An alkaloid and a partial agonist of nAChRs (EC50 = 1 µM for α4β2 subunit-containing nAChRs expressed in Xenopus oocytes); inhibits current induced by acetylcholine by 50% in Xenopus oocytes expressing α4β2-subunit containing nAChRs at 20 nM; binds to α2β2

Cytisine – 100 mg

Brand:
Cayman
CAS:
485-35-8
Storage:
-20
UN-No:
- 1544 / 6.1

Cytisine is an alkaloid that has been found in C. laburnum.{47481} It is a partial agonist of nicotinic acetylcholine receptors (nAChRs) with an EC50 value of approximately 1 µM for increasing current in Xenopus oocytes expressing α4β2 subunit-containing nAChRs. Cytisine (20 nM) inhibits current induced by acetylcholine (Item No. 23829) by 50% in Xenopus oocytes expressing α4β2-subunit containing nAChRs. It binds to α2β2, α2β4, α3β2, α3β4, α4β2, and α4β4 nAChR subunits expressed in HEK293 cells with Ki values of 1.1, 5.4, 37, 220, 1.5, and 2.1 nM, respectively.{27175} Cytisine (3 mg/kg) reduces increases in the intracranial self-stimulation (ICSS) threshold of rats withdrawing from nicotine self-administration, indicating a decrease in the dysphoric state induced by nicotine withdrawal.{47482}  

 

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Description

An alkaloid and a partial agonist of nAChRs (EC50 = 1 µM for α4β2 subunit-containing nAChRs expressed in Xenopus oocytes); inhibits current induced by acetylcholine by 50% in Xenopus oocytes expressing α4β2-subunit containing nAChRs at 20 nM; binds to α2β2, α2β4, α3β2, α3β4, α4β2, and α4β4 nAChR subunits (Kis = 1.1, 5.4, 37, 220, 1.5, and 2.1 nM, respectively); reduces increases in the ICSS threshold of nicotine-withdrawing rats at 3 mg/kg

Formal name: (1R,5S)-1,2,3,4,5,6-hexahydro-1,5-methano-8H-pyrido[1,2-a][1,5]diazocin-8-one

Synonyms:  Baptitoxine|Cytiton|Laburnin|Sophorine|Tsitafat

Molecular weight: 190.2

CAS: 485-35-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Activators||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research

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