Free sample high purity Cytisine /Sophorine /Cytisine

Free sample high purity Cytisine /Sophorine /Cytisine 

Molecular Formula : C11H14N2O

Molecular weight : 190.24

CAS NO.485-35-8

MOQ: 50grams

Sample policy :  free sample can be provided for checking .

Short brief : Cytisine, a naturally occurring bioactive compound isolated mainly extracted from Sophora alopecuroides、Sophora flavescens,Thermopsis lanceolata,Thermopsis chinensis,which has been marketed for over 50 years in Central and Eastern Europe as an aid to clinical management of smoking cessation. Its main target is the neuronal nicotinic acetylcholine receptors (nAChRs) and preclinical studies have shown that its interaction with various nAChR subtypes located in different regions of the central and peripheral nervous system has neuroprotective effects against nicotine and alcohol addiction, regulates mood, food intake and motor activity, and affects the autonomic and cardiovascular systems.

Fucntion of Cytisine :

1. 2.1 Nicotinic receptor binding

Nicotinic acetylcholine receptors (nAChRs) belong to the family of ligand-gated ion channels. It is divided into muscle-type receptors found at the skeletal neuromuscular junction and neuronal receptors found in the central and peripheral nervous system, but also in non-neuronal tissues. Neuronal nAChRs have a regulatory role in neurotransmitter release, synaptic efficacy and neuronal function. A total of 17 different nAChR subunits have been identified, and nicotinic receptors are pentamers of these subunits formed in different combinations. Heterodimers (α4)2(β2)3, (α3)2(β4)3 and homodimers (α7)5 are the most important subunits in the brain and they are named α4β2, α3β4 and α7. The large number of subunits and the various combinations of these subunits make the design of specific modulators difficult, the low abundance of some of these subunits in the brain and the lack of selective ligands to study the nAChRs in physiological and pathological conditions.

1. 1) nAChRs ligand-Cytisine

The binding characteristics of cytisine to brain membranes have been studied extensively since 1980. The dissociation constants (KD) of Cytisine nAChRs in rat brain were less than 1 nM, and the density of chrysoprase binding sites in rat cerebral cortex was similar to that of sites labelled with other nicotinic cholinergic agonist ligands, but with a higher affinity for Cytisine. The conclusions conclude that Cytisine is a key ligand for the quantification of neuronal nAChRs and suggest that Cytisine derivatives appropriately labelled with positron-emitting radionuclides may be useful for the study of nicotinic neurotransmission in human central nervous system emission tomography (PET)

2) Smoking cessation effects

Cytisine is a potent and competitive partial agonist of the α4β2 subunit, a receptor associated with nicotine dependence, and is the target of action of some smoking cessation preparations. Some studies have shown that smoking cessation preparations using the tartrate salt of cytisine as the main ingredient are up to 22% effective in quitting smoking over a one-year period. Whereas at alpha 7, it acts as a full agonist with lower effects, its physiological and behavioural effects are complex and different from those of nicotine . With a weak peripheral effect on the cardiovascular system, cystisine has a higher activity and lower oral toxicity than nicotine, making it a natural alternative to nicotine for smoking cessation.

2.2 Cytisine has the function of  Enhancement of myocardial contractility

Cytisine was effective in enhancing cardiac papillary muscle contractility and improving adrenaline-induced papillary muscle autoregulation, with no effect on its functional nonstop and excitability, while accelerating right atrial heart rate in guinea pigs

2.3 Cytisine with Excitatory respiratory effect

In anesthetized cats, intravenous administration of 0.02 mg/kg or 1.5 mg/cat resulted in a strong respiratory excitation and a rapid increase in heart rate and blood pressure, followed by a loss of respiratory excitation and a return to normal . It has been shown that the respiratory excitatory effect of auriculine 0.06 mg/kg is not only much stronger than that of santaline at the same dose, but also slightly stronger than that of santaline at 5 times the dose (0.3 mg/kg). Its derivative, methyl chrysoprine, has similar but weaker effects than cytisine.

2.4 Cytisine with Antidepressant effects

It has been shown that Cytisine is a partial agonist of the α4β2 nicotinic receptor and has antidepressant effects in chronically stressed animals. Experiments using mice as a model demonstrated that mice exhibited significant depressive behaviour after 5 weeks of unpredictable chronic mild stress, such as reduced locomotion and prolonged immobility in the tail suspension test and forced swimming test. Cytisine (1 mg/kg) reduced depressive-like behaviour in chronically stressed mice

2.5 Enhancing exercise capacity

Nicotine and other nAChRs receptor agonists enhance locomotor performance, and the locomotor activating effect of nicotine becomes more pronounced through repeated testing. It was demonstrated experimentally that cystisine administration to the ventral tegmental area also enhanced locomotor performance in rats, which may be due to substrates in the ventral tegmental area mediating the locomotor activation associated with systemic administration of nicotine, Cytisine and other nAChRs agonists

2.6 Improving cognitive function

Epidemiological studies have found a negative correlation between smoking, Parkinson's disease and the incidence of Alzheimer's disease. Nicotine enhances cognitive function and is thought to treat Alzheimer's disease. Scientists then speculated whether Cytisine could mimic nicotine to treat these diseases. Animal studies have concluded that Cytisine improves memory, with effects comparable to those of nicotine. Injection of the dopamine receptor antagonist (D1/D2) haloperidol had no effect on memory, but pre-administration of haloperidol blocked the memory-improving effects of Cytisine, a result that suggests that dopamine release may affect Cytisine's ability to improve cognitive function