang, Ming-Jiuh Wang, Su-Jane
Published in
Pharmacology
Background: Ropivacaine, a long-acting amide local anesthetic agent, has been demonstrated to inhibit glutamatergic transmission. Glutamate neurotoxicity plays a pivotal role in the pathogenesis of brain disorders. The purpose of this study is to investigate the neuroprotective effect of ropivacaine against brain damage induced by kainic acid (KA),...
Shemesh, Gil Kara, Nirit Einat, Haim
Published in
Pharmacology
Background: Lithium (Li) is the prototypic mood-stabilizing drug, but the individual response to Li is highly heterogeneous. Some evidence suggest interactions between Li and stress, and it is possible to hypothesize that lithium’s effects are modified by stress conditions. The current study examines the interaction between 2 chronic stressors, con...
Lv, Chang-Cheng Xia, Man-Li Shu, Shu-Juan Chen, Fei Jiang, Li-Shan
Published in
Pharmacology
Remifentanil-induced hyperalgesia (RIH) is known to be associated with oxidative stress and inflammation. Betulinic acid (BA) was reported to reduce visceral pain owing to its anti-oxidative and anti-inflammatory potential. Here, we explored whether BA can attenuate RIH through inhibiting oxidative stress and inflammation in spinal dorsal horn. Sp...
Imanishi, Masaki Izawa-Ishizawa, Yuki Sakurada, Takumi Kohara, Yusuke Horinouchi, Yuya Sairyo, Eriko Zamami, Yoshito Takechi, Kenshi Chuma, Masayuki Fukushima, Keijo
...
Published in
Pharmacology
Background/Aims: We have reported that nitrosonifedipine (NO-NIF), a photodegradation product of nifedipine, has strong antioxidant and endothelial protective effects, and can suppress several cardiovascular diseases in animal models. The objective of the present study was to investigate the effects of NO-NIF on aortic aneurysm formation. Methods: ...
Dong, Penghong Gu, Xiaochuan Zhu, Guiling Li, Ming Ma, Bin Zi, Ying
Published in
Pharmacology
The function of melatonin (MLT) in promoting fracture healing has been demonstrated in previous studies. However, the molecular mechanism underlying therapeutic effects of MLT is not entirely clear. In this study, mesenchymal stem cells (MSCs) were isolated from rat bone marrow and identified by flow cytometry. We found that MLT treatment upregulat...
Lee, Chih-Hsin Lin, Yuan-Feng Chen, Yen-Chou Wong, Shuit-Mun Juan, Shu-Hui Huang, Huei-Mei
Published in
Pharmacology
We previously synthesized new tubulin inhibitors, MPT0B169 and MPT0B002, which induced growth inhibition and apoptosis in leukemia cells. However, their effects on solid tumor cells have not been determined. In this study, we investigated the effects of MPT0B169 and MPT0B002 on glioblastoma, breast, lung, and colorectal cancer (CRC) cell lines. A c...
