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
| Molecular Formula | C28H32N2O |
| Molecular Weight | 412.5665 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
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 |
|---|---|---|
| Substance P receptors on human astrocytoma cells are linked to glycogen breakdown. | 1994 Feb 14 |
|
| Agonist-induced internalization of the substance P (NK1) receptor expressed in epithelial cells. | 1994 Oct 1 |
|
| Effect of tachykinin receptor antagonists in experimental neuropathic pain. | 1998 Nov 20 |
|
| Acetylcholine and tachykinin receptor antagonists attenuate wood smoke-induced bronchoconstriction in guinea pigs. | 1998 Nov 6 |
|
| NK1-receptor activation prevents hydrocarbon-induced lung injury in mice. | 1999 Feb |
|
| Neurokinin-1 receptor antagonists CP-96,345 and L-733,060 protect mice from cytokine-mediated liver injury. | 2003 Apr |
|
| Neurokinin-1 receptor antagonists protect mice from CD95- and tumor necrosis factor-alpha-mediated apoptotic liver damage. | 2004 Mar |
|
| Phosphorylation of TRPV1 by neurokinin-1 receptor agonist exaggerates the capsaicin-mediated substance P release from cultured rat dorsal root ganglion neurons. | 2008 Dec |
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.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 18:11:57 GMT 2023
by
admin
on
Fri Dec 15 18:11:57 GMT 2023
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| Record UNII |
W22ILA2I52
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| Record Status |
Validated (UNII)
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| Record Version |
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104943
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132746-60-2
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admin on Fri Dec 15 18:11:57 GMT 2023 , Edited by admin on Fri Dec 15 18:11:57 GMT 2023
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