Cytisine

Cytisine

CAT N°: 26437
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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 ?4?2 subunit-containing nAChRs. Cytisine (20 nM) inhibits current induced by acetylcholine (Item No. 23829) by 50% in Xenopus oocytes expressing ?4?2-subunit containing nAChRs. It binds to ?2?2, ?2?4, ?3?2, ?3?4, ?4?2, and ?4?4 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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