Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C16H17ClN2OS.ClH |
Molecular Weight | 357.298 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.ClC1=CC=CC2=C1SC(=C2)C(=O)N[C@H]3CN4CCC3CC4
InChI
InChIKey=OIJYTJGIDVTCFF-ZOWNYOTGSA-N
InChI=1S/C16H17ClN2OS.ClH/c17-12-3-1-2-11-8-14(21-15(11)12)16(20)18-13-9-19-6-4-10(13)5-7-19;/h1-3,8,10,13H,4-7,9H2,(H,18,20);1H/t13-;/m0./s1
Molecular Formula | C16H17ClN2OS |
Molecular Weight | 320.837 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://adisinsight.springer.com/drugs/800027229Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/22085888 | https://www.ecnp.eu/~/media/Files/ecnp/Projects%20and%20initiatives/Medicines%20Chest/EVP%206124.pdf
Sources: http://adisinsight.springer.com/drugs/800027229
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/22085888 | https://www.ecnp.eu/~/media/Files/ecnp/Projects%20and%20initiatives/Medicines%20Chest/EVP%206124.pdf
Encenicline (EVP-6124; MT-4666) acts as a potent partial and selective agonist at alpha-7 nicotinic acetylcholine receptor. Encenicline significantly improved memory function in animal models. FORUM Pharmaceuticals (formerly EnVivo Pharmaceuticals) is developing encenicline for the treatment of cognition disorders such as schizophrenia and for Alzheimer's disease.
Originator
Sources: http://adisinsight.springer.com/drugs/800027229
Curator's Comment: # Bayer HealthCare
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2492 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22085888 |
4.33 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
35.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
4.66 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
7 mg single, oral dose: 7 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.588 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
100 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2800 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
358 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
7 mg single, oral dose: 7 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
45.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
8890 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
63 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
60.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
7 mg single, oral dose: 7 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
52.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
60.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
PubMed
Title | Date | PubMed |
---|---|---|
Natalizumab: AN 100226, anti-4alpha integrin monoclonal antibody. | 2004 |
|
Discovery and development of α7 nicotinic acetylcholine receptor modulators. | 2011 Dec 8 |
|
EVP-6124, a novel and selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors. | 2012 Feb |
|
The novel α7 nicotinic acetylcholine receptor agonist EVP-6124 enhances dopamine, acetylcholine, and glutamate efflux in rat cortex and nucleus accumbens. | 2014 Dec |
|
Randomized, Double-Blind, Placebo-Controlled Study of Encenicline, an α7 Nicotinic Acetylcholine Receptor Agonist, as a Treatment for Cognitive Impairment in Schizophrenia. | 2015 Dec |
|
Pharmacodynamics, pharmacokinetics, safety, and tolerability of encenicline, a selective α7 nicotinic receptor partial agonist, in single ascending-dose and bioavailability studies. | 2015 Feb 1 |
Patents
Sample Use Guides
Encenicline was well tolerated at single doses up to 180 mg, and doses as low as 1 mg had dose- and time-dependent pharmacodynamic effects on the central nervous system.
Results from a phase IIb trial showed that encenicline (2.0mg once daily) significantly improved cognition and clinical function in patients with mild-to-moderate Alzheimer's disease.
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:46:38 GMT 2023
by
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on
Sat Dec 16 09:46:38 GMT 2023
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Record UNII |
VYV1YE9W06
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Record Status |
Validated (UNII)
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Record Version |
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550999-74-1
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VYV1YE9W06
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CHEMBL2151572
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300000044458
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ZZ-157
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C169947
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46208542
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DTXSID40673090
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DBSALT002058
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PARENT -> SALT/SOLVATE | |||
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SOLVATE->ANHYDROUS |
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ACTIVE MOIETY |