Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C9H11ClN2O.ClH |
Molecular Weight | 235.11 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.ClC1=NC=C(OC[C@H]2CCN2)C=C1
InChI
InChIKey=GYVARJONEFSAJB-OGFXRTJISA-N
InChI=1S/C9H11ClN2O.ClH/c10-9-2-1-8(5-12-9)13-6-7-3-4-11-7;/h1-2,5,7,11H,3-4,6H2;1H/t7-;/m1./s1
ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine] is a potent cholinergic neuronal nicotinic acetylcholine receptor (nAChR) ligand with analgesic properties. ABT-594 binds alpha-4/ beta-2 neuronal nAChRs acting as an agonist. ABT-594 is studying for the treatment of diabetic peripheral neuropathic pain.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1907589 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9580626 |
55.0 pM [Ki] | ||
Target ID: CHEMBL1907589 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9580626 |
55.0 pM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
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2.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19632048 |
300 μg 2 times / day multiple, oral dose: 300 μg route of administration: Oral experiment type: MULTIPLE co-administered: |
TEBANICLINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2.73 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19632048 |
300 μg 2 times / day multiple, oral dose: 300 μg route of administration: Oral experiment type: MULTIPLE co-administered: |
TEBANICLINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
22.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19632048 |
300 μg 2 times / day multiple, oral dose: 300 μg route of administration: Oral experiment type: MULTIPLE co-administered: |
TEBANICLINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
25 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19632048 |
300 μg 2 times / day multiple, oral dose: 300 μg route of administration: Oral experiment type: MULTIPLE co-administered: |
TEBANICLINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Sample Use Guides
Efficacy, safety and pharmacokinetics of ABT-594 in subjects with painful diabetic polyneuropathy were evaluated in a randomized, double-blind, placebo-controlled, parallel-group, multi-centre, 7-week Phase 2 study: subjects were approximately equally divided into four groups to receive BID regimens of placebo or 150, 225 and 300 ug of ABT-594.
ABT-894 was evaluated in 2 separate randomized, double-blind, multicenter, placebo-controlled clinical trials in patients with diabetic peripheral neuropathic pain. Study 1 (280 patients randomized) tested 1, 2, and 4 mg ABT-894 twice daily compared with placebo and 60 mg duloxetine once per day over 8 weeks of treatment. Study 2 (124 patients randomized) tested 6 mg ABT-894 twice daily vs placebo for 8 weeks.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9580626
ABT-594 (30 uM) inhibits the release of calcitonin gene-related peptide from C-fibers terminating in the dorsal horn of the spinal cord, an effect mediated via nAChRs.
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72193963
Created by
admin on Sat Dec 16 08:58:14 GMT 2023 , Edited by admin on Sat Dec 16 08:58:14 GMT 2023
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203564-54-9
Created by
admin on Sat Dec 16 08:58:14 GMT 2023 , Edited by admin on Sat Dec 16 08:58:14 GMT 2023
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m10497
Created by
admin on Sat Dec 16 08:58:14 GMT 2023 , Edited by admin on Sat Dec 16 08:58:14 GMT 2023
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48U2WUT775
Created by
admin on Sat Dec 16 08:58:14 GMT 2023 , Edited by admin on Sat Dec 16 08:58:14 GMT 2023
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PARENT (SALT/SOLVATE)
SUBSTANCE RECORD