786592-95-8
Chemical Structure
Oxprenoate
Synonym(s): RU 28318 free base
- CAS No.: 786592-95-8
- Formula:C25H38O4
- Molecular Weight:402.58
IUPAC Name: 3-((7R,8R,9S,10R,13S,14S,17R)-17-hydroxy-10,13-dimethyl-3-oxo-7-propyl-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)propanoic acid
InChIKey: DNHCHRGCTVRAFT-JEHIOXJOSA-N
SMILES: C(CC)[C@H]1[C@]2([C@]3([C@@](C)([C@@](CCC(O)=O)(O)CC3)CC[C@@]2([C@]4(C)C(C1)=CC(=O)CC4)[H])[H])[H]
Biological Activity: Oxprenoate (RU 28318 (free base)) is an orally active, brain-penetrant selective mineralocorticoid receptor antagonist that blocks Aldosterone (HY-113313) signaling through competitive binding to MR, and exhibits anxiolytic and neuroprotective activities, as well as modulates Corticosterone (HY-B1618) levels. Oxprenoate is used in research on hypertension, anxiety disorders, depression, Alzheimer's disease, and glucocorticoid-related neuronal injury[1][2][3][4][5][6][7][8][9][10].
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Oxprenoate | Oxprenoate (RU 28318 (free base)) is an orally active, brain-penetrant selective mineralocorticoid receptor antagonist that blocks Aldosterone (HY-113313) signaling through competitive binding to MR, and exhibits anxiolytic and neuroprotective activities, as well as modulates Corticosterone (HY-B1618) levels. Oxprenoate is used in research on hypertension, anxiety disorders, depression, Alzheimer's disease, and glucocorticoid-related neuronal injury. | |||||||||||||||||||||
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References
- [1]. Pavlides C, et al. Opposing roles of type I and type II adrenal steroid receptors in hippocampal long-term potentiation. Neuroscience. 1995 Sep;68(2):387-94.
- [2]. Bitran D, et al. Corticosterone is permissive to the anxiolytic effect that results from the blockade of hippocampal mineralocorticoid receptors. Pharmacology, biochemistry, and behavior. 1998 Aug;60(4):879-87.
- [3]. Jadavji NM, et al. Blockade of mineralocorticoid and glucocorticoid receptors reverses stress-induced motor impairments. Neuroendocrinology. 2011;94(4):278-90.
- [4]. Lazarovici P. Dexamethasone-induced down-regulation of nerve growth factor receptor p75NTR is mediated by glucocorticoid type II receptor in PC12 cell model[J]. The Open Pharmacology Journal, 2007.
- [5]. Fahlke C, et al. Consequence of long-term exposure to corticosterone or dexamethasone on ethanol consumption in the adrenalectomized rat, and the effect of type I and type II corticosteroid receptor antagonists. Psychopharmacology. 1995 Jan;117(2):216-24.
- [6]. Morris MJ, et al. Mineralocorticoid receptor antagonism prevents hedonic deficits induced by a chronic sodium appetite. Behavioral neuroscience. 2010 Apr;124(2):211-24.
- [7]. Alexandre J, et al. Rapid and MR-Independent IK1 Activation by Aldosterone during Ischemia-Reperfusion. PloS one. 2015;10(7):e0132592.
- [8]. Mills NJ, et al. Aldosterone Mediated Regulation of Epithelial Sodium Channel (ENaC) Subunits in the Rat Hypothalamus. Neuroscience. 2018 Oct 15;390:278-292.
- [9]. Moura AM, et al. Direct action of aldosterone on transmembrane 22Na efflux from arterial smooth muscle. Rapid and delayed effects. Hypertension. 1984 May-Jun;6(3):425-30.
- [10]. Calvo N, et al. Glucocorticoid and mineralocorticoid receptors are involved in the facilitation of anxiety-like response induced by restraint. Neuroendocrinology. 2001 Apr;73(4):261-71.
