PF-03382792

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PF-03382792 is a potent 5-HT₄ partial agonist with a K_i of 2.7 nM and an EC₅₀ of 0.9 nM for 5-HT_4d. PF-03382792 can penetrate the brain. PF-03382792 produces moderate increases in cortical Ach in the rat prefrontal cortex.

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PF-03382792 Chemical Structure

CAS No. : 1400811-63-3

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5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

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Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

5-HT_4d Receptor

2.7 nM (Ki)

5-HT_4d Receptor

0.9 nM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	0.8 nM Compound: 3	Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay	[PMID: 22974325]
HEK293	EC₅₀	0.9 nM Compound: 3	Agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay Agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay	[PMID: 22974325]
HEK293	EC₅₀	1.15 nM Compound: 3	Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay	[PMID: 22974325]
HEK293	EC₅₀	1.2 nM Compound: 3	Agonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay Agonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay	[PMID: 22974325]
HEK293	EC₅₀	1.3 nM Compound: 3	Agonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay Agonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay	[PMID: 22974325]
HEK293	EC₅₀	1.52 nM Compound: 3	Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay	[PMID: 22974325]
HEK293	EC₅₀	2.15 nM Compound: 3	Agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay Agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay	[PMID: 22974325]

Molecular Weight

433.52

Formula

C₂₃H₃₂FN₃O₄

CAS No.

1400811-63-3

SMILES

O=C(N1C(C(C)(C)C2=C1C=C(F)C=C2)=O)NCC3CCN(CC4(O)CCOCC4)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Michael A Brodney, et al.Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease. J Med Chem. 2012 Nov 8;55(21):9240-54. [Content Brief]

PF-03382792 Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-033827921400811-63-3PF03382792PF 033827925-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT4Achprefrontal cortexInhibitorinhibitorinhibit

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