The use of drugs interfering with somatostatin receptors (ssR) is now consolidated practice in diagnostics and therapy, stimulating the development of new and more efficient molecules offering improved pharmacodynamics. Over the years, we have passed from the use of native somatostatin to mini-somatostatin and then octapeptides, above all octreotide. Subsequently, peptides were synthesized with specific affinities for a single receptorial subtype, like compound BIM23268 and compound CH275. More recently, somatostatin analogs were synthesized with a non-peptide structure. Another important aspect in the history of sst analogs is represented by the development of new pharmaceutical formulas for these drugs in order to improve patient compliance by reducing dose frequency.
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Ther Adv Med Oncol
November 2024
Hôpital Edouard Herriot, Lyon, France.
Background: Sunitinib, a multitarget tyrosine kinase inhibitor, showed encouraging antitumor activity and manageable toxicity in patients with advanced midgut neuroendocrine tumors (NETs) in earlier results from phase I and II trials.
Patients And Methods: In this phase II trial, patients with a nonresectable grade 1 or 2 midgut progressive NET and Eastern Cooperative Oncology Group performance status 0-1 were randomly assigned 1:1 to receive 37.5 mg sunitinib or a placebo, combined with 120 mg lanreotide autogel every 28 days.
iScience
October 2024
NMPA Key Laboratory for Research and Evaluation of Narcotic and Psychotropic Drugs, Xuzhou 221002, Jiangsu, China.
Somatostatin (SOM)-expressing neurons in the central lateral amygdala (CeL) are responsible for fear memory learning, but the circuit and molecular mechanisms underlying this biology remain elusive. Here, we found that glutamatergic neurons in the lateral parabrachial nucleus (LPB) directly dominated the activity of CeL neurons, and that selectively inhibiting the LPB→CeL pathway suppressed fear memory acquisition. By contrast, inhibiting CeL-projecting glutamatergic neurons in the paraventricular thalamic nucleus (PVT) interfered with consolidation-related processes.
View Article and Find Full Text PDFSci Rep
September 2024
Department of Biophysics and Neuroscience, Wroclaw Medical University, 3a Chalubinskiego Str., 50-368, Wroclaw, Poland.
Schizophr Res
May 2024
Department of Pharmacology and Center for Biomedical Neuroscience, University of Texas Health Science Center, San Antonio, TX 78229, USA; South Texas Veterans Health Care System, Audie L. Murphy Division, San Antonio, USA.
A decreased expression of specific interneuron subtypes, containing either the calcium binding protein parvalbumin (PV) or the neurotransmitter somatostatin (SST), are observed in the cortex and hippocampus of both patients with schizophrenia and rodent models used to study the disorder. Moreover, preclinical studies suggest that this loss of inhibitory function is a key pathological mechanism underlying the symptoms of schizophrenia. Interestingly, decreased expression of Lhx6, a key transcriptional regulator specific to the development and migration of PV and SST interneurons, is seen in human postmortem studies and following multiple developmental disruptions used to model schizophrenia preclinically.
View Article and Find Full Text PDFDev Neurobiol
January 2024
Department of Cellular and Molecular Neuropathology, Juntendo University Graduate School of Medicine, Tokyo, Japan.
Transient expression of somatostatin (SST) has been observed in the olfactory epithelium (OE) and nerves of chick embryos. Intense expression of SST in these regions on embryonic days (E) 5-8 coincides with the migration of neurons producing gonadotropin-releasing hormone (GnRH) from the OE to the forebrain (FB), suggesting that SST plays a role in the development of GnRH neurons. Using in ovo electroporation of small interfering RNA, we found that the suppression of SST mRNA in the olfactory placode (OP) of E3.
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