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

Nelonicline 

Cat. No.: HY-16748
Handling Instructions

Nelonicline is a selective neuronal nicotinic receptor agonist.

For research use only. We do not sell to patients.

Nelonicline Chemical Structure

Nelonicline Chemical Structure

CAS No. : 1026134-63-3

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Nelonicline is a selective neuronal nicotinic receptor agonist.

IC50 & Target

neuronal nicotinic receptor[1].

In Vivo

The 0.03 mg/kg dose Nelonicline has no significant effect on LIDs. ABT-126 at 0.10 mg/kg reduces LIDs by ~40%, while the 0.30 and 1.0 mg/kg ABT-126 doses decrease LIDs up to ~60%. The effect of Nelonicline (1.0 mg/kg) is also tested for its ability to reduce LIDs at a higher dose of L-dopa (15 mg/kg)/carbidopa (3.75 mg/kg). The higher dose of L-dopa leads to greater LID scores in vehicle treated monkeys. Nelonicline treatment reduces LIDs by 70%, after the morning dose of L-dopa and 60% after the aftemoon dose. The effect of Nelonicline is most pronounced during the latter weeks, possibly because of a greater decline with continued drug treatment. A washout is in progress to determine if LIDs return to vehicle-treated levels after Nelonicline discontinuation. There is no effect of the drug on Parkinsonism or cognitive ability. Overall, these data indicate that Nelonicline would be useful as an antidyskinetic drug in Parkinson's disease[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1906 mL 15.9530 mL 31.9061 mL
5 mM 0.6381 mL 3.1906 mL 6.3812 mL
10 mM 0.3191 mL 1.5953 mL 3.1906 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Monkeys[1]
MPTP-lesioned monkeys are used. All monkeys have been administered MPTP and exhibited mild to moderate parkinsonism. All monkeys are orally gavaged with L-dopa/carbidopa twice daily, which lead to the development of stable abnormal involuntary movements or dyskinesias. The treatment groups are as follows: vehicle-treated (n=6), nicotine-treated (n=5), Nelonicline treated (set 1, n=5) and Nelonicline-treated (set 2, n=5). These latter two sets of monkeys have previously been given ABT-894 and ABT-107 but using somewhat different treatment regimens. The present study is done after a 7 wk washout period, when LIDs are similar in all groups. Nelonicline is administered orally in a small cracker 30 min before L-dopa (10 mg/kg) and carbidopa (2.5 mg/kg). Nicotine, a positive control, is provided in the drinking water. Nelonicline is tested at 0.03, 0.10, 0.30 and 1.0 mg/kg, with each dose of Nelonicline tested for 1 or 2 wk[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

313.42

Formula

C₁₇H₁₉N₃OS

CAS No.

1026134-63-3

SMILES

[[email protected]]1([[email protected]]2C[[email protected]](C3)C[[email protected]@H]1C[[email protected]]3C2)OC4=NN=C(C5=CC=CC=C5)S4

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Nelonicline
Cat. No.:
HY-16748
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Nelonicline

Cat. No.: HY-16748