Details
Stereochemistry | ACHIRAL |
Molecular Formula | C24H24FN3O2 |
Molecular Weight | 405.4647 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
FC1=CC=C(C=C1)C2=CN=CC(CN3CCN(CC3)C4=CC=CC5=C4OCCO5)=C2
InChI
InChIKey=IUVSEUFHPNITEQ-UHFFFAOYSA-N
InChI=1S/C24H24FN3O2/c25-21-6-4-19(5-7-21)20-14-18(15-26-16-20)17-27-8-10-28(11-9-27)22-2-1-3-23-24(22)30-13-12-29-23/h1-7,14-16H,8-13,17H2
Molecular Formula | C24H24FN3O2 |
Molecular Weight | 405.4647 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/24164194Curator's Comment: description was created based on several sources, including
http://www.solvay.com/en/binaries/20080930_Pharma-135290.pdf
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24164194
Curator's Comment: description was created based on several sources, including
http://www.solvay.com/en/binaries/20080930_Pharma-135290.pdf
Adoprazine (SVL-313) is a full 5-HT1A receptor agonist and full D2/3 receptor antagonist possessing characteristics of an atypical antipsychotic, representing a potential novel treatment for schizophrenia and bipolar disorder. This drug together with some others, e.g. Mazapertine succinate, PF-217830 was discontinued from clinical trials due to either non-optimal pharmacokinetic properties or insufficient therapeutical efficacy.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL214 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16710314 |
9.0 null [pEC50] | ||
Target ID: CHEMBL2095169 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16710314 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator​
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes [IC50 10.684 uM] | ||||
yes [IC50 4.7724 uM] | ||||
yes [IC50 9.5221 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no |
PubMed
Title | Date | PubMed |
---|---|---|
Novel antipsychotic agents with 5-HT(1A) agonist properties: role of 5-HT(1A) receptor activation in attenuation of catalepsy induction in rats. | 2005 Aug |
|
SAR study of 1-aryl-4-(phenylarylmethyl)piperazines as ligands for both dopamine D2 and serotonin 5-HT1A receptors showing varying degrees of (Ant)agonism. Selection of a potential atypical antipsychotic. | 2006 Sep |
|
SLV313 (1-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-4- [5-(4-fluoro-phenyl)-pyridin-3-ylmethyl]-piperazine monohydrochloride): a novel dopamine D2 receptor antagonist and 5-HT1A receptor agonist potential antipsychotic drug. | 2007 Jan |
Patents
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16710314
Curator's Comment: SLV313 (ADOPRAZINE) possessed high affinity at human recombinant D(2), D(3), D(4), 5-HT(2B), and 5-HT(1A) receptors, moderate affinity at 5-HT(7) and weak affinity at 5-HT(2A) receptors, with little-no affinity at 5-HT(4), 5-HT(6), alpha(1), and alpha(2) (rat), H(1) (guinea pig), M(1), M(4), 5-HT(3) receptors, and the 5-HT transporter. SLV313 had full agonist activity at cloned h5-HT(1A) receptors (pEC(50)=9.0) and full antagonist activity at hD(2) (pA(2)=9.3) and hD(3) (pA(2)=8.9) receptors.
Unknown
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:10:36 GMT 2023
by
admin
on
Fri Dec 15 16:10:36 GMT 2023
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Record UNII |
7SNB18Q89D
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C265
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C81482
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TARGET -> INHIBITOR |
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TARGET -> INHIBITOR |
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TARGET -> AGONIST |
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |
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