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version 2.7.1
Substance Class Chemical
Record UNII
D26C95A960
Record Status Validated
Record Version
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Details

Stereochemistry ABSOLUTE
Molecular Formula C18H23NO2
Molecular Weight 285.3807
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0
Created by admin on Sat Jun 26 06:52:20 EDT 2021
Edited by GUEST on Wed Jul 21 15:55:17 EDT 2021
Structure of ORM-12741

Systematic Names:

  • None recorded

SMILES

[H][C@]12N(CCC[C@]1(C)COC)CCC3=C2OC4=C3C=CC=C4

InChI

OCUKPFWNSAAHRP-QZTJIDSGSA-N
InChI=1S/C18H23NO2/c1-18(12-20-2)9-5-10-19-11-8-14-13-6-3-4-7-15(13)21-16(14)17(18)19/h3-4,6-7,17H,5,8-12H2,1-2H3/t17-,18-/m1/s1
Name Type Language Details Access References
ORM-12741
Common Name
English  
ORM-10921
Code
English  
2H-BENZOFURO(2,3-A)QUINOLIZINE, 1,3,4,6,7,12B-HEXAHYDRO-1-(METHOXYMETHYL)-1-METHYL-, (1S,12BS)-
Systematic Name
English  
(1S,12BS)-1-(METHOXYMETHYL)-1-METHYL-2,3,4,6,7,12B-HEXAHYDROBENZOFURO(2,3-A)QUINOLIZINE
Systematic Name
English  
Code System Code Type Description Access References
CAS
610782-82-6
Created by admin on Sat Jun 26 06:52:20 EDT 2021 , Edited by admin on Sat Jun 26 06:52:20 EDT 2021
PRIMARY
DRUG BANK
DB12057
Created by admin on Sat Jun 26 06:52:20 EDT 2021 , Edited by admin on Sat Jun 26 06:52:20 EDT 2021
PRIMARY
FDA UNII
D26C95A960
Created by admin on Sat Jun 26 06:52:20 EDT 2021 , Edited by admin on Sat Jun 26 06:52:20 EDT 2021
PRIMARY
PUBCHEM
71301276
Created by admin on Sat Jun 26 06:52:20 EDT 2021 , Edited by admin on Sat Jun 26 06:52:20 EDT 2021
PRIMARY
Related Record Type Details Access References
ACTIVE MOIETY
Mediator Substance Details
none
Standard in vitro receptor assays and antagonism of .ALPHA.2, and .ALPHA.1-AR agonist-evoked responses in vivo were used to demonstrate the .ALPHA.2C-AR selectivity for ORM-10921 which was tested in established behavioural models related to schizophrenia and cognitive dysfunction with an emphasis on pharmacologically induced hypoglutamatergic state by phencyclidine or MK-801. The Kb values of in vitro .ALPHA.2C-AR antagonism for ORM-10921 varied between 0.078-1.2 nM depending on the applied method. The selectivity ratios compared to .ALPHA.2A-AR subtype and other relevant receptors were 10-100 times in vitro. The in vivo experiments supported its potent .ALPHA.2C-antagonism combined with only a weak .ALPHA.2A-antagonism. In the pharmacodynamic microdialysis study, ORM-10921 was found to increase extracellular dopamine levels in prefrontal cortex in the baseline conditions.
Created by admin on Sat Jun 26 06:52:20 EDT 2021 , Edited by admin on Sat Jun 26 06:52:20 EDT 2021
ACTIVE MOIETY
Mediator Substance Details
none
Originator: Juvantia Pharma (CEASED), Orion; Class: Neuropsychotherapeutic; Mechanism of Action: Alpha 2c adrenergic receptor antagonist; Highest Development Phase: Discontinued for Major depressive disorder, Schizophrenia; Most Recent Events: 10 May 2006 Discontinued - Phase-I for Schizophrenia in Finland (unspecified route), 10 May 2006 Discontinued - Preclinical for Depression in Finland (unspecified route)
Created by admin on Sat Jun 26 06:52:20 EDT 2021 , Edited by admin on Sat Jun 26 06:52:20 EDT 2021
Created Sat Jun 26 06:52:20 EDT 2021
Created By admin
Last Edited Sat Jun 26 06:52:20 EDT 2021
Last Edited By admin
Index Source Text / Citation Source Type Tags Date Accessed File Access
1 dump-public-2021-06-23_UPDATED.gsrs BATCH_IMPORT Sat Jun 26 06:52:19 EDT 2021
2 SRS CODE IMPORT SRS NOMEN Fri Apr 28 15:27:01 EDT 2017
3 ADIS-INSIGHT:ORM-12741 WEBSITE NOMEN
4 SYSTEM
5 CHEMDRAW SRS NOMEN PUBLIC_DOMAIN_RELEASE AUTO_SELECTED
6 stn SRS NOMEN
7 STN STN (SCIFINDER)
8 SRS import [D26C95A960] SRS NOMEN Fri Apr 28 15:27:01 EDT 2017
9 STN SRS NOMEN
10 https://en.wordpress.com/tag/orm-12741/ SRS NOMEN
11 BASIC CLIN PHARMACOL TOXICOL. 2013 OCT;113(4):239-49. DOI: 10.1111/BCPT.12090. EPUB 2013 JUN 20. JOURNAL ARTICLE NOMEN

Molecular Formula C18H23NO2
Molecular Weight 285.3807
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED