Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C28H32N2O |
| Molecular Weight | 412.5665 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(CN[C@H]2C3CCN(CC3)[C@H]2C(C4=CC=CC=C4)C5=CC=CC=C5)C=CC=C1
InChI
InChIKey=FLNYLINBEZROPL-NSOVKSMOSA-N
InChI=1S/C28H32N2O/c1-31-25-15-9-8-14-24(25)20-29-27-23-16-18-30(19-17-23)28(27)26(21-10-4-2-5-11-21)22-12-6-3-7-13-22/h2-15,23,26-29H,16-20H2,1H3/t27-,28-/m0/s1
CP-96,345 is a potent, selective nonpeptide Substance P (NK1) receptor antagonist. Rather than being a primary neurotransmitter, it prolongs the nociception produced by other neurotransmitters. By controlling endothelial permeability, SP plays a major role in inflammation and inflammatory aspects of asthma, possibly by regulating the access of neutrophils to an inflammatory site. These results indicate potential therapeutic applications for SP antagonists in the treatment of chronic pain, inflammation, and inflammatory aspects of asthma.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Release of beta-endorphin immunoreactivity into ventriculo-cisternal perfusate by lumbar intrathecal capsaicin in the rat. | 1995 Dec 1 |
|
| Effect of tachykinin receptor antagonists in experimental neuropathic pain. | 1998 Nov 20 |
|
| Neurokinin-1 receptor antagonists protect mice from CD95- and tumor necrosis factor-alpha-mediated apoptotic liver damage. | 2004 Mar |
Patents
Sample Use Guides
in rats:
The acute administration of 5 or 10 mg/kg of CP 96,345 produced a significant decrease in the number of spontaneously active SNC and VTA dopamine cells compared to vehicle-treated rats.
The chronic administration of CP 96,345 (5 or 10 mg/kg, i.p.) for 21 days also produced a significant decrease in the number of sontaneously active SNC and VTA DA cells compared to vehicle controls.
Route of Administration:
Intravenous
CP-96,345 (10*(-7)M), potently inhibited HIV (R5 strains) replication in human peripheral blood monocyte-derived macrophages (MDM). P-96,345 down-regulated CCR5 expression in MDM, downregulation of CCR5 is functionally relevant to the decreased susceptibility to HIV infection by MDM.
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DTXSID30927796
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104943
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132746-60-2
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W22ILA2I52
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ACTIVE MOIETY
