Pharmacology Research and Perspectives This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.

Metabolite profiling of foslevodopa/foscarbidopa in plasma of healthy human participants by LC ‐HRMS indicates no major differences compared to administration of levodopa/carbidopa intestinal gel
Extracted ion chromatograms of drug-related material from pooled plasma after administration of LCIG and foslevodopa/foscarbidopa to healthy human participants AbstractAnalysis was conducted to compare levodopa/carbidopa pharmacokinetics and drug-related material in plasma of healthy participants after receiving a continuous infusion of Levodopa/Carbidopa Intestinal Gel (LCIG) to a continuous subcutaneous infusion of foslevodopa/foscarbidopa. Study samples were from a randomized, open-label, 2-period crossover study in 20 healthy participants. Participants received either 24-h foslevodopa/foscarbidopa SC infusion to the ab...
Source: Pharmacology Research and Perspectives - April 11, 2024 Category: Drugs & Pharmacology Authors: John P. Savaryn, Richard L. Smith, Matthew Rosebraugh, Melina Neenan, Richard Burton, Kennan Marsh, David Wagner Tags: ORIGINAL ARTICLE Source Type: research

Absorption and pharmacokinetics of bupivacaine after bilateral topical administration in tonsillar fossae for posttonsillectomy pain relief
In conclusion, this study shows that applying 4 mL of bupivacaine 5 mg/mL by a swab in the tons illar fossae posttonsillectomy yields very low plasma concentrations, suggesting its safe application without any risk of systemic toxic effects. (Source: Pharmacology Research and Perspectives)
Source: Pharmacology Research and Perspectives - April 10, 2024 Category: Drugs & Pharmacology Authors: Kristin Sandal Berg, Ellisiv Seines, Peter G ál, Lise Løberg‐Emanuelsen, Audun Stubhaug, Erik Waage Nielsen, Olav Spigset Tags: ORIGINAL ARTICLE Source Type: research

Ursodeoxycholic acid may protect from severe acute respiratory syndrome coronavirus 2 Omicron variant by reducing angiotensin ‐converting enzyme 2
We found that UDCA-fed hamsters effectively inhibited viral transmission from Omicron variant-infected hamsters and verified UDCA-derived downregulation of ACE2 expression in respiratory organs. As an FXR antagonist, UDCA may protect against SARS-CoV-2 Omicron variant. AbstractThe SARS-CoV-2 caused COVID-19 pandemic has posed a global health hazard. While some vaccines have been developed, protection against viral infection is not perfect because of the urgent approval process and the emergence of mutant SARS-CoV-2 variants. Here, we employed UDCA as an FXR antagonist to regulate ACE2 expression, which is one of the key pa...
Source: Pharmacology Research and Perspectives - April 5, 2024 Category: Drugs & Pharmacology Authors: Kyungmin Lee, Yujeong Na, Minjin Kim, Dongjin Lee, Jongseo Choi, Gwanyoung Kim, Min ‐Soo Kim Tags: ORIGINAL ARTICLE Source Type: research

Lanthanum hydroxide protects kidney through gut microbiota in a rat model of chronic kidney disease
This study underscores the significance of lanthanum hydroxide in kidney protection, attributing its benefits to the modulation of gut microbiota in a rat model of CKD. (Source: Pharmacology Research and Perspectives)
Source: Pharmacology Research and Perspectives - April 2, 2024 Category: Drugs & Pharmacology Authors: Yuan Gao, Shengnan Wang, Lijun Sun, Bing Li, Hong Liu, Ren Bu, Changhai Su, Min Guo, Yang Liu, Lulu Zhao, Chao Gu, Xiaojia Li, Xiaorong Yuan, Qiwen Wang, Gang Li Tags: ORIGINAL ARTICLE Source Type: research

