1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. nAChR
  3. Pozanicline

Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.

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Pozanicline

Pozanicline Estructura química

No. CAS : 161417-03-4

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Descripciòn

Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction[1].

IC50 & Target

Ki: 16 nM (α4β2* nAChR)[1]

Cellular Effect
Cell Line Type Value Description References
IMR-32 EC50
150 3
Compound: S-4 (ABT-089)
Concentration required to elicit ganglionic receptors measured using [86Rb+] flux functional assay in a human neuroblastoma-derived IMR-32 cell line
Concentration required to elicit ganglionic receptors measured using [86Rb+] flux functional assay in a human neuroblastoma-derived IMR-32 cell line
[PMID: 9022806]
IMR-32 EC50
150 3
Compound: S-4 (ABT-089)
Concentration required to elicit ganglionic receptors measured using [86Rb+] flux functional assay in a human neuroblastoma-derived IMR-32 cell line
Concentration required to elicit ganglionic receptors measured using [86Rb+] flux functional assay in a human neuroblastoma-derived IMR-32 cell line
[PMID: 9022806]
IMR-32 EC50
150 3
Compound: S-4 (ABT-089)
Concentration required to elicit ganglionic receptors measured using [86Rb+] flux functional assay in a human neuroblastoma-derived IMR-32 cell line
Concentration required to elicit ganglionic receptors measured using [86Rb+] flux functional assay in a human neuroblastoma-derived IMR-32 cell line
[PMID: 9022806]
Peso molecular

192.26

Fòrmula

C11H16N2O

No. CAS
SMILES

CC1=C(OC[C@H]2NCCC2)C=CC=N1

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
Pozanicline
Cat. No.:
HY-14565
Cantidad:
MCE Japan Authorized Agent: