Catalog Number
ACM252870534
Description
Ispronicline, also known as AZD3480; TC 1734; TC-0173, and RJR 1734, is a alpha4beta2 nicotinic acetylcholine receptor-selective agonist with cognition-enhancing and neuroprotective properties. Ispronicline is potentially useful for the treatment of attention-deficit/hyperactivity disorder in adults.
Synonyms
Ispronicline; AZD3480; AZD-3480; AZD 3480; TC 1734; TC-01734; TC1734; TC01734; TC 1734; TC 01734; RJR 1734; RJR-1734; RJR1734
IUPAC Name
(S,E)-5-(5-isopropoxypyridin-3-yl)-N-methylpent-4-en-2-amine
Molecular Formula
C14H22N2O
Canonical SMILES
C[C@H](NC)C/C=C/C1=CC(OC(C)C)=CN=C1
InChI
InChI=1S/C14H22N2O/c1-11(2)17-14-8-13(9-16-10-14)7-5-6-12(3)15-4/h5,7-12,15H,6H2,1-4H3/b7-5+/t12-/m0/s1
InChI Key
RPCVIAXDAUMJJP-PZBABLGHSA-N
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Alternative CAS
252870-53-4 (free base); 252870-54-5 (hemigalactarate); 957106-98-8 (phosphate); 957107-01-6 (citrate)
Biological Target
Ispronicline (TC-1734) is a brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist that binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR.
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 71.76; H, 9.46; N, 11.95; O, 6.83
HS Tariff Code
2934.99.9001
In Vivo Activity
Adult female Sprague-Dawley rats were trained to perform an operant visual signal detection task to a stable baseline of accuracy. The rats were then injected subcutaneously following a repeated measures, counter-balanced design with saline, AZD3480 (0.01, 0.1, and 1 mg/kg), dizocilpine (0.05 mg/kg), or their combinations 30 min before the test. Dizocilpine caused a significant (p < 0.0005) impairment in percent correct performance. This attentional impairment was significantly (p < 0.0005) reversed by 0.01 and 0.1 mg/kg of AZD3480. AZD3480 by itself did not alter the already high baseline control performance. AZD3480 also showed significant efficacy for counteracting the attentional impairment caused by the NMDA glutamate antagonist dizocilpine. Low doses of AZD3480 may provide therapeutic benefit for reversing attentional impairment in patients suffering from cognitive impairment due to glutamatergic dysregulation and likely other attentional disorders.
Reference: Psychopharmacology (Berl). 2012 Oct;223(3):251-8. https://pubmed.ncbi.nlm.nih.gov/22526540/
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).
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