PRE-084: Difference between revisions

PRE-084
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number	140376-53-4
PubChem	3086015
DrugBank
ChemSpider	2340985
KEGG

Latest revision as of 19:22, 22 March 2025

A sigma receptor agonist

PRE-084 is a synthetic compound that acts as a selective agonist for the sigma-1 receptor. It is primarily used in scientific research to study the role of sigma receptors in the central nervous system and their potential therapeutic applications.

Chemical Structure and Properties[edit]

PRE-084 is chemically known as 2-(4-Methoxyphenyl)-1-[2-(N-pyrrolidinyl)ethyl]-4-methyl-1H-pyrrole. It has a molecular formula of C₁₆H₂₃N₂O and a molecular weight of 259.37 g/mol. The compound features a pyrrole ring substituted with a methoxyphenyl group and a pyrrolidinyl ethyl chain.

Mechanism of Action[edit]

PRE-084 functions as an agonist at the sigma-1 receptor, a chaperone protein located in the endoplasmic reticulum of cells. The activation of sigma-1 receptors by PRE-084 modulates various cellular processes, including calcium signaling, neuroprotection, and neuroplasticity. These receptors are implicated in the regulation of ion channels, neurotransmitter release, and apoptosis.

Pharmacological Effects[edit]

Research indicates that PRE-084 exhibits neuroprotective effects, potentially offering therapeutic benefits in neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. It has been shown to enhance cognitive function and memory in animal models. Additionally, PRE-084 may have antidepressant and anxiolytic properties, making it a compound of interest in the study of mental health disorders.

Research Applications[edit]

PRE-084 is widely used in preclinical studies to explore the physiological and pathological roles of sigma-1 receptors. It serves as a tool to investigate the potential of sigma-1 receptor modulation in treating various conditions, including neuropathic pain, stroke, and schizophrenia.

Safety and Toxicity[edit]

While PRE-084 is primarily used in research settings, its safety profile in humans is not well-established. Studies in animal models suggest that it is generally well-tolerated at research doses, but further investigation is needed to determine its safety and efficacy in humans.

Related Pages[edit]

