TC-2216

Identification

Generic Name
TC-2216
DrugBank Accession Number
DB06044
Background

TC-2216 is an investigational novel small molecule that is being developed as an oral treatment for depression and anxiety disorders. TC-2216 showed greater potency than and anti-depressant effects comparable to selective serotonin reuptake inhibitors and tricyclics, which are commonly used treatments for depression, as well as anxiety-relieving effects.

Type
Small Molecule
Groups
Investigational
Structure
Weight
Average: 239.75
Monoisotopic: 239.1189253
Chemical Formula
C12H18ClN3
Synonyms
  • 1,7-DIAZASPIRO(4.4)NONANE, 7-(3-PYRIDINYL)-, HYDROCHLORIDE (1:3)
  • TC-2216 TRIHYDROCHLORIDE

Pharmacology

Indication

Investigated for use/treatment in anxiety disorders and depression.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

TC-2216 targets specific neuronal nicotinic receptors (NNRs), a class of receptors found in the central nervous system that play a critical role in regulating nervous system activity. TC-2216 selectively inhibits the alpha4beta2 NNR to modulate the release of neurotransmitters that are involved in mood regulation.

TargetActionsOrganism
UNeuronal acetylcholine receptor subunit alpha-4Not AvailableHumans
UNeuronal acetylcholine receptor subunit beta-2Not AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Not Available
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
N6H5AE63T5
CAS number
1159824-71-1
InChI Key
IKLDZHHQXNAQSS-UHFFFAOYSA-N
InChI
InChI=1S/C12H17N3.ClH/c1-3-11(9-13-6-1)15-8-5-12(10-15)4-2-7-14-12;/h1,3,6,9,14H,2,4-5,7-8,10H2;1H
IUPAC Name
SMILES
Cl.C1CNC2(C1)CCN(C2)C1=CN=CC=C1

References

General References
Not Available
ChemSpider
114868798
Wikipedia
TC-2216

Clinical Trials

Clinical Trials
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PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
1CompletedTreatmentHealthy Volunteers (HV)1somestatusstop reasonjust information to hide

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeable to sodium ions
Specific Function
Acetylcholine binding
Gene Name
CHRNA4
Uniprot ID
P43681
Uniprot Name
Neuronal acetylcholine receptor subunit alpha-4
Molecular Weight
69956.47 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeable to sodiun ions
Specific Function
Acetylcholine binding
Gene Name
CHRNB2
Uniprot ID
P17787
Uniprot Name
Neuronal acetylcholine receptor subunit beta-2
Molecular Weight
57018.575 Da

Drug created at November 18, 2007 18:29 / Updated at July 20, 2024 09:09