دورية أكاديمية
أعرض في EDS

Nicotinic Acetylcholine Receptor Partial Antagonist Polyamides from Tunicates and Their Predatory Sea Slugs.

التفاصيل البيبلوغرافية
العنوان: Nicotinic Acetylcholine Receptor Partial Antagonist Polyamides from Tunicates and Their Predatory Sea Slugs.
المؤلفون: Paguigan ND; Department of Medicinal Chemistry, University of Utah, Salt Lake City, Utah 84112, United States., Tun JO; School of Biological Sciences, University of Utah, Salt Lake City, Utah 84112, United States., Leavitt LS; School of Biological Sciences, University of Utah, Salt Lake City, Utah 84112, United States., Lin Z; Department of Medicinal Chemistry, University of Utah, Salt Lake City, Utah 84112, United States., Chase K; School of Biological Sciences, University of Utah, Salt Lake City, Utah 84112, United States., Dowell C; School of Biological Sciences, University of Utah, Salt Lake City, Utah 84112, United States., Deering-Rice CE; Department of Pharmacology and Toxicology, University of Utah, Salt Lake City, Utah 84112, United States., Lim AL; Department of Medicinal Chemistry, University of Utah, Salt Lake City, Utah 84112, United States., Karthikeyan M; School of Biological Sciences, University of Utah, Salt Lake City, Utah 84112, United States., Hughen RW; Department of Anesthesiology, School of Medicine, University of Utah, Salt Lake City, Utah 84112, United States., Zhang J; Department of Anesthesiology, School of Medicine, University of Utah, Salt Lake City, Utah 84112, United States., Peterson RT; Department of Pharmacology and Toxicology, University of Utah, Salt Lake City, Utah 84112, United States., Reilly CA; Department of Pharmacology and Toxicology, University of Utah, Salt Lake City, Utah 84112, United States., Light AR; Department of Anesthesiology, School of Medicine, University of Utah, Salt Lake City, Utah 84112, United States., Raghuraman S; School of Biological Sciences, University of Utah, Salt Lake City, Utah 84112, United States., McIntosh JM; Department of Psychiatry, and School of Biological Sciences, University of Utah, Salt Lake City, Utah 84112, United States.; George E Whalen Veterans Affairs Medical Center, Salt Lake City, Utah 84148, United States., Olivera BM; School of Biological Sciences, University of Utah, Salt Lake City, Utah 84112, United States., Schmidt EW; Department of Medicinal Chemistry, University of Utah, Salt Lake City, Utah 84112, United States.
المصدر: ACS chemical neuroscience [ACS Chem Neurosci] 2021 Jul 21; Vol. 12 (14), pp. 2693-2704. Date of Electronic Publication: 2021 Jul 02.
نوع المنشور: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.
اللغة: English
بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101525337 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1948-7193 (Electronic) Linking ISSN: 19487193 NLM ISO Abbreviation: ACS Chem Neurosci Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Washington, D.C. : American Chemical Society
مواضيع طبية MeSH: Receptors, Nicotinic* , Urochordata*, Animals ; Aplysia ; Mice ; Nicotinic Antagonists/pharmacology ; Nylons ; Rats ; alpha7 Nicotinic Acetylcholine Receptor
مستخلص: In our efforts to discover new drugs to treat pain, we identified molleamines A-E ( 1 - 5 ) as major neuroactive components of the sea slug, Pleurobranchus forskalii , and their prey, Didemnum molle , tunicates. The chemical structures of molleamines were elucidated by spectroscopy and confirmed by the total synthesis of molleamines A ( 1 ) and C ( 3 ). Synthetic 3 completely blocked acetylcholine-induced calcium flux in peptidergic nociceptors (PNs) in the somatosensory nervous system. Compound 3 affected neither the α7 nAChR nor the muscarinic acetylcholine receptors in calcium flux assays. In addition to nociceptors, 3 partially blocked the acetylcholine-induced calcium flux in the sympathetic nervous system, including neurons from the superior cervical ganglion. Electrophysiology revealed a block of α3β4 (mouse) and α6/α3β4 (rat) nicotinic acetylcholine receptors (nAChRs), with IC 50 values of 1.4 and 3.1 μM, respectively. Molleamine C ( 3 ) is a partial antagonist, reaching a maximum block of 76-82% of the acetylcholine signal and showing no partial agonist response. Molleamine C ( 3 ) may thus provide a lead compound for the development of neuroactive compounds with unique biological properties.
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معلومات مُعتمدة: R35 GM122521 United States GM NIGMS NIH HHS; R35 GM136430 United States GM NIGMS NIH HHS
فهرسة مساهمة: Keywords: Polyamide; molleamine; mollecarbamate; molleurea; nicotinic acetylcholine receptors
المشرفين على المادة: 0 (Nicotinic Antagonists)
0 (Nylons)
0 (Receptors, Nicotinic)
0 (alpha7 Nicotinic Acetylcholine Receptor)
تواريخ الأحداث: Date Created: 20210702 Date Completed: 20210802 Latest Revision: 20220722
رمز التحديث: 20240628
مُعرف محوري في PubMed: PMC8487611
DOI: 10.1021/acschemneuro.1c00345
PMID: 34213884
قاعدة البيانات: MEDLINE
الوصف
تدمد:1948-7193
DOI:10.1021/acschemneuro.1c00345