Results 11 to 20 of about 1,394 (176)

Evaluation of In-Batch and In-Flow Synthetic Strategies towards the Stereoselective Synthesis of a Fluorinated Analogue of Retro-Thiorphan

Molecules, 2019
A stereoselective synthetic strategy for the preparation of trifluoromethylamine mimics of retro-thiorphan, involving a diastereoselective, metal-free catalytic step, has been studied in batch and afforded the target molecule in good yields and high ...
Margherita Pirola, Alessandra Puglisi, Laura Raimondi, Alessandra Forni, Maurizio Benaglia   +4 more
doaj   +3 more sources

Thiorphan, a neutral endopeptidase inhibitor used for diarrhoea, is neuroprotective in newborn mice [PDF]

Brain, 2006
Excitotoxic damage appears to be a critical factor in the formation of perinatal brain lesions associated with cerebral palsy (CP). When injected into newborn mice, the glutamatergic analogue, ibotenate, produces cortical lesions and white matter cysts that mimic human perinatal brain lesions.
Medja, Fadia, Lelièvre, Vincent, Fontaine, Romain H, Lebas, Fanny, Leroux, Philippe, Ouimet, Tanja, Saria, Alois, Rougeot, Catherine, Dournaud, Pascal, Gressens, Pierre   +9 more
openaire   +4 more sources

Polarization Controlled Assembly of Ultrathin Thiorphan Nanostructures on ZnO Surface Facets

Langmuir, 2023
Despite the importance of thiorphan as a small molecule with vital biological roles, its interactions with zinc oxide (ZnO) nanomaterials that are prospective in drug delivery and theranostic applications have not yet been sufficiently explored.
Egor Ukraintsev, Hadi Hematian, Bohuslav Rezek   +2 more
openaire   +3 more sources

Thiorphan, tiopronin, and related analogs as substrates and inhibitors of peptidylglycine α‐amidating monooxygenase (PAM) [PDF]

FEBS Letters, 2005
Peptidyglycine α‐amidating monooxygenase is a copper‐ and zinc‐dependent, bifunctional enzyme that catalyzes the cleavage of glycine‐extended peptides or N‐acylglycines to the corresponding amides and glyoxylate. This reaction is a key step in the biosynthesis of bioactive α‐amidated peptides and, perhaps, the primary fatty acids amides also.
McIntyre, Neil R., Lowe, Edward W., Chew, Geoffrey H., Owen, Terrence C., Merkler, David J.   +4 more
openaire   +3 more sources

Substance P-induced effects in guinea pig lungs: effects of thiorphan and captopril

Journal of Applied Physiology, 1989
The effects of the neutral metalloendopeptidase inhibitor, thiorphan, and the angiotensin-converting enzyme inhibitor, captopril, on the changes in airway opening pressure (PaO), pulmonary arterial pressure (Ppa), and weight induced by intravascular administration of substance P were examined in isolated perfused and ventilated guinea pig lungs ...
J M, Drazen, S A, Shore, N P, Gerard
openaire   +3 more sources

Contribution of ANP to plasma protein escape during VE: effects of thiorphan and atrial appendectomy

American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, 1996
The effects of endopeptidase inhibition and right atrial appendectomy (AA) on plasma immunoreactive atrial natriuretic peptide (irANP) concentrations and extravascular accumulation of 131I-labeled bovine serum albumin (CBSA) during volume expansion (VE) were examined in pentobarbital sodium-anesthetized rats (n = 5 per group).
V. L. Tucker
openaire   +3 more sources

Pharmacophore-Based Identification and Molecular Characterization of Potent Neprilysin Inhibitors: Biochemical and Therapeutic Implications for Cardiovascular Diseases. [PDF]

Chem Biol Drug Des
Pharmacophore‐based virtual screening and molecular dynamics identified pentagalloylglucose and tannic acid as potent, non‐toxic neprilysin inhibitors. These natural compounds demonstrated strong binding affinity and stable interactions with the catalytic Zn2+ site, offering promising leads for cardiovascular drug development. ABSTRACT Neprilysin (NEP),
Kuo CT, Wu YC, Li JM, Ju TC, Tseng TS.
europepmc   +2 more sources

Acute Inhibition of Intestinal Neprilysin Enhances Insulin Secretion via GLP-1 Receptor Signaling in Male Mice. [PDF]

Endocrinology, 2023
peer reviewedThe peptidase neprilysin modulates glucose homeostasis by cleaving and inactivating insulinotropic peptides, including some produced in the intestine such as glucagon-like peptide-1 (GLP-1).
Esser N, Mundinger TO, Barrow BM, Zraika S.   +3 more
europepmc   +2 more sources

Thiorphan reprograms neurons to promote functional recovery after spinal cord injury. [PDF]

Nature
Abstract We previously identified an embryonic shift in the corticospinal motor neuronal transcriptome after spinal cord injury associated with successful axonal regeneration 1 .
van Niekerk EA, de Freria CM, Mancarci BO, Groeniger K, Kulinich D, Riley T, Kawaguchi R, Okawa S, Vokes T, Rosenzweig ES, Sinopoulou E, Castle MJ, Huie R, Ferguson AR, Kfoury-Beaumont N, Khalessi A, Pavlidis P, Tuszynski MH.   +17 more
europepmc   +3 more sources

Concomitant medication in patients with bradykinin‐mediated angioedema – there's more than ACE inhibitors

JDDG: Journal der Deutschen Dermatologischen Gesellschaft, Volume 21, Issue 11, Page 1283-1289, November 2023., 2023
Summary Bradykinin‐mediated angioedema is a rare, non‐allergic, potentially life‐threatening disease. ACE inhibitor‐induced angioedema and hereditary angioedema (HAE) are the two most common presentations. Therapeutic options, pathophysiology and diagnosis continue to be investigated, with considerable progress in HAE over the last few decades. For all
Robin Lochbaum, Thomas K. Hoffmann, Jens Greve, Janina Hahn   +3 more
wiley   +1 more source