@@ Line 1: / Line 1: @@
-[[File:PRE-084_SVG_file.svg|thumb|{{PAGENAME}} structure]]
+{{Short description|A sigma receptor agonist}}
+{{Drugbox
+| verifiedfields = changed
+| verifiedrevid = 477318123
+| IUPAC_name = 2-(4-Methoxyphenyl)-1-[2-(N-pyrrolidinyl)ethyl]-4-methyl-1H-pyrrole
+| image = PRE-084_structure.png
+| image2 = PRE-084_3D_structure.png
+| width = 200
+| width2 = 200
+| CAS_number = 140376-53-4
+| PubChem = 3086015
+| ChemSpiderID = 2340985
+| UNII = 0F8K4Y6YN1
+| C=16
+| H=23
+| N=2
+| O=1
+| smiles = COC1=CC=C(C=C1)C2=C(C)C=CN2CCN3CCCC3
+}}
-'''PRE-084''' is a [[sigma receptor]] [[agonist]], selective for the [[Sigma-1 receptor|σ<sub>1</sub>]] subtype. It has [[nootropic]] and [[antidepressant]] actions in animal studies, as well as [[antitussive]] and reinforcing effects.<ref name="pmid7886099">{{cite journal |author=Maurice T, Su TP, Parish DW, Nabeshima T, Privat A |title=PRE-084, a sigma selective PCP derivative, attenuates MK-801-induced impairment of learning in mice |journal=Pharmacology, Biochemistry, and Behavior |volume=49 |issue=4 |pages=859–69 |date=December 1994 |pmid=7886099 |doi= 10.1016/0091-3057(94)90235-6|url=}}</ref><ref name="pmid11728429">{{cite journal |author=Maurice T |title=Beneficial effect of the sigma(1) receptor agonist PRE-084 against the spatial learning deficits in aged rats |journal=European Journal of Pharmacology |volume=431 |issue=2 |pages=223–7 |date=November 2001 |pmid=11728429 |doi= 10.1016/S0014-2999(01)01436-4|url=}}</ref><ref name="pmid14691051">{{cite journal |author=Brown C, Fezoui M, Selig WM, Schwartz CE, Ellis JL |title=Antitussive activity of sigma-1 receptor agonists in the guinea-pig |journal=[[British Journal of Pharmacology]] |volume=141 |issue=2 |pages=233–40 |date=January 2004 |pmid=14691051 |pmc=1574192 |doi=10.1038/sj.bjp.0705605 |url=}}</ref><ref name="pmid20081254">{{cite journal |author=Skuza G, Rogóz Z |title=Antidepressant-like effect of PRE-084, a selective sigma1 receptor agonist, in Albino Swiss and C57BL/6J mice |journal=Pharmacological Reports : PR |volume=61 |issue=6 |pages=1179–83 |year=2009 |pmid=20081254 |doi= |url=}}</ref><ref name="pmid19892920">{{cite journal |author=Hiranita T, Soto PL, Tanda G, Katz JL |title=Reinforcing effects of sigma-receptor agonists in rats trained to self-administer cocaine |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=332 |issue=2 |pages=515–24 |date=February 2010 |pmid=19892920 |doi=10.1124/jpet.109.159236 |url= |pmc=2812106}}</ref> PRE-084 increases the expression of [[GDNF]].<ref>{{cite journal | doi = 10.1089/neu.2010.1674 | pmid = 21332255 | volume=28 | issue=5 | title=Sigma receptor agonist 2-(4-morpholinethyl)1 phenylcyclohexanecarboxylate (Pre084) increases GDNF and BiP expression and promotes neuroprotection after root avulsion injury |date=May 2011 | journal=J. Neurotrauma | pages=831–40 | author=Penas C, Pascual-Font A, Mancuso R, For&eacute;s J, Casas C, Navarro X}}</ref>
+'''PRE-084''' is a synthetic compound that acts as a selective agonist for the [[sigma-1 receptor]]. It is primarily used in scientific research to study the role of sigma receptors in the [[central nervous system]] and their potential therapeutic applications.
-==References==
+==Chemical Structure and Properties==
-{{reflist}}
+PRE-084 is chemically known as 2-(4-Methoxyphenyl)-1-[2-(N-pyrrolidinyl)ethyl]-4-methyl-1H-pyrrole. It has a molecular formula of C<sub>16</sub>H<sub>23</sub>N<sub>2</sub>O and a molecular weight of 259.37 g/mol. The compound features a pyrrole ring substituted with a methoxyphenyl group and a pyrrolidinyl ethyl chain.
-{{Sigmaergics}}
+==Mechanism of Action==
+PRE-084 functions as an agonist at the [[sigma-1 receptor]], a chaperone protein located in the [[endoplasmic reticulum]] of cells. The activation of sigma-1 receptors by PRE-084 modulates various cellular processes, including calcium signaling, [[neuroprotection]], and [[neuroplasticity]]. These receptors are implicated in the regulation of [[ion channels]], [[neurotransmitter]] release, and [[apoptosis]].
-[[Category:Sigma agonists]]
+==Pharmacological Effects==
-[[Category:Carboxylate esters]]
+Research indicates that PRE-084 exhibits neuroprotective effects, potentially offering therapeutic benefits in [[neurodegenerative diseases]] such as [[Alzheimer's disease]] and [[Parkinson's disease]]. It has been shown to enhance [[cognitive function]] and memory in animal models. Additionally, PRE-084 may have [[antidepressant]] and [[anxiolytic]] properties, making it a compound of interest in the study of [[mental health]] disorders.
-[[Category:Morpholines]]
-{{pharm-stub}}
+==Research Applications==
+PRE-084 is widely used in preclinical studies to explore the physiological and pathological roles of sigma-1 receptors. It serves as a tool to investigate the potential of sigma-1 receptor modulation in treating various conditions, including [[neuropathic pain]], [[stroke]], and [[schizophrenia]].
+==Safety and Toxicity==
+While PRE-084 is primarily used in research settings, its safety profile in humans is not well-established. Studies in animal models suggest that it is generally well-tolerated at research doses, but further investigation is needed to determine its safety and efficacy in humans.
+==Related Pages==
+* [[Sigma-1 receptor]]
+* [[Neuroprotection]]
+* [[Neurodegenerative diseases]]
+* [[Cognitive function]]
+[[Category:Sigma receptor agonists]]
+[[Category:Research chemicals]]
+[[Category:Neuropharmacology]]