Evaluation of OCT2 ‐mediated drug–drug interactions between ulotaront and metformin in subjects with schizophrenia
Plasma and urine pharmacokinetic parameters of metformin along and in combination with ulotaront. AbstractUlotaront (SEP-363856) is a TAAR1 agonist, with 5-HT1A agonist activity, currently in clinical development for the treatment of schizophrenia. In  vitro studies indicate ulotaront is an OCT2-specific inhibitor with IC50 of 1.27  μM. The primary objective of this study is to determine if a single dose of ulotaront affects the PK of metformin, an index substrate of OCT2, in subjects with schizophrenia. In a randomized, single-blind, 2-period crossover study, 25 adults with schizophrenia received a single dose of metf...
Source: Pharmacology Research and Perspectives - March 26, 2024 Category: Drugs & Pharmacology Authors: Guangqing Xiao, Hironobu Tsukada, Yu ‐Luan Chen, Lei Shi, Seth C. Hopkins, Gerald R. Galluppi Tags: ORIGINAL ARTICLE Source Type: research

Synthesis of salcaprozate sodium and its significance in enhancing pancreatic kininogenase absorption performance
This study has established a low-cost, environmentally friendly, and safe SNAC synthesis route with high process yield suitable for industrial production. SNAC demonstrates an absorption-enhancing effect on PK, and the optimal ratio of SNAC to PK is determined to be 32:1. (Source: Pharmacology Research and Perspectives)
Source: Pharmacology Research and Perspectives - March 22, 2024 Category: Drugs & Pharmacology Authors: Zhong Lv, Qian ‐Dong Luo, Zhang‐Yong Tang, Xiao‐Hu Lv, Tao Wu, Ling‐Kai Huang, Can Tang Tags: ORIGINAL ARTICLE Source Type: research

Modulation of TNF ‐α, interleukin‐6, and interleukin‐10 by nebivolol–valsartan and nebivolol–lisinopril polytherapy in SHR rats
This study provides compelling evidence that concurrent administration of nebivolol with lisinopril or valsartan exerts time-dependent effects, reducing proinflammatory cytokines TNF-α and IL-6 while modifying IL-10 levels in an experimental hypertensive model. (Source: Pharmacology Research and Perspectives)
Source: Pharmacology Research and Perspectives - March 20, 2024 Category: Drugs & Pharmacology Authors: Lezama ‐Martinez Diego, Flores‐Monroy Jazmin, Ramirez‐Hernandez Diana, Garrido‐Farina German‐Isauro, Fonseca‐Coronado Salvador, Hernandez‐Campos Maria‐Elena Tags: ORIGINAL ARTICLE Source Type: research

Preclinical metabolism and the disposition of vornorexant/TS ‐142, a novel dual orexin 1/2 receptor antagonist for the treatment of insomnia
Proposed metabolic pathways of vornorexant are presented. Vornorexant is rapidly absorbed and undergoes extensive metabolism. Vornorexant and its metabolites are rapidly eliminated without tissue residue. The unchanged form mainly contributes to the drug efficacy. AbstractWe investigated the metabolism and disposition of vornorexant, a novel dual orexin receptor antagonist, in rats and dogs, and clarified in  vitro metabolite profiles in humans. Furthermore, we investigated the pharmacokinetics of active metabolites in rats and dogs and their CNS distribution in rats to elucidate its contribution to drug efficacy. [14C]vo...
Source: Pharmacology Research and Perspectives - March 16, 2024 Category: Drugs & Pharmacology Authors: Yoshihiro Konno, Shunsuke Kamigaso, Hidetoh Toki, Shuichi Terasaka, Hirohiko Hikichi, Hiromi Endo, Jun ‐Ichi Yamaguchi, Akiko Mizuno‐Yasuhira Tags: ORIGINAL ARTICLE Source Type: research

The role of histamine H1 receptor in the anterior cingulate cortex on nociception level following acute restraint stress in male rats
Analgesic effect of intra-ACC microinjection of histamine and mepyramine. AbstractConsidering the importance of pain and stress, we decided to investigate the intra-anterior cingulate cortex (ACC) microinjection of histamine and mepyramine alone and concurrently on acute pain induced by hot plate following restraint stress in male rats. 24-gauge, 10  mm stainless steel guide cannula was implanted over the ACC in the incised scalp of 4 groups. Restraint stress in healthy rats produced a significant increase (p <  .05) in the pain threshold. The simultaneous microinjection of 4 μg/side histamine and 8 μg/side ...
Source: Pharmacology Research and Perspectives - March 14, 2024 Category: Drugs & Pharmacology Authors: Roxana Daniali, Fatemeh Zeraati, Mozhdeh Mohammadi, Rasool Haddadi Tags: ORIGINAL ARTICLE Source Type: research