主要研究目的：研究空腹和餐后状态下单次口服受试制剂氨酚咖妥胶囊（规格：布他比妥50mg；对乙酰氨基酚300mg；咖啡因40mg，宜昌人福药业有限责任公司生产）与参比制剂氨酚咖妥胶囊（规格：布他比妥50mg；对乙酰氨基酚300mg；咖啡因40mg；LGM Pharma Solutions, LLC持证）在健康研究参与者体内的药代动力学，评价空腹和餐后状态口服两种制剂的生物等效性。次要研究目的：研究受试制剂氨酚咖妥胶囊和参比制剂氨酚咖妥胶囊在健康研究参与者中的安全性。

[Translation]

The main purpose of the study is to study the pharmacokinetics of the test preparation Aminocafe Capsules (specifications: butalbital 50 mg; acetaminophen 300 mg; caffeine 40 mg, produced by Yichang Renfu Pharmaceutical Co., Ltd.) and the reference preparation Aminocafe Capsules (specifications: butalbital 50 mg; acetaminophen 300 mg; caffeine 40 mg; licensed by LGM Pharma Solutions, LLC) in healthy study participants after a single oral administration in the fasting and fed state, and to evaluate the bioequivalence of the two preparations when taken orally in the fasting and fed state. Secondary purpose of the study is to study the safety of the test preparation Aminocafe Capsules and the reference preparation Aminocafe Capsules in healthy study participants.

Start Date16 Nov 2023

Sponsor / Collaborator

Yichang Humanwell Pharmaceuticals Co., Ltd.

CTR20223229 / CompletedNot Applicable

氨酚咖妥胶囊人体生物等效性研究

[Translation] Study on the bioequivalence of Aminophenecato capsules in healthy volunteers

主要研究目的：研究空腹状态下单次口服受试制剂氨酚咖妥胶囊（规格：布他比妥50mg；对乙酰氨基酚300mg；咖啡因40mg，宜昌人福药业有限责任公司生产）与参比制剂氨酚咖妥胶囊（商品名：Fioricet，规格：布他比妥50mg；对乙酰氨基酚300mg；咖啡因40mg；Nexgen Pharma,Inc生产）在健康受试者体内的药代动力学，评价空腹状态口服两种制剂的生物等效性。次要研究目的：研究受试制剂氨酚咖妥胶囊和参比制剂氨酚咖妥胶囊（Fioricet®）在健康受试者中的安全性。

[Translation]

The main purpose of the study is to study the pharmacokinetics of the test preparation Aminocafe Capsules (specifications: butalbital 50 mg; acetaminophen 300 mg; caffeine 40 mg, produced by Yichang Renfu Pharmaceutical Co., Ltd.) and the reference preparation Aminocafe Capsules (trade name: Fioricet, specifications: butalbital 50 mg; acetaminophen 300 mg; caffeine 40 mg; produced by Nexgen Pharma, Inc) in healthy subjects after a single oral administration under fasting conditions, and to evaluate the bioequivalence of the two preparations when taken orally under fasting conditions. Secondary purpose of the study: to study the safety of the test preparation Aminocafe Capsules and the reference preparation Aminocafe Capsules (Fioricet®) in healthy subjects.

Start Date24 Dec 2022

Sponsor / Collaborator

Yichang Humanwell Pharmaceuticals Co., Ltd.

CTR20220333 / CompletedNot Applicable

氨酚咖妥胶囊人体生物等效性研究（正式试验）

[Translation] Bioequivalence study of acetaminophen capsules in humans (formal trial)

主要研究目的:研究空腹和餐后状态下单次口服受试制剂氨酚咖妥胶囊（规格：布他比妥50mg；对乙酰氨基酚300mg；咖啡因40mg，宜昌人福药业有限责任公司生产）与参比制剂氨酚咖妥胶囊（Fioricet，规格：布他比妥50mg；对乙酰氨基酚300mg；咖啡因40mg；Nexgen Pharma,Inc生产）在健康受试者体内的药代动力学，评价空腹和餐后状态口服两种制剂的生物等效性。次要研究目的:研究受试制剂氨酚咖妥胶囊和参比制剂氨酚咖妥胶囊（Fioricet）在健康受试者中的安全性。

[Translation]

The main purpose of the study is to study the pharmacokinetics of the test preparation Aminocafetol Capsules (specifications: butalbital 50 mg; acetaminophen 300 mg; caffeine 40 mg, produced by Yichang Renfu Pharmaceutical Co., Ltd.) and the reference preparation Aminocafetol Capsules (Fioricet, specifications: butalbital 50 mg; acetaminophen 300 mg; caffeine 40 mg; produced by Nexgen Pharma, Inc) in healthy subjects after a single oral administration in the fasting and fed state, and to evaluate the bioequivalence of the two preparations in the fasting and fed state. Secondary purpose of the study: to study the safety of the test preparation Aminocafetol Capsules and the reference preparation Aminocafetol Capsules (Fioricet) in healthy subjects.

Start Date23 Feb 2022

Sponsor / Collaborator

Yichang Humanwell Pharmaceuticals Co., Ltd.

