1217837-17-6
Chemical Structure
5-Iodo-A-85380 dihydrochloride
Synonym(s): 5-I A-85380 dihydrochloride
- CAS No.: 1217837-17-6
- Formula:C9H13Cl2IN2O
- Molecular Weight:363.02
IUPAC Name: (S)-3-(azetidin-2-ylmethoxy)-5-iodopyridine dihydrochloride
InChIKey: ZJVVFYWEBSHGBV-JZGIKJSDSA-N
SMILES: IC1=CC(OC[C@@H]2CCN2)=CN=C1.[H]Cl.[H]Cl
Biological Activity: 5-Iodo-A-85380 dihydrochloride (5-I A-85380 dihydrochloride) is a blood-brain barrier-permeable selective ligand for α4β2 nicotinic acetylcholine receptors (nAChR). The Ki of 5-Iodo-A-85380 dihydrochloride binding to rat α4β2 nAChRs is 0.01 nM. 5-Iodo-A-85380 dihydrochloride activates receptor currents, elicits single-channel currents, and promotes calcium influx, dopamine release, and calcium-dependent neuroprotection, acting as a full agonist at high-sensitivity α4β2 and a partial agonist at low-sensitivity α4β2 and α6-containing nAChRs. 5-Iodo-A-85380 dihydrochloride can be used for research on glutamate-induced neurotoxicity, pain, Alzheimer's disease, Parkinson's disease, schizophrenia, and attention deficit hyperactivity disorder[1][2][3][4][5][6][7][8].
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5-Iodo-A-85380 dihydrochloride | 98.97% | 5-Iodo-A-85380 dihydrochloride (5-I A-85380 dihydrochloride) is a blood-brain barrier-permeable selective ligand for α4β2 nicotinic acetylcholine receptors (nAChR). The Ki of 5-Iodo-A-85380 dihydrochloride binding to rat α4β2 nAChRs is 0.01 nM. 5-Iodo-A-85380 dihydrochloride activates receptor currents, elicits single-channel currents, and promotes calcium influx, dopamine release, and calcium-dependent neuroprotection, acting as a full agonist at high-sensitivity α4β2 and a partial agonist at low-sensitivity α4β2 and α6-containing nAChRs. 5-Iodo-A-85380 dihydrochloride can be used for research on glutamate-induced neurotoxicity, pain, Alzheimer's disease, Parkinson's disease, schizophrenia, and attention deficit hyperactivity disorder. | ||||||||||||||||||||
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References
- [1]. Li P, et al. The neuronal nicotinic α4β2 receptor has a high maximal probability of being open. British journal of pharmacology. 2010 Aug;160(8):1906-15. [Content Brief]
- [2]. Ueda M, et al. 5-Iodo-A-85380, a specific ligand for α4β2 nicotinic acetylcholine receptors, prevents glutamate neurotoxicity in rat cortical cultured neurons. Brain research. 2008 Mar 14;1199:46-52.
- [3]. Mukhin AG, et al. 5-Iodo-A-85380, an alpha4beta2 subtype-selective ligand for nicotinic acetylcholine receptors. Mol Pharmacol. 2000 Mar;57(3):642-9. [Content Brief]
- [4]. Akinola LS, et al. Pharmacological characterization of 5-iodo-A-85380, a β2-selective nicotinic receptor agonist, in mice. Journal of psychopharmacology (Oxford, England). 2022 Nov;36(11):1280-1293. [Content Brief]
- [5]. Pimlott SL, et al. Nicotinic acetylcholine receptor distribution in Alzheimer's disease, dementia with Lewy bodies, Parkinson's disease, and vascular dementia: in vitro binding study using 5-[(125)i]-a-85380. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2004 Jan;29(1):108-16.
- [6]. Harrington L, et al. Role of β4 Nicotinic Acetylcholine Receptors in the Habenulo-Interpeduncular Pathway in Nicotine Reinforcement in Mice. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2016 Jun;41(7):1790-802.
- [7]. Huang LZ, et al. Nicotinic receptor agonists decrease L-dopa-induced dyskinesias most effectively in partially lesioned parkinsonian rats. Neuropharmacology. 2011 May;60(6):861-8.
- [8]. Livingstone PD, et al. alpha7 and non-alpha7 nicotinic acetylcholine receptors modulate dopamine release in vitro and in vivo in the rat prefrontal cortex. The European journal of neuroscience. 2009 Feb;29(3):539-50.
