Meclinertant

DCTPepD ID  DCTPepD0039

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

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

Structure

 

Show IUPAC/InChI/SMILES

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.





DCTPep is developed by Dr.Zheng's team.