PF-04455242: Difference between revisions

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{{DISPLAYTITLE:PF-04455242}}
{{Short description|Investigational drug}}
{{Drugbox
| verifiedfields = changed
| verifiedrevid = 477318123
| IUPAC_name = 1-(4-fluorophenyl)-3-((4-((2-methylpyrimidin-4-yl)oxy)piperidin-1-yl)methyl)urea
| image = PF-4455242.svg
| image_size = 200px
| image_alt = Chemical structure of PF-04455242
| width =
| alt =
| CAS_number = 956905-27-4
| PubChem = 16005106
| ChemSpiderID = 13180813
| UNII = 0F3X4Q3XUS
| KEGG = D09992
| ChEMBL = 2103874
| C=18
| H=23
| F=1
| N=4
| O=1
| smiles = CC1=NC=NC(=C1)OC2CCN(CC2)CNC(=O)NC3=CC=C(C=C3)F
| StdInChI = 1S/C18H23FN4O2/c1-13-21-9-10-22-18(13)25-16-7-5-15(6-8-16)23-11-14(24)20-17-3-2-4-19-12-17/h2-4,5-10,12,14H,11H2,1H3,(H,20,24)
| StdInChIKey = ZQKZQXJZQXJZQX-UHFFFAOYSA-N
}}


== Overview ==
'''PF-04455242''' is an investigational drug that was developed by [[Pfizer]] for the treatment of [[cognitive disorders]] such as [[schizophrenia]] and [[Alzheimer's disease]]. It acts as a selective [[dopamine receptor]] D1 antagonist.
[[File:PF-4455242.svg|Chemical structure of PF-04455242|thumb|right]]
PF-04455242 is a chemical compound that was developed as a selective antagonist for the [[cannabinoid receptor]] CB1. It was investigated for its potential therapeutic effects in various [[neurological disorders]], including [[schizophrenia]] and [[anxiety]]. The compound is notable for its high selectivity and affinity for the CB1 receptor, distinguishing it from other cannabinoid receptor antagonists.


== Chemical Properties ==
==Pharmacology==
PF-04455242 is a synthetic compound with a complex chemical structure. The molecular formula is C23H21F3N4O2, and it has a molecular weight of 442.44 g/mol. The compound is characterized by the presence of a trifluoromethyl group, which contributes to its high binding affinity and selectivity for the CB1 receptor.
PF-04455242 is designed to target the [[dopamine receptor D1]], which is implicated in various [[neurological disorders]]. By antagonizing this receptor, PF-04455242 aims to modulate the dopaminergic system, potentially improving cognitive function in patients with disorders like schizophrenia and Alzheimer's disease.


== Mechanism of Action ==
==Mechanism of Action==
As a CB1 receptor antagonist, PF-04455242 works by blocking the action of endogenous cannabinoids at the CB1 receptor site. This receptor is primarily found in the [[central nervous system]] and is involved in the regulation of various physiological processes, including mood, appetite, and pain sensation. By inhibiting the CB1 receptor, PF-04455242 can modulate these processes, potentially offering therapeutic benefits in conditions where the endocannabinoid system is dysregulated.
The drug functions by selectively binding to the D1 subtype of dopamine receptors, inhibiting their activity. This action is thought to help in balancing the dopaminergic activity in the brain, which is often disrupted in cognitive disorders. The modulation of D1 receptors is believed to enhance [[working memory]] and [[executive function]], which are typically impaired in these conditions.


== Potential Therapeutic Applications ==
==Development and Research==
PF-04455242 has been studied for its potential use in treating several conditions:
[[File:PF-4455242.svg|Chemical structure of PF-04455242|thumb|right]]
 
PF-04455242 has undergone various stages of clinical trials to assess its efficacy and safety. Initial studies focused on its potential benefits in improving cognitive deficits associated with schizophrenia. However, the development of PF-04455242 has faced challenges, including the complexity of targeting specific dopamine receptors without affecting others, which can lead to side effects.
* '''Schizophrenia''': The compound was investigated for its ability to alleviate symptoms of schizophrenia, particularly cognitive deficits and negative symptoms, which are not adequately addressed by current antipsychotic medications.
 
