Specific beta-adrenergic receptors were demonstrated in the urinary bladder of adult and developing rats, by direct tissue binding with LD [125I]-cyanopindolol (CYP). The maximum number of binding sites (Bmax) was 167 +/- 25 fmol/mg membrane protein and the dissociation constant (KD) equalled 61 +/- 33 pM. The Hill slopes of the LD [125I]-CYP binding showed a single class of noncooperative receptor sites. The rank order of potency of agonist competition for LD [125I]-CYP binding suggests that the receptors are mostly of the beta 2 subtype. Beta-adrenergic receptor density was approximately half in the first 10 days of life (Bmax 63 to 77 fmol/mg protein) compared with the older age-groups studied (Bmax 91 to 167 fmol/ng protein). On the 1st day after delivery, the calculated beta-adrenergic receptor number/bladder was 9.4, and it increased significantly with age to 2,496 in the adult rat. This is a 250-fold increase in the number of receptors/bladder, while only a 20-fold increase in membrane protein and a five- to sixfold increase in the bladder weight was observed. Thus, an age-dependent increase of beta-adrenergic receptors on the cell membrane surface area occurred in the developing urinary bladder of the rat.
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J Comput Chem
January 2025
Departamento de Fisicoquímica, Facultad de Química, Universidad Nacional Autónoma de México, Coyoacán, CDMX, Mexico.
The G protein-coupled receptor (GPCR) pharmacology accounts for a significant field in research, clinical studies, and therapeutics. Computer-aided drug discovery is an evolving suite of techniques and methodologies that facilitate accelerated progress in drug discovery and repositioning. However, the structure-activity relationships of molecules targeting GPCRs are highly challenging in many cases since slight structural modifications can lead to drastic changes in biological functionality.
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January 2025
Programa de Investigación de Cancer de Mama, Instituto de Investigaciones Biomédicas, Universidad Nacional Autónoma de México, Mexico City, Mexico; Departamento de Medicina Genómica y Toxicología Ambiental, Instituto de Investigaciones Biomédicas, Universidad Nacional Autónoma de México, Mexico City, Mexico. Electronic address:
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January 2025
Pharmacology, Toxicology and Biochemistry Department, Faculty of Pharmacy, Future University in Egypt (FUE), Cairo, Egypt; Pharmacology and Toxicology Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
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January 2025
Department of Biotechnology, Daegu University, Gyeongsan, Gyeongbuk, 38453, Republic of Korea. Electronic address:
Capsaicin, a polyphenol, is known to regulate energy expenditure and thermogenesis in adipocytes and muscles. However, its role in modulating uncoupling proteins (UCPs) and adenosine triphosphate (ATP)-dependent thermogenesis in muscles remains unclear. This study investigated the mechanisms underlying the role of capsaicin in modulating the UCP- and ATP-dependent thermogenesis in C2C12 myoblasts, as well as the gastrocnemius (GM) and soleus muscles (SM) of mice.
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