scholarly journals Small Molecule Drugs for Treatment of Alzheimer’s Diseases Developed on the Basis of Mechanistic Understanding of the Serotonin Receptors 4 and 6

2021 ◽  
Author(s):  
Charlotte Uldahl Jansen ◽  
Katrine M. Qvortrup
Keyword(s):  
Small Molecule ◽  
Serotonin Receptors ◽  
Medicinal Chemistry ◽  
Neurotransmitter System ◽  
Biological Targets ◽  
System A ◽  
Small Molecule Drugs ◽  
Promising Target ◽  
Disease Modifying ◽  
Number Of Publications

Alzheimer’s disease (AD) is the most common form of dementia affecting millions of people worldwide and currently, the only possible treatment is the use of symptomatic drugs. Therefore, there is a need for new and disease-modifying approaches. Among the numbers of biological targets which are today explored in order to prevent or limit the progression of AD, the modulation of serotonin receptors the subtype 4 and 6 receptors (5-HT4R and 5-HT6R) has received increasing attention and has become a promising target for improving cognition and limit the amyloid pathology through modulation of the neurotransmitter system. A large number of publications describing the development of ligands for these serotonin receptors have emerged, and their pharmaceutical potential is now quite evident. However, 5-HT4R and 5-HT6R functionality is much more complex than initially defined. This chapter describes recent advances in the understanding of this modulation as well as the medicinal chemistry efforts towards development of selective 5-HT4R or 5-HT6R ligands.

Syntheses and Medicinal Chemistry of Azepinoindolones: A Look Back to Leap Forward

2021 ◽  
Author(s):  
Manasa Kadagathur ◽  
Neelima D. Tangellamudi ◽  
Dilep Kumar Sigalapalli ◽  
Shankaraiah Nagula ◽  
Sandip Patra
Keyword(s):  
Small Molecule ◽  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Heterocyclic Ring ◽  
Ring Structure ◽  
Small Molecule Drugs ◽  
Look Back

Nearly 75% of small-molecule drugs contain N-based heterocyclic ring structure. Among the heterocyclic compounds, indole-fused azepine, termed as azepinoindolone, has come under the radar of medicinal chemists since past few...

scholarly journals Cyclodextrin-Based Supramolecular Complexes of Osteoinductive Agents for Dental Tissue Regeneration

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 136
Author(s):  
Masahiko Terauchi ◽  
Atsushi Tamura ◽  
Yoshinori Arisaka ◽  
Hiroki Masuda ◽  
Tetsuya Yoda ◽  
...  
Keyword(s):  
Growth Factors ◽  
Bone Formation ◽  
Small Molecule ◽  
Tissue Regeneration ◽  
Alveolar Bone ◽  
Inclusion Complexation ◽  
Dental Tissue ◽  
Polyelectrolyte Complexes ◽  
Small Molecule Drugs

Oral tissue regeneration has received growing attention for improving the quality of life of patients. Regeneration of oral tissues such as alveolar bone and widely defected bone has been extensively investigated, including regenerative treatment of oral tissues using therapeutic cells and growth factors. Additionally, small-molecule drugs that promote bone formation have been identified and tested as new regenerative treatment. However, treatments need to progress to realize successful regeneration of oral functions. In this review, we describe recent progress in development of regenerative treatment of oral tissues. In particular, we focus on cyclodextrin (CD)-based pharmaceutics and polyelectrolyte complexation of growth factors to enhance their solubility, stability, and bioactivity. CDs can encapsulate hydrophobic small-molecule drugs into their cavities, resulting in inclusion complexes. The inclusion complexation of osteoinductive small-molecule drugs improves solubility of the drugs in aqueous solutions and increases in vitro osteogenic differentiation efficiency. Additionally, various anionic polymers such as heparin and its mimetic polymers have been developed to improve stability and bioactivity of growth factors. These polymers protect growth factors from deactivation and degradation by complex formation through electrostatic interaction, leading to potentiation of bone formation ability. These approaches using an inclusion complex and polyelectrolyte complexes have great potential in the regeneration of oral tissues.

scholarly journals Bioanalysis of small-molecule drugs in nasal and paranasal tissues and secretions: Current status and perspectives

2012 ◽  
Vol 10 (3) ◽  
pp. 686-702
Author(s):  
Ana Serralheiro ◽  
Gilberto Alves ◽  
Amílcar Falcão
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Small Molecule ◽  
Intranasal Administration ◽  
Quantitative Measurement ◽  
Current Status ◽  
Small Molecule Drugs ◽  
Development And Validation ◽  
Liquid Chromatographic

AbstractOver the last years, interest in intranasal administration as an alternative and promising route for the delivery of drugs withlocal, systemic, and even central nervous system action has tremendously increased. Accordingly, understanding of the propertiesand characteristics of the nasal cavity as well as the biodisposition processes of drugs into the nasal compartments is acquiringa significant prominence in the field of pharmacology. In this context, the development and validation of bioanalytical methodologies for the quantitative measurement of drugs and their metabolites in nasal and paranasal tissues and/or secretions is of the utmostimportance. However, currently, information concerning bioanalysis of drugs in nasal and paranasal tissues and/or secretionsis scattered. This review aims to provide a valuable overview of the methodologies that have been used for the collectionand preparation of nasal and paranasal samples with special emphasis placed on the review of liquid chromatographic methodsemployed for the quantitative determination of small-molecule drugs and their metabolites in such specimens.

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