* '''Anxiety Disorders''': Due to its action on the CB1 receptor, PF-04455242 was also explored as a treatment for anxiety disorders, where it might help reduce anxiety symptoms by modulating the endocannabinoid system.
 
* '''Obesity''': Although not its primary focus, the compound's ability to influence appetite regulation through CB1 receptor antagonism suggested potential applications in weight management and obesity treatment.


== Development and Research ==
==Potential Applications==
Research on PF-04455242 has primarily been conducted in preclinical and early clinical trials. The compound demonstrated promising results in animal models, showing efficacy in reducing anxiety-like behaviors and improving cognitive function. However, further clinical trials are necessary to fully understand its safety profile and therapeutic potential in humans.
The primary focus of PF-04455242 is on cognitive enhancement in disorders like schizophrenia and Alzheimer's disease. By improving cognitive functions, the drug could potentially enhance the quality of life for patients suffering from these debilitating conditions. However, further research is needed to fully understand its efficacy and safety profile.


== Challenges and Considerations ==
==Challenges and Considerations==
While PF-04455242 shows promise, there are challenges associated with its development. The complexity of the endocannabinoid system and the potential for off-target effects necessitate careful evaluation of its safety and efficacy. Additionally, the development of selective CB1 antagonists must consider the risk of psychiatric side effects, as seen with other compounds in this class.
Developing drugs that target the dopaminergic system is challenging due to the intricate balance required to avoid side effects. The specificity of PF-04455242 for the D1 receptor is crucial in minimizing unwanted interactions with other dopamine receptors, which could lead to adverse effects.


== Related Pages ==
==Related pages==
* [[Cannabinoid receptor]]
* [[Dopamine receptor D1]]
* [[Endocannabinoid system]]
* [[Schizophrenia]]
* [[Schizophrenia]]
* [[Anxiety disorder]]
* [[Alzheimer's disease]]
* [[Cognitive disorders]]


[[Category:Pharmacology]]
[[Category:Investigational drugs]]
[[Category:Cannabinoid receptor antagonists]]
[[Category:Dopamine antagonists]]

Latest revision as of 06:22, 5 March 2025

Investigational drug


PF-04455242
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number 956905-27-4
PubChem 16005106
DrugBank
ChemSpider 13180813
KEGG D09992


PF-04455242 is an investigational drug that was developed by Pfizer for the treatment of cognitive disorders such as schizophrenia and Alzheimer's disease. It acts as a selective dopamine receptor D1 antagonist.

Pharmacology[edit]

PF-04455242 is designed to target the dopamine receptor D1, which is implicated in various neurological disorders. By antagonizing this receptor, PF-04455242 aims to modulate the dopaminergic system, potentially improving cognitive function in patients with disorders like schizophrenia and Alzheimer's disease.

Mechanism of Action[edit]

The drug functions by selectively binding to the D1 subtype of dopamine receptors, inhibiting their activity. This action is thought to help in balancing the dopaminergic activity in the brain, which is often disrupted in cognitive disorders. The modulation of D1 receptors is believed to enhance working memory and executive function, which are typically impaired in these conditions.

Development and Research[edit]

Chemical structure of PF-04455242

PF-04455242 has undergone various stages of clinical trials to assess its efficacy and safety. Initial studies focused on its potential benefits in improving cognitive deficits associated with schizophrenia. However, the development of PF-04455242 has faced challenges, including the complexity of targeting specific dopamine receptors without affecting others, which can lead to side effects.

Potential Applications[edit]

The primary focus of PF-04455242 is on cognitive enhancement in disorders like schizophrenia and Alzheimer's disease. By improving cognitive functions, the drug could potentially enhance the quality of life for patients suffering from these debilitating conditions. However, further research is needed to fully understand its efficacy and safety profile.

Challenges and Considerations[edit]

Developing drugs that target the dopaminergic system is challenging due to the intricate balance required to avoid side effects. The specificity of PF-04455242 for the D1 receptor is crucial in minimizing unwanted interactions with other dopamine receptors, which could lead to adverse effects.

Related pages[edit]

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