Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C19H24N2O |
| Molecular Weight | 296.4067 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(CN[C@H]2CCCN[C@H]2C3=CC=CC=C3)C=CC=C1
InChI
InChIKey=DTQNEFOKTXXQKV-HKUYNNGSSA-N
InChI=1S/C19H24N2O/c1-22-18-12-6-5-10-16(18)14-21-17-11-7-13-20-19(17)15-8-3-2-4-9-15/h2-6,8-10,12,17,19-21H,7,11,13-14H2,1H3/t17-,19-/m0/s1
| Molecular Formula | C19H24N2O |
| Molecular Weight | 296.4067 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/7693914Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800002331 | https://www.ncbi.nlm.nih.gov/pubmed/9834049 | https://www.ncbi.nlm.nih.gov/pubmed/20651222 | https://www.ncbi.nlm.nih.gov/pubmed/7663799
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7693914
Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800002331 | https://www.ncbi.nlm.nih.gov/pubmed/9834049 | https://www.ncbi.nlm.nih.gov/pubmed/20651222 | https://www.ncbi.nlm.nih.gov/pubmed/7663799
CP 99994 dihydrochloride have shown the compound to be a potent, selective and competitive NK-1 receptor antagonist. In preclinical studies, CP 99994 decreased cough number, peak abdominal activity, and peak tracheal pressure, without affecting baseline respiration. But in clinical trial administration of CP 99994 over 2 h does not significantly inhibit hypertonic saline-induced bronchoconstriction or cough in subjects with mild asthma. CP 99994 significantly suppressed acute postoperative pain at 90 min after surgery.
CNS Activity
Originator
Sources: http://adisinsight.springer.com/drugs/800002331
Curator's Comment: # Pfizer
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL249 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7693914 |
0.25 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7663799 |
Primary | Unknown Approved UseUnknown |
||
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Endothelium-dependent contraction in intrapulmonary arteries: mediation by endothelial NK1 receptors and TXA2. | 1995-08 |
|
| Pharmacology of CP-99,994; a nonpeptide antagonist of the tachykinin neurokinin-1 receptor. | 1993-10 |
|
| A new NK1 receptor antagonist (CP-99,994) prevents the increase in tracheal vascular permeability produced by hypertonic saline. | 1993-07 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7693914
Dose range 0.178 to 10 mg/kg 30 min after [Sar9,Met(O2)11]-SPinfusion.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7582548
The endothelium-dependent contraction induced by substance P (10(-8) M) was abolished by NK1 antagonist CP-99994 (0.01 nM – 100 nM).
| Substance Class |
Chemical
Created
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admin
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Edited
Tue Apr 01 21:49:40 GMT 2025
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Tue Apr 01 21:49:40 GMT 2025
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| Record UNII |
5KM4QA7RZC
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| Record Status |
Validated (UNII)
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