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1.
Expert Opin Ther Pat ; 34(8): 611-625, 2024 Aug.
Article in English | MEDLINE | ID: mdl-38889204

ABSTRACT

INTRODUCTION: The P2Y14 receptor (P2Y14R), a member of the G protein-coupled receptor family, is activated by extracellular nucleotides. Due to its involvement in inflammatory, immunological and other associated processes, P2Y14R has emerged as a promising therapeutic target. Despite lacking a determined three-dimensional crystal structure, the homology modeling technique based on closely related P2Y receptors' crystallography has been extensively utilized for developing active compounds targeting P2Y14R. Recent discoveries have unveiled numerous highly effective and subtype-specific P2Y14R inhibitors. This study presents an overview of the latest advancements in P2Y14R inhibitors. AREAS COVERED: This review presents an overview of the advancements in P2Y14R inhibitor research over the past five years, encompassing new patents, journal articles, and highlighting the therapeutic prospects inherent in these compounds. EXPERT OPINION: The recent revelation of the vast potential of P2Y14R inhibitors has led to the development of novel compounds that exhibit promising capabilities for the treatment of sterile inflammation of the kidney, potentially diabetes, and asthma. Despite being a relatively nascent class of compounds, certain members have already exhibited their capacity to surmount specific challenges posed by conventional P2Y14R inhibitors. Targeting P2Y14R through small molecules may present a promising therapeutic strategy for effectively managing diverse inflammatory diseases.


Subject(s)
Drug Development , Inflammation , Patents as Topic , Animals , Humans , Asthma/drug therapy , Asthma/physiopathology , Diabetes Mellitus/drug therapy , Drug Design , Inflammation/drug therapy , Inflammation/physiopathology , Receptors, Purinergic P2
2.
Article in Zh | WPRIM | ID: wpr-735538

ABSTRACT

Objective To investigate the occurrence of postural hypotension (PH) in patients suffering from type 2 diabetes mellitus with or without hypertension (DMH or DM), and the relationship of PH and diabetic neuropathy, hyperinsulinemia and insulin resistance. Methods A total of 30 cases of type 2 DM and 30 cases of DMH were included in this study. The blood pressure of all subjects were measured in supine and standing body positions respectively and PH was defined as a decline from supine to standing was ≥20 mmHg in systolic blood pressures (SBP). The concentrations of blood glucose and plasma insulin were measured to calculate the insulin sensitive index (ISI). Autonomic and peripheral function was determined by measuring the postural heart rates and the conduction speeds of superficial peroneal and communicating branch of peroneal nerves etc respectively. Results Significant difference (P<0.01) was found in the occurrence of PH in the patients with DM (40%) and those with DMH (67%). The changes of postural blood pressure were more obvious in those with DM+PH and DMH+PH than in those with simple DM (P<0.01). The conduction speeds of newes were significantly lower in those with DMH+PH than with simple DM (P<0.05), but the occurrence of autonomic neuropathy had no difference between the 2 groups. There was no difference in postural heart rate, body mass index and blood glucose levels in fasting and 2 h after meal among the DM, DM+PH and DMH+PH groups. The concentrations of plasma insulin of those with DMH+PH were significantly higher, but their ISI significantly lower than those of the patients with DM respectively (P<0.01). The decline of postural SBP in patients with DMH+PH had a significantly positive correlation with their plasma insulin levels in fasting condition (r=0.689, P<0.01). Conclusion The patients with DMH are more prone to PH compared with those only with DM and PH damages their peripheral nerves. Most of diabetic patients with PH suffer from obvious IR and hyperinsulinemia, and if with hypertension, the above metabolic disturbances are more severe.

3.
Article in Zh | WPRIM | ID: wpr-737006

ABSTRACT

Objective To investigate the occurrence of postural hypotension (PH) in patients suffering from type 2 diabetes mellitus with or without hypertension (DMH or DM), and the relationship of PH and diabetic neuropathy, hyperinsulinemia and insulin resistance. Methods A total of 30 cases of type 2 DM and 30 cases of DMH were included in this study. The blood pressure of all subjects were measured in supine and standing body positions respectively and PH was defined as a decline from supine to standing was ≥20 mmHg in systolic blood pressures (SBP). The concentrations of blood glucose and plasma insulin were measured to calculate the insulin sensitive index (ISI). Autonomic and peripheral function was determined by measuring the postural heart rates and the conduction speeds of superficial peroneal and communicating branch of peroneal nerves etc respectively. Results Significant difference (P<0.01) was found in the occurrence of PH in the patients with DM (40%) and those with DMH (67%). The changes of postural blood pressure were more obvious in those with DM+PH and DMH+PH than in those with simple DM (P<0.01). The conduction speeds of newes were significantly lower in those with DMH+PH than with simple DM (P<0.05), but the occurrence of autonomic neuropathy had no difference between the 2 groups. There was no difference in postural heart rate, body mass index and blood glucose levels in fasting and 2 h after meal among the DM, DM+PH and DMH+PH groups. The concentrations of plasma insulin of those with DMH+PH were significantly higher, but their ISI significantly lower than those of the patients with DM respectively (P<0.01). The decline of postural SBP in patients with DMH+PH had a significantly positive correlation with their plasma insulin levels in fasting condition (r=0.689, P<0.01). Conclusion The patients with DMH are more prone to PH compared with those only with DM and PH damages their peripheral nerves. Most of diabetic patients with PH suffer from obvious IR and hyperinsulinemia, and if with hypertension, the above metabolic disturbances are more severe.

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