N1H- and N1-Substituted Phenylguanidines as α7 Nicotinic Acetylcholine (nACh) Receptor Antagonists: Structure–Activity Relationship Studies

Autor: Osama I. Alwassil, Marvin K. Schulte, Sanjay S Aripaka, Malgorzata Dukat, Jens D. Mikkelsen, Shailesh Khatri

Publikováno v: ACS Chemical Neuroscience. 12:2194-2201

We previously reported that N-(3-chlorophenyl)guanidine (1) represents a novel α7 nicotinic ACh (nACh) receptor antagonist chemotype. In the present study, a small series of compounds was synthesized with the intent to investigate the structure-acti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fe04bcc6a96b6d5445dc8eddf06741ca
https://doi.org/10.1021/acschemneuro.1c00212

Direction of action of presynaptic GABAA receptors is highly dependent on the level of receptor activation

Autor: Wan-Chen Wu, Ying Yang, Jason R. Pugh, Shailesh Khatri

Publikováno v: Journal of Neurophysiology. 121:1896-1905

Many synapses, including parallel fiber synapses in the cerebellum, express presynaptic GABAA receptors. However, reports of the functional consequences of presynaptic GABAA receptor activation are variable across synapses, from inhibition to enhance

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f5067c1234f8323e9051f05f44bb2a07
https://doi.org/10.1152/jn.00779.2018

Allosterism of Nicotinic Acetylcholine Receptors: Therapeutic Potential for Neuroinflammation Underlying Brain Trauma and Degenerative Disorders

Autor: Shailesh Khatri, Abel Bult-Ito, Swarup Mitra, Malabika Maulik, Marvin K. Schulte

Publikováno v: International Journal of Molecular Sciences
International Journal of Molecular Sciences, Vol 21, Iss 4918, p 4918 (2020)

Inflammation is a key physiological phenomenon that can be pervasive when dysregulated. Persistent chronic inflammation precedes several pathophysiological conditions forming one of the critical cellular homeostatic checkpoints. With a steady global

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9d864531d86b486fe30069445aa561e
https://pubmed.ncbi.nlm.nih.gov/32664647

Rabies virus modifies host behaviour through a snake-toxin like region of its glycoprotein that inhibits neurotransmitter receptors in the CNS

Autor: Shailesh Khatri, Shane Alexander Rideout, Marvin K. Schulte, Michael E. Harris, Clare Stokes, Roger L. Papke, Karsten Hueffer

Publikováno v: Scientific Reports, Vol 7, Iss 1, Pp 1-8 (2017)
Scientific Reports

Rabies virus induces drastic behaviour modifications in infected hosts. The mechanisms used to achieve these changes in the host are not known. The main finding of this study is that a region in the rabies virus glycoprotein, with homologies to snake

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de42b9f64bd25d8eb58152a58a822e23
http://link.springer.com/article/10.1038/s41598-017-12726-4

Superagonist, Full Agonist, Partial Agonist, and Antagonist Actions of Arylguanidines at 5-Hydroxytryptamine-3 (5-HT3) Subunit A Receptors

Autor: Michael M. White, Heather L. Nyce, Katie Alix, Marvin K. Schulte, Malgorzata Dukat, Samantha Casterlow, Shailesh Khatri, Philip D. Mosier, Dong Yan

Publikováno v: ACS Chemical Neuroscience. 7:1565-1574

Introduction of minor variations to the substitution pattern of arylguanidine 5-hydroxytryptamine-3 (5-HT3) receptor ligands resulted in a broad spectrum of functionally-active ligands from antagonist to superagonist. For example, (i) introduction of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::18d73945b1a8ffbc3798d0f736db6730
https://doi.org/10.1021/acschemneuro.6b00196