2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. PF-03382792

PF-03382792 is a potent 5-HT4 partial agonist with a Ki of 2.7 nM and an EC50 of 0.9 nM for 5-HT4d. 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

PF-03382792 Chemical Structure

CAS No. : 1400811-63-3

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PF-03382792 Related Antibodies

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Description

PF-03382792 is a potent 5-HT4 partial agonist with a Ki of 2.7 nM and an EC50 of 0.9 nM for 5-HT4d. PF-03382792 can penetrate the brain. PF-03382792 produces moderate increases in cortical Ach in the rat prefrontal cortex[1].

IC50 & Target[1]

5-HT4d Receptor

2.7 nM (Ki)

5-HT4d 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.
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
References
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PF-03382792 Related Classifications

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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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