CP 96345 - CAS 132746-60-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C28H32N2O
Molecular Weight:
412.57
COA:
Inquire
Targets:
Neurokinin Receptor
Description:
CP 96345 is an effective and selective non-peptide NK1 receptor antagonist and has been found to show activities in restraining neurogenic inflammation in vivo.
Purity:
≥98% by HPLC
Appearance:
White Solid
Synonyms:
CP-96345; CP 96345; CP96345; (2S,3S)-N-(2-Methoxyphenyl)methyl-2-diphenylmethyl-1-azabicyclo[2.2.2]octan-3-amine
MSDS:
Inquire
InChIKey:
FLNYLINBEZROPL-NSOVKSMOSA-N
InChI:
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
Canonical SMILES:
COC1=CC=CC=C1CNC2C3CCN(C2C(C4=CC=CC=C4)C5=CC=CC=C5)CC3
1.Neurokinin-1 receptor antagonists CP-96,345 and L-733,060 protect mice from cytokine-mediated liver injury.
Bang R;Sass G;Kiemer AK;Vollmar AM;Neuhuber WL;Tiegs G J Pharmacol Exp Ther. 2003 Apr;305(1):31-9.
Previously, we have shown that primary afferent sensory neurons are necessary for disease activity in T cell-mediated immune hepatitis in mice. In the present study, we analyzed the possible role of substance P (SP), an important proinflammatory neuropeptide of these nerve fibers, in an in vivo mouse model of liver inflammation. Liver injury was induced by bacterial lipopolysaccharide (LPS) in D-galactosamine (GalN)-sensitized mice. Depletion of primary afferent nerve fibers by neonatal capsaicin treatment down-regulated circulating levels of the proinflammatory cytokines tumor necrosis factor-alpha (TNFalpha) and interferon-gamma (IFNgamma) and protected mice from GalN/LPS-induced liver injury. Likewise, pretreatment of mice with antagonists of the SP-specific neurokinin-1 receptor (NK-1R), i.e., (2S,3S)-cis-2-(diphenylmethyl)-N-((2-methoxyphenyl)-methyl)-1-azabicyclo(2.2.2.)-octan-3-amine (CP-96,345) and (2S,3S)3-([3,5-bis(trifluoromethyl)phenyl]methoxy)-2-phenylpiperidine (L-733,060), dose dependently protected mice from GalN/LPS-induced liver injury. The presence of the NK-1R in the murine liver was demonstrated by reverse transcription-polymerase chain reaction, sequence analysis, and immunocytochemistry.
2.The substance P (NK1) receptor antagonist (+/-)-CP-96,345 causes sedation and motor impairment in Swiss albino mice in the black-and-white box behavioral paradigm.
Zernig G;Dietrich H;Maggi CA;Saria A Neurosci Lett. 1992 Aug 31;143(1-2):169-72.
In order to test the suggested involvement of substance P (NK1) receptors in anxiety, the non-peptide NK1 antagonist (+/-)-CP-96,345 was tested in Swiss albino mice using the black-and-white box behavioral paradigm. Intraperitoneal (+/-)-CP-96,345 dose-dependently decreased the motor activity and the number of exploratory rearings in both the brightly lit and dark compartment as well as the transitions between the compartments, whereas it increased the latency of the initial movement into the dark compartment as well as the time spent in the light section. ED50 or ID50 values ranged from 1.9 to 3.6 mg/kg and Hill slopes from 1.4 to 5.0. (+/-)-CP-96,345 also produced rotatory behavior of no preferred lateralization as well as the Straub phenomenon in some animals. The effects of (+/-)-CP-96,345 (5 mg/kg) were not affected by 2 mg/kg naloxone (i.p.) which was also ineffective when given alone. Thus, (+/-)-CP-96,345 does not display any anxiogenic effect but causes dose-dependent sedation and motor impairment.
3.Neurokinin 1 receptors mediate substance P-induced changes in ion transport in guinea-pig ileum.
Reddix RA;Cooke HJ Regul Pept. 1992 Jun 11;39(2-3):215-25.
Tachykinin receptors mediating substance P-induced secretion were examined in muscle-stripped segments of guinea-pig ileum set up in flux chambers. Changes in the short-circuit current (Isc) served as an index of active, electrogenic ion transport. Substance P evoked a transient increase in Isc which was concentration-dependent. The maximal change in Isc occurred at 1 microM concentration. [Sar9,Met(O2)11]-substance P, a neurokinin 1 (NK-1) receptor agonist, evoked a similar concentration-dependent increase in Isc. [Nle10]NKA(4-10) (1 microM) or [Pro7]NKB (1 microM), selective NK2 and NK3 agonists, respectively, had minimal effects on Isc. CP-96,345 (5 microM), a nonpeptide NK-1 antagonist, and the peptide NK-1 antagonist, GR82334 (1 microM), reduced the secretory response to substance P (50 nM) in the presence and absence of tetrodotoxin (0.2 microM). The NK2 antagonist, [Tyr5,D-Trp6,8,9,Arg10]NKA(4-10) MEN 10207 had no effect on the substance P response. Tetrodotoxin (0.2 microM) significantly reduced, but did not abolish the Isc response to substance P (1 microM) and [Sar9,Met(O2)11]substance P (1 microM). The substance P response was unaltered by 5 microM atropine and 50 microM mecamylamine.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Neurokinin Receptor Products


CAS 148700-85-0 L-733,060

L-733,060
(CAS: 148700-85-0)

L-733,061, a phenylpiperidine derivative, has been found to be a NK1 receptor antagonist that could probably be antidepressant/ anxiolytic agent and also show a...

CAS 86933-75-7 Neurokinin B

Neurokinin B
(CAS: 86933-75-7)

Neurokinin B, one of the tachykinin family of peptides, binds a family of GPCRs—including neurokinin receptor 1 (NK1R), NK2R, and NK3R to mediate their biologic...

CAS 135721-56-1 MDL 29913

MDL 29913
(CAS: 135721-56-1)

MDL 29913 is a selective NK2 tachykinin receptor antagonist which can be used in the treatment of IBS.

CAS 86933-74-6 Neurokinin A

Neurokinin A
(CAS: 86933-74-6)

Neurokinin A is a member of the endogenous tachykinin agonist with preference for the NK-2R (NK-2 receptor).

CAS 147116-67-4 Maropitant

Maropitant
(CAS: 147116-67-4)

Maropitant is a neurokinin (NK1) receptor antagonist.

CAS 160492-56-8 Osanetant

Osanetant
(CAS: 160492-56-8)

Osanetant is a non-peptide neurokinin 3 (NK3) receptor antagonist. It is developed for the treatment of schizophrenia and other central nervous system (CNS) dis...

CAS 264618-38-4 SSR 146977 hydrochloride

SSR 146977 hydrochloride
(CAS: 264618-38-4)

SSR 146977 hydrochloride is a potent and selective NK3 receptor antagonist (Ki = 0.26 and 19.3 nM in CHO cells expressing the human NK3 and NK2 receptor, respec...

CAS 188923-01-5 L760735

L760735
(CAS: 188923-01-5)

L760735 is a high-affinity NK1 receptor antagonist with IC50 value of 0.19 nM. It is selective over NK2 and NK3 receptors. It is used in the synthetic preparati...

Chemical Structure

CAS 132746-60-2 CP 96345

Quick Inquiry

Verification code

Featured Items