| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Pachycarpine targets nicotinic acetylcholine receptors (nAChRs) in autonomic ganglia, where it acts as a competitive antagonist. By blocking nAChRs, pachycarpine inhibits synaptic transmission in autonomic ganglia, leading to effects on the parasympathetic and sympathetic nervous systems. The compound also modulates sodium channels. Its ganglionic blocking activity is responsible for its pharmacological effects, including its use as an antiarrhythmic agent. Pachycarpine has also been used as an oxytocic agent.
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| ln Vitro |
(+)-Sparteine (2 μM) decreases voltage-independent ACh-induced currents brought on by nicotinic AChR activation. (+)-Sparteine (5, 10 μM) diminishes both the time constant of EPSC decay and the amplitude of excitatory postsynaptic currents (EPSCs) [1].
In vitro, pachycarpine acts as a competitive antagonist of nicotinic acetylcholine receptors in neurons. It blocks ganglionic transmission by inhibiting nAChR activity. The compound also modulates sodium channels. Its ability to inhibit nAChR-mediated signaling has been demonstrated in electrophysiological studies using neuronal preparations. Pachycarpine's effects on autonomic ganglia have been characterized in various in vitro models. |
| ln Vivo |
In vivo, pachycarpine has been used as an oxytocic agent to stimulate uterine contractions and as an antiarrhythmic agent to treat cardiac arrhythmias. Its ganglionic blocking activity mediates its pharmacological effects on the cardiovascular and reproductive systems. However, specific in vivo efficacy data in animal models are not extensively detailed in the available literature. The compound is a naturally occurring alkaloid with a long history of use in medicine.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for pachycarpine are radioligand binding assays using membrane preparations from tissues expressing nicotinic acetylcholine receptors, such as brain or muscle. The compound's binding affinity is determined by its ability to displace a labeled nAChR ligand such as [3H]epibatidine or [3H]nicotine. Functional assays such as electrophysiological recordings can also be used to measure the compound's antagonist activity at nAChRs.
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| Cell Assay |
In vitro cellular assays for pachycarpine are performed using cell lines expressing nicotinic acetylcholine receptors or primary neuronal cultures. Cells are treated with pachycarpine, and nAChR-mediated ion currents are measured using patch-clamp electrophysiology. The compound's ability to inhibit nAChR-mediated calcium influx or other downstream signaling events is assessed. These assays confirm the functional antagonism of pachycarpine at nAChRs.
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| Animal Protocol |
In vivo animal experiments for pachycarpine have been conducted to evaluate its antiarrhythmic and oxytocic effects. Animal models of cardiac arrhythmias may be used to assess the compound's antiarrhythmic efficacy. Uterine contraction models may be used to evaluate its oxytocic effects. However, specific in vivo experimental details are not extensively detailed in the available literature. The compound is a research tool for studying ganglionic transmission.
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| ADME/Pharmacokinetics |
Pachycarpine has a molecular weight of 234.38 g/mol and a molecular formula of C15H26N2. The compound is a liquid with a refractive index of n/D 1.527. It is soluble in organic solvents. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported. As an alkaloid, pachycarpine is expected to be absorbed after oral or parenteral administration and to cross the blood-brain barrier.
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| Toxicity/Toxicokinetics |
Pachycarpine has been associated with potential toxicity. It is classified as acute toxic category 4 for dermal, inhalation, and oral routes. The compound may cause adverse effects including nausea, vomiting, hypotension, and bradycardia due to its ganglionic blocking activity. Comprehensive toxicology studies would be necessary to fully assess its safety for clinical use. The compound is a naturally occurring alkaloid with a narrow therapeutic index.
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| References | |
| Additional Infomation |
(+)-Sparteine has been reported to be present in lupins, beech, and other organisms for which data are available. It is a quinolinic acid alkaloid isolated from several leguminous plants, including lupins; spartim; and CYTISUS. It has been used as an oxytocin and antiarrhythmic agent. It has also attracted interest as an indicator of the CYP2D6 genotype. See also: Sparteine (note moved to).
Pachycarpine is a naturally occurring alkaloid that acts as a ganglionic blocking agent by competitively inhibiting nicotinic acetylcholine receptors. It has been used as an oxytocic agent to stimulate uterine contractions and as an antiarrhythmic agent. Pachycarpine also modulates sodium channels. It is also known as (+)-sparteine and is a research compound for studying ganglionic transmission and autonomic pharmacology. |
| Molecular Formula |
C15H26N2
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| Molecular Weight |
234.387
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| Exact Mass |
234.209
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| CAS # |
492-08-0
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| Related CAS # |
(+)-Sparteine sulfate pentahydrate;(-)-Sparteine;90-39-1;(-)-Sparteine sulfate;299-39-8
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| PubChem CID |
7014
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| Appearance |
Colorless to light yellow liquid
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
340.9±10.0 °C at 760 mmHg
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| Melting Point |
201ºC
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| Flash Point |
148.3±6.8 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.570
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| LogP |
3.21
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
17
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| Complexity |
263
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| Defined Atom Stereocenter Count |
4
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| SMILES |
N12C([H])([H])C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])[C@@]1([H])C([H])([H])N3C([H])([H])C([H])([H])C([H])([H])C([H])([H])[C@]3([H])[C@@]([H])(C2([H])[H])C1([H])[H]
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| InChi Key |
SLRCCWJSBJZJBV-TUVASFSCSA-N
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| InChi Code |
InChI=1S/C15H26N2/c1-3-7-16-11-13-9-12(14(16)5-1)10-17-8-4-2-6-15(13)17/h12-15H,1-11H2/t12-,13-,14-,15+/m1/s1
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| Chemical Name |
(1R,2S,9R,10R)-7,15-diazatetracyclo[7.7.1.02,7.010,15]heptadecane
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| Synonyms |
d-Sparteine; (+)-Sparteine; Pachycarpine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~2.5 mg/mL (~10.67 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2664 mL | 21.3320 mL | 42.6639 mL | |
| 5 mM | 0.8533 mL | 4.2664 mL | 8.5328 mL | |
| 10 mM | 0.4266 mL | 2.1332 mL | 4.2664 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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