Zobrazeno 1 - 10
of 333
pro vyhledávání: '"biased agonist"'
Autor:
Mehri Hajiaghayi, Fatemeh Gholizadeh, Eric Han, Samuel R. Little, Niloufar Rahbari, Isabella Ardila, Carolina Lopez Naranjo, Kasra Tehranimeh, Steve C. C. Shih, Peter J. Darlington
Publikováno v:
Frontiers in Immunology, Vol 15 (2024)
IntroductionAdrenergic receptors regulate metabolic, cardiovascular, and immunological functions in response to the sympathetic nervous system. The effect of β2-adrenergic receptor (AR) as a high expression receptor on different subpopulations of T
Externí odkaz:
https://doaj.org/article/2748ccac46664ec28689a1c92833c090
Autor:
Jingchao Sun, Ying Xiao, Wei Xing, Wenjuan Jiang, Xuefeng Hu, Hongchao Li, Zhaojun Liu, Qian Jin, Peng Ren, Hongmei Zhang, Peter E. Lobie
Publikováno v:
Biomedicine & Pharmacotherapy, Vol 177, Iss , Pp 116965- (2024)
Background and purpose: GLP-1 receptor agonists are clinically utilized for type 2 diabetes and obesity. In vitro and in vivo preclinical studies were performed to assess the druggability of a novel small molecule GLP-1 receptor biased agonist SAL011
Externí odkaz:
https://doaj.org/article/a51f40fb0a8445d1b98d5441114b45cf
Publikováno v:
International Journal of Molecular Sciences, Vol 25, Iss 19, p 10470 (2024)
Biased agonists of G-protein-coupled receptors (GPCRs) have emerged as promising selective modulators of signaling pathways by offering therapeutic advantages over unbiased agonists to minimize side effects. The dopamine D3 receptor (D3R), a pivotal
Externí odkaz:
https://doaj.org/article/d9502cc574bb4992bcf292f60622ddc2
Publikováno v:
Biomedicines, Vol 12, Iss 7, p 1551 (2024)
Cannabielsoin (CBE) is primarily recognized as an oxidation byproduct of cannabidiol (CBD) and a minor mammalian metabolite of CBD. The pharmacological interactions between CBE and cannabinoid receptors remain largely unexplored, particularly with re
Externí odkaz:
https://doaj.org/article/dbcb16ea056b4660912088d736fc1d13
Autor:
Yanhao Guo, Ruimin Yu, Tao Zhang, Fengxia Ren, Zixing Yu, Jingchao Cheng, Hongxin Jia, Weiguo Shi, Yatong Zhang
Publikováno v:
Molecules, Vol 29, Iss 13, p 2961 (2024)
This study explored the potential of a series of PZM21 analogues for pain treatment. Specifically, the hydroxyphenyl ring of PZM21 was replaced with a naphthyl ring, the thienyl ring was substituted with either a phenyl ring or furan rings, and the e
Externí odkaz:
https://doaj.org/article/0626dfa7d7794f97bdf996ed2d0f30cd
Publikováno v:
Pharmacological Research, Vol 199, Iss , Pp 107047- (2024)
The 5-hydroxytryptamine 7 receptor (5-HT7) is necessary for 5-HT to cause a concentration-dependent vascular relaxation and hypotension. 5-HT7 is recognized as having biased signaling, transduced through either Gs or β -arrestin. It is unknown wheth
Externí odkaz:
https://doaj.org/article/342e21f4d0ad4ee79f6ca65f2ca09868
Autor:
Alba Vidal-Torres, Begoña Fernández-Pastor, Mónica García, Eva Ayet, Anna Cabot, Javier Burgueño, Xavier Monroy, Bertrand Aubel, Xavier Codony, Luz Romero, Rosalía Pascual, Maria Teresa Serafini, Gregorio Encina, Carmen Almansa, Daniel Zamanillo, Manuel Merlos, José Miguel Vela
Publikováno v:
Acta Pharmaceutica Sinica B, Vol 13, Iss 1, Pp 82-99 (2023)
Opioids are the most effective painkillers, but their benefit-risk balance often hinder their therapeutic use. WLB-73502 is a dual, bispecific compound that binds sigma-1 (S1R) and mu-opioid (MOR) receptors. WLB-73502 is an antagonist at the S1R. It
Externí odkaz:
https://doaj.org/article/5db3e49f2136462cbd27dfe08f2a9b36
Autor:
Liang Ye, Chunmei Li, Wanglin Jiang, Yifei Yang, Wenyan Wang, Haibo Zhu, Zhengping Hu, Ning Li, Xiaobo Cen, Hongbo Wang, Jingwei Tian
Publikováno v:
Frontiers in Pharmacology, Vol 14 (2023)
Opiates produce analgesia via G-protein signaling, and adverse effects, such as respiratory depression and decreased bowel motility, by β-arrestin pathway. Oliceridine, a G protein-biased MOR agonist, only presents modest safety advantages as compar
Externí odkaz:
https://doaj.org/article/171eca7687f743f59105a10c35232dfc
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Akademický článek
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