| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g | |||
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| Targets |
Lobeline hydrochloride targets nicotinic acetylcholine receptors (nAChRs) and dopamine transporters (DAT). It acts as a partial agonist at nAChRs and inhibits dopamine uptake via DAT. These mechanisms are similar to those of other compounds used in addiction research. Lobeline's interaction with nAChRs and DAT makes it of interest for studying nicotine addiction and other substance use disorders. It also has respiratory stimulant effects, likely mediated through its action on nAChRs in the respiratory center.
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| ln Vitro |
In a calcium-independent way, lobeline (0.1-100 μM) hydrochloride stimulates [3H]DA salvage [1]. [3H]DA is inhibited by lobeline hydrochloride via vesicles (IC50=0.88 μM) and synaptosomes (IC50=80 μM). food [1].
In vitro, Lobeline hydrochloride displaces radiolabeled ligands from nAChR binding sites and inhibits dopamine uptake in synaptosomes or cells expressing DAT. It modulates dopamine release in brain slice preparations. It also shows activity at other receptors, including serotonin and opioid receptors. Detailed IC50 values for these activities are not extensively reported in the available literature. |
| ln Vivo |
A single subcutaneous injection of lobeline hydrochloride (0.3–3.0 mg/kg) decreases the model's capacity to self-medicate with d-methamphetamine reserve [3]. notably promotes tolerance development and non-competitively reduces d-methamphetamine responses [3].
In vivo, Lobeline hydrochloride has been studied for its respiratory stimulant effects and its potential in treating addiction. It has been investigated in animal models of nicotine self-administration and conditioned place preference, where it may reduce drug-seeking behavior. It has also been studied for its effects on respiratory depression. Detailed in vivo efficacy data are not extensively reported. |
| Enzyme Assay |
Non-cell-based receptor binding assays for Lobeline hydrochloride use membrane preparations from brain tissue or cells expressing nAChRs or DAT. The compound is incubated with radiolabeled ligands (e.g., [3H]-nicotine for nAChRs, [3H]-WIN 35,428 for DAT) at varying concentrations. Binding affinity (IC50 or Ki) is determined by measuring displacement of the radiolabeled ligand. Selectivity for different receptor subtypes can be assessed.
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| Cell Assay |
Cellular assays for Lobeline hydrochloride utilize cell lines expressing nAChRs or DAT. For nAChR activity, electrophysiological techniques (patch-clamp) or calcium imaging are used. For DAT activity, dopamine uptake assays are performed using cells expressing DAT and radiolabeled dopamine. Dopamine release can be measured in brain slice preparations or in cultured neurons.
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| Animal Protocol |
Animal/Disease Models: SD (SD (Sprague-Dawley)) rat (200-250 g) [3]
Doses: 0.3 mg/kg, 1.0 mg/kg and 3.0 mg/kg for acute administration; 3 mg/kg for chronic administration Doses: subcutaneous injection; 15 minutes before measurement, or every 15 minutes for a total of 7 injections; separated by 2 maintenance days of d-methamphetamine self-administration (0.05 mg/kg/infusion) Experimental Results: d-methamphetamine self-administration The dose is diminished. In vivo animal models for Lobeline hydrochloride include models of addiction (e.g., nicotine self-administration, conditioned place preference) and models of respiratory depression. The compound is administered via appropriate routes. Drug-seeking behavior is assessed using operant conditioning or other behavioral paradigms. Respiratory parameters (respiratory rate, tidal volume) are measured. Detailed protocols are not extensively reported. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Lobeline hydrochloride include CAS number 134-63-4. The compound is a small molecule piperidine alkaloid. Detailed PK parameters such as molecular weight, half-life, bioavailability, and solubility are not extensively reported in the available literature. The compound is supplied as a research reagent for laboratory use only.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for Lobeline hydrochloride are not extensively reported in the available literature. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is supplied for research use only. Given its mechanism of nAChR modulation and DAT inhibition, potential effects on the CNS and cardiovascular system would be key safety considerations.
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| References |
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| Additional Infomation |
See also: Lobeline (note moved to).
Mechanism of Action The pharmacological activity of two natural alkaloids, nicotine and lobeline, is primarily attributed to their effects on autonomic ganglia. …Lobeline has many of the same effects as nicotine in vivo, but with less potency. /Lobeline/ …Lobeline…acts similarly to nicotine and theobromine, first stimulating and then paralyzing autonomic ganglia. /Lobeline/ Therapeutic Uses It has been used as a respiratory stimulant; it has also been used to treat tobacco addiction. Water-soluble hydrochloride and sulfate have been administered via parenteral route. (Veterinary Drug) Used as a respiratory stimulant, for ruminants /Lobeline/ Lobeline hydrochloride is also known as C-07475. It has CAS number 134-63-4. It is a piperidine alkaloid from Lobelia inflata. It targets nicotinic acetylcholine receptors and dopamine transporters. It has been studied for its respiratory stimulant effects and potential in treating addiction. It is used as a research tool for studying cholinergic and dopaminergic signaling. It is for research use only. |
| Molecular Formula |
C22H28CLNO2
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|---|---|
| Molecular Weight |
373.9162
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| Exact Mass |
373.18
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| CAS # |
134-63-4
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| Related CAS # |
Lobeline sulfate;134-64-5;Lobeline;90-69-7
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| PubChem CID |
101615
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| Appearance |
White to off-white solid powder
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| Boiling Point |
485.6ºC at 760mmHg
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| Melting Point |
183-185 °C (dec.)(lit.)
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| Flash Point |
247.5ºC
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| Vapour Pressure |
3.02E-11mmHg at 25°C
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| Index of Refraction |
-57.5 ° (C=1, H2O)
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| LogP |
4.975
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
412
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CN1[C@@H](CCC[C@@H]1CC(=O)C2=CC=CC=C2)C[C@@H](C3=CC=CC=C3)O.Cl
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| InChi Key |
MKMYPTLXLWOUSO-NFQNBQCWSA-N
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| InChi Code |
InChI=1S/C22H27NO2.ClH/c1-23-19(15-21(24)17-9-4-2-5-10-17)13-8-14-20(23)16-22(25)18-11-6-3-7-12-18/h2-7,9-12,19-21,24H,8,13-16H2,1H31H/t19-,20+,21-/m0./s1
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| Chemical Name |
2-[(2R,6S)-6-[(2S)-2-Hydroxy-2-phenylethyl]-1-methylpiperidin-2-yl]-1-phenylethanone hydrochloride
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| Synonyms |
C-07475C 07475C07475α-Lobeline hydrochloride L-Lobeline hydrochloride
Lobeline HCl
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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 : ~6 mg/mL (~16.05 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 | 2.6744 mL | 13.3718 mL | 26.7437 mL | |
| 5 mM | 0.5349 mL | 2.6744 mL | 5.3487 mL | |
| 10 mM | 0.2674 mL | 1.3372 mL | 2.6744 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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