CP 122721
CP 122721 is an orally active NK1 receptor antagonist. CP 122721 attenuates cisplatin-induced vomiting in ferrets (ID50: 0.08 mg/kg). CP 122721 inhibits kainate (KA)-induced seizure activity and CA1 neuronal cell death in rats. CP 122721 is useful in the study of depression, asthma, and irritable bowel syndrome (IBS).
For research use only. We do not sell to patients.
- CAS No.: 145742-28-5
- Formula: C20H23F3N2O2
- Molecular Weight:380.40
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.14 nM
Compound: (+/-) 2
|
Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed in CHO cells
Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed in CHO cells
|
[PMID: 9804700] |
| CHO | IC50 |
0.14 nM
Compound: CP-122721
|
Displacement of [125I]-labeled substance P from cloned human NK1 receptor expressed in CHO cells
Displacement of [125I]-labeled substance P from cloned human NK1 receptor expressed in CHO cells
|
[PMID: 16307878] |
| IM-9 | IC50 |
0.19 nM
Compound: 3f
|
Antagonist activity for Tachykinin receptor 1 as displacement of [3H]-Substance P in human IM-9 cells
Antagonist activity for Tachykinin receptor 1 as displacement of [3H]-Substance P in human IM-9 cells
|
[PMID: 9871670] |
| IM-9 | IC50 |
0.4 nM
Compound: CP-122721
|
Displacement of [3H]spiperone from NK1 receptor in human IM9 cells
Displacement of [3H]spiperone from NK1 receptor in human IM9 cells
|
[PMID: 18640044] |
Chemical Information
-
CAS No. 145742-28-5
-
Molecular Weight 380.40
-
Formula C20H23F3N2O2
-
SMILES
FC(F)(F)OC1=CC=C(OC)C(CN[C@@H]2[C@H](C3=CC=CC=C3)NCCC2)=C1
-
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
[1]. Gonsalves S, et al. Broad spectrum antiemetic effects of CP-122,721, a tachykinin NK1 receptor antagonist, in ferrets. Eur J Pharmacol. 1996 Jun 3;305(1-3):181-5. [Content Brief]
[2]. Zachrisson O, Lindefors N, Brené S. A tachykinin NK1 receptor antagonist, CP-122,721-1, attenuates kainic acid-induced seizure activity. Brain Res Mol Brain Res. 1998 Oct 1;60(2):291-5. [Content Brief]
[3]. Duffy RA. Potential therapeutic targets for neurokinin-1 receptor antagonists. Expert Opin Emerg Drugs. 2004 May;9(1):9-21. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz