Meclinertant
DRACPC ID DRACPC0039
Active Ingredients Meclinertant
Description A nonpeptide antagonist of neurotensin (NT) receptors, is selective for the NTR1. NT is a endogenously expressed tridecapeptide, present within specific regions of the central nervous system. Up regulation of NT receptor (NTR) expression has been observed in cancers of the Lung, Breast, Pancreas, Pituitary and of the Prostate. The two neurotensin receptor subtypes known to date, NTR1 and NTR2, belong to the family of G-protein-coupled receptors with seven putative transmembrane domains (TM). Similar to many GPCR’s, NTR1 and NTR2 have been shown to activate several signal transduction pathways, up-regulating intracellular cAMP, inositol phosphate, and intracellular calcium levels.
Synonyms SR-48692; 2-((1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)pyrazol-3-yl)carbonylamino)tricyclo(3.3.1.1.(3.7))decan-2-carboxylic Acid; SR 48692; Tricyclo(3.3.1.13,7)decane-2-carboxylic Acid, 2-(((1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl)carbonyl)amino)-; Meclinertant
Type Small Molecule
Disease Colorectal cancer, Prostate cancer, Schizophrenia, Schizoaffective disorders, Psychosis, Depression, Lung cancer
Classification
NTR antagonist Amino acid and derivative
Structure Information
Molecular Formula C32H31ClN4O5
Molecular Weight 587.1
Active Sequence Not available
Sequence Length Not available
Modification Not available
IUPAC Name 2-[[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acid
InChI InChI=1S/C32H31ClN4O5/c1-41-27-4-3-5-28(42-2)29(27)26-16-24(36-37(26)25-8-9-34-23-15-21(33)6-7-22(23)25)30(38)35-32(31(39)40)19-11-17-10-18(13-19)14-20(32)12-17/h3-9,15-20H,10-14H2,1-2H3,(H,35,38)(H,39,40)/t17-,18+,19-,20+,32-
InChI_Key DYLJVOXRWLXDIG-LWXMPVTCSA-N
SMILES ClC1=CC=C(C(N2C(C3=C(OC)C=CC=C3OC)=CC(C(N[C@@]4(C(O)=O)[C@H]5C[C@@H](C[C@@H]4C6)C[C@@H]6C5)=O)=N2)=CC=N7)C7=C1
External Codes
PubChem CID 119192
DrugBank Accession Number DB06455
NCI Thesaurus Code C156766
UNII 5JBP4SI96H GSRS
CAS 146362-70-1
Drug approval
Drug indication
Investigated for use/treatment in colorectal cancer, prostate cancer, schizophrenia and schizoaffective disorders, psychosis, depression, and lung cancer.
The drug is not approved.
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT00290953 | A Double Blind, Randomized, Phase II-III Maintenance Study of SR48692 Versus Placebo in Patients With Extensive Stage Small Cell Lung Cancer Following a First Line Chemotherapy With Cisplatin + Etoposide | Lung Cancer; Pulmonary Neoplasms; Small Cell Lung Cancer | Phase 2/3 | Treatment |
More clinical information is obtained from ClinicalTrials.gov.