100 Clinical Results associated with COX x GABAA receptor

100 Translational Medicine associated with COX x GABAA receptor

0 Patents (Medical) associated with COX x GABAA receptor

Literatures (Medical) associated with COX x GABAA receptor

01 Aug 2024·Pharmacology Research & Perspectives

Interplay between microbial‐derived GABA and host GABA receptor signaling collectively influence the tumorigenic function of GABA in colon cancer

Article

Author: Fernandes, Philana ; Hyland, Niall P. ; Joyce, Susan A. ; Stanton, Catherine ; Gahan, Cormac G. M. ; Houston, Aileen ; Keane, Jonathan M. ; Kratz, Florian ; O'Callaghan, Grace

AbstractAlthough classically recognized as a neurotransmitter, gamma aminobutyric acid (GABA) has also been identified in colonic tumors. Moreover, the gut microbiome represents another potential source of GABA. Both GABAA and GABAB receptors have been implicated in contributing to the effects of GABA in colorectal cancer, with both pro‐ and anti‐tumorigenic functions identified. However, their subunit composition is often overlooked. Studies to date have not addressed whether the GABA‐producing potential of the microbiome changes over the course of colon tumor development or whether receptor subunit expression patterns are altered in colon cancer. Therefore, we investigated the clusters of orthologous group frequencies of glutamate decarboxylase (GAD) in feces from two murine models of colon cancer and found that the frequency of microbial GAD was significantly decreased early in the tumorigenic process. We also determined that microbial‐derived GABA inhibited proliferation of colon cancer cells in vitro and that this effect of GABA on SW480 cells involved both GABAA and GABAB receptors. GABA also inhibited prostaglandin E2 (PGE2)‐induced proliferation and interleukin‐6 (IL‐6) expression in these cells. Gene expression correlations were assessed using the “Cancer Exploration” suite of the TIMER2.0 web tool and identified that GABA receptor subunits were differentially expressed in human colon cancer. Moreover, GABAA receptor subunits were predominantly positively associated with PGE2 synthase, cyclooxygenase‐2 and IL‐6. Collectively, these data demonstrate decreased potential of the microbiome to produce GABA during tumorigenesis, a novel anti‐tumorigenic pathway for GABA, and that GABA receptor subunit expression adds a further layer of complexity to GABAergic signaling in colon cancer.

01 May 2024·Heliyon

Muscle relaxant and antipyretic effects of pentacyclic triterpenes isolated from the roots of Diospyros lotus L

Article

Author: Mabood, Fazal ; Khan, Ajmal ; Kashtoh, Hamdy ; Bahadar, Haji ; Aleem, Awan A ; Shareef, Huma ; Al-Harrasi, Ahmed ; Halim, Sobia Ahsan ; Rauf, Abdur ; Baek, Kwang-Hyun ; Khalid, Asaad

The present article describes the muscle relaxant and antipyretic effects of pentacyclic triterpenes, oleanolic acid (OA), ursolic acid (UA) and betulinic acid (BA) isolated from roots of Diospyros lotus in animal models. The muscle relaxant effects of isolated pentacyclic triterpenes were determined by chimney and inclined plane tests. In the chimney test, pretreatment of pentacyclic triterpenes evoked significant dose dependent influence on muscle coordination. When administered intraperitoneally (i.p.) to mice at 10 mg/kg for 90 min, OA, UA, and BA exhibited muscle relaxant effects of 66.72 %, 60.21 %, and 50.77 %, respectively. Similarly, OA, UA, and BA (at 10 mg/kg) illustrated 65.74 %, 59.84 % and 51.40 % muscle relaxant effects in the inclined plane test. In the antipyretic test, significant amelioration was caused by pretreatment of all compounds in dose dependent manner. OA, UA, and BA (at 5 mg/kg) showed 39.32 %, 34.32 % and 29.99 % anti-hyperthermic effects, respectively 4 h post-treatment, while at 10 mg/kg, OA, UA, and BA exhibited 71.59 %, 60.99 % and 52.44 % impact, respectively. The muscle relaxant effect of benzodiazepines is well known for enhancement of GABA receptors. There may exist a similar mechanism for muscle relaxant effect of pentacyclic triterpenes. The in-silico predicted binding pattern of all the compounds reflects good affinity of compounds with GABA_A receptor and COX-2. These results indicate that the muscle relaxant and antipyretic activities of these molecules can be further improved by structural optimization.

23 Mar 2023·NatureQ1 · CROSS-FIELD

An airway-to-brain sensory pathway mediates influenza-induced sickness

Q1 · CROSS-FIELD

Article

Author: Liberles, Stephen D ; Wang, Yandan ; Horio, Nao ; Chiu, Isaac M ; Prescott, Sara L ; Bin, Na-Ryum

AbstractPathogen infection causes a stereotyped state of sickness that involves neuronally orchestrated behavioural and physiological changes1,2. On infection, immune cells release a ‘storm’ of cytokines and other mediators, many of which are detected by neurons3,4; yet, the responding neural circuits and neuro–immune interaction mechanisms that evoke sickness behaviour during naturalistic infections remain unclear. Over-the-counter medications such as aspirin and ibuprofen are widely used to alleviate sickness and act by blocking prostaglandin E2 (PGE2) synthesis5. A leading model is that PGE2 crosses the blood–brain barrier and directly engages hypothalamic neurons2. Here, using genetic tools that broadly cover a peripheral sensory neuron atlas, we instead identified a small population of PGE2-detecting glossopharyngeal sensory neurons (petrosal GABRA1 neurons) that are essential for influenza-induced sickness behaviour in mice. Ablating petrosal GABRA1 neurons or targeted knockout of PGE2 receptor 3 (EP3) in these neurons eliminates influenza-induced decreases in food intake, water intake and mobility during early-stage infection and improves survival. Genetically guided anatomical mapping revealed that petrosal GABRA1 neurons project to mucosal regions of the nasopharynx with increased expression of cyclooxygenase-2 after infection, and also display a specific axonal targeting pattern in the brainstem. Together, these findings reveal a primary airway-to-brain sensory pathway that detects locally produced prostaglandins and mediates systemic sickness responses to respiratory virus infection.

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