Provided herein are novel ergoline compounds as 5-HT2A agonists, pharmaceutical compositions, use of such compounds in treating mood disorders such as depressive disorders and bipolar disorders, and processes for preparing such compounds.
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http://dx.doi.org/10.1021/acsmedchemlett.4c00593 | DOI Listing |
Cephalalgia
January 2025
Department of Pharmacology, University of Arizona College of Medicine, Tucson, AZ, USA.
Background: Women with endometriosis are more likely to have migraine. The mechanisms underlying this co-morbidity are unknown. Prolactin, a neurohormone secreted and released into circulation from the anterior pituitary, can sensitize sensory neurons from female, but not male, rodents, monkeys and human donors.
View Article and Find Full Text PDFACS Med Chem Lett
January 2025
Smith, Gambrell & Russell LLP, 1105 W. Peachtree Street NE, Suite 1000, Atlanta, Georgia 30309, United States.
Provided herein are novel ergoline compounds as 5-HT2A agonists, pharmaceutical compositions, use of such compounds in treating mood disorders such as depressive disorders and bipolar disorders, and processes for preparing such compounds.
View Article and Find Full Text PDFACS Med Chem Lett
January 2025
Usona Institute, Fitchburg, Wisconsin 53711-5300, United States.
Recent advancements in pharmaceutical research have focused on developing novel psychoactive compounds and receptor modulators that enhance therapeutic outcomes while minimizing adverse effects. This Patent Highlight examines three innovative approaches: (1) transmucosal delivery of dephosphorylated psychoactive alkaloids, (2) nonhallucinogenic serotonin receptor modulators, and (3) ergoline analogues designed for treating neurological disorders. These innovations offer breakthroughs in drug delivery, receptor targeting, and structural modifications, aiming to address challenges in the treatment of mood disorders, neurological diseases, and chronic pain while improving bioavailability and reducing side effects and hallucinogenic properties.
View Article and Find Full Text PDFZhong Nan Da Xue Xue Bao Yi Xue Ban
July 2024
Department of Endocrinology &Metabolism, West China Hospital, Sichuan University, Chengdu 610041.
Cushing's disease is a rare endocrine disorder characterized by hypercortisolism. Chronic elevated cortisol levels can lead to dysfunction or complications in multiple organs of systems, including cardiovascular, glucose, and bone metabolism, severely impacting patients' quality of life and posing life-threatening risks. Surgery is the first-line treatment for Cushing's disease.
View Article and Find Full Text PDFInt J Pharm
January 2025
Department of Pharmaceutics, School of Pharmacy, Harbin Medical University, Harbin, Heilongjiang 150086, China. Electronic address:
Parkinson's disease confronts challenges in drug delivery due to the blood-brain barrier. Intranasal delivery bypasses the blood-brain barrier for improved drug bioavailability, yet narrow nasal space and brief retention time hinder clinical applicability. We conducted a Bromocriptine Mesylate-loaded PLGA nanoparticles co-modified with low molecular weight protamine (LMWP) and lactoferrin (Lf) (LMWP/Lf-BCM-NPs) for nose-to-brain delivery.
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