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| Targets |
ent Naxagolide HCl targets the dopamine D2 receptor, a G protein-coupled receptor that plays a critical role in motor control, reward, and cognition. As a potent and selective dopamine D2 receptor agonist, ent Naxagolide HCl stimulates the release of dopamine in the brain, activating D2 receptor-mediated signaling. This activation leads to the inhibition of adenylyl cyclase and modulation of neuronal excitability, which helps to restore dopamine-mediated neurotransmission in Parkinson's disease. The compound also has high affinity for the serotonin 5-HT1A receptor.
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| ln Vitro |
In vitro, ent Naxagolide HCl acts as a potent and selective dopamine D2 receptor agonist. It stimulates dopamine receptor-mediated signaling, which can be measured by inhibition of cAMP accumulation in cells expressing D2 receptors. The compound also shows high affinity for the serotonin 5-HT1A receptor. Its ability to activate D2 receptors has been confirmed in various cell-based assays.
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| ln Vivo |
In vivo, ent Naxagolide HCl is used for the treatment of extrapyramidal disorders and has antiparkinsonian activity. It has pharmacological effects as an anticonvulsant and anti-Parkinson's disease agent. However, specific in vivo efficacy data in animal models are not extensively detailed in the available literature. The compound is a research tool for studying dopamine D2 receptor signaling in Parkinson's disease and other neurological disorders.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for ent Naxagolide HCl are radioligand binding assays using membrane preparations from cells expressing recombinant dopamine D2 receptors or serotonin 5-HT1A receptors. The compound's binding affinity (Ki) is determined by its ability to displace a labeled receptor ligand such as [3H]spiperone or [3H]8-OH-DPAT. Functional assays such as cAMP accumulation assays are used to measure the compound's agonist activity at D2 receptors.
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| Cell Assay |
In vitro cellular assays for ent Naxagolide HCl are performed using cell lines expressing dopamine D2 receptors or serotonin 5-HT1A receptors. Cells are treated with varying concentrations of ent Naxagolide HCl, and receptor activation is assessed by measuring the inhibition of forskolin-stimulated cAMP accumulation (since D2 receptors are Gi-coupled). The EC50 for inhibition of cAMP accumulation is determined from dose-response curves.
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| Animal Protocol |
In vivo animal experiments for ent Naxagolide HCl are conducted in rodent models of Parkinson's disease, such as the 6-hydroxydopamine (6-OHDA)-lesioned rat model. Animals are administered ent Naxagolide HCl via oral or subcutaneous injection, and motor function is assessed using behavioral tests such as rotational behavior or locomotor activity. Anticonvulsant activity is evaluated in models of seizures. However, detailed protocols are not extensively documented in the available literature.
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| ADME/Pharmacokinetics |
ent Naxagolide HCl has a molecular weight of approximately 297.82 g/mol and a molecular formula of C14H19NO2·HCl. It is a dopamine D2 receptor agonist with high affinity for the serotonin 5-HT1A receptor. The compound should be stored under recommended conditions. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported. As a research compound, ent Naxagolide HCl is primarily used in preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicological profile of ent Naxagolide HCl has not been extensively characterized. As a dopamine D2 receptor agonist, the compound may have potential side effects including nausea, dizziness, and psychiatric symptoms such as hallucinations and impulse control disorders. No significant toxicity has been reported in the available literature. Standard toxicology studies would be necessary to establish its safety profile.
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| References |
[1]. G E Martin, et al. Pharmacologic profile of a novel potent direct-acting dopamine agonist, (+)-4-propyl-9-hydroxynaphthoxazine [(+)-PHNO]. J Pharmacol Exp Ther. 1984 Sep;230(3):569-76.
[2]. E F Domino, et al. Relative potency and efficacy of some dopamine agonists with varying selectivities for D1 and D2 receptors in MPTP-induced hemiparkinsonian monkeys. J Pharmacol Exp Ther. 1993 Jun;265(3):1387-91. |
| Additional Infomation |
Naxagol hydrochloride is the hydrochloride salt of Naxagol. It has pharmacological effects as an anticonvulsant, anti-Parkinson's disease agent, and dopamine agonist. It contains Naxagol (1+) molecules.
See also: Naxagol (note moved here). ent Naxagolide HCl is a potent and selective dopamine D2 receptor agonist used for the treatment of extrapyramidal disorders. It is also known as (-)-PHNO hydrochloride. The compound has pharmacological effects as an anticonvulsant and anti-Parkinson's disease agent. ent Naxagolide HCl also has a high affinity for the serotonin 5-HT1A receptor. It is a research compound and is not an approved drug. |
| Molecular Formula |
C15H22CLNO2
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| Molecular Weight |
283.79
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| Exact Mass |
283.134
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| Elemental Analysis |
C, 63.48; H, 7.81; Cl, 12.49; N, 4.94; O, 11.28
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| CAS # |
100935-99-7
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| Related CAS # |
99705-65-4 (HCl);88058-88-2;100935-99-7 (S-isomer HCl);
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| PubChem CID |
57532
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.23
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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 |
2
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| Heavy Atom Count |
19
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| Complexity |
284
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| Defined Atom Stereocenter Count |
2
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| SMILES |
Cl.CCCN1CCO[C@@H]2C3C=C(O)C=CC=3CC[C@@H]12
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| InChi Key |
NNEACMQMRLNNIL-CTHHTMFSSA-N
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| InChi Code |
InChI=1S/C15H21NO2.ClH/c1-2-7-16-8-9-18-15-13-10-12(17)5-3-11(13)4-6-14(15)16;/h3,5,10,14-15,17H,2,4,6-9H2,1H3;1H/t14-,15-;/m1./s1
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| Chemical Name |
(4aR,10bR)-4-propyl-2,3,4a,5,6,10b-hexahydrobenzo[h][1,4]benzoxazin-9-ol;hydrochloride
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| Synonyms |
ent Naxagolide Hydrochloride
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.5237 mL | 17.6187 mL | 35.2373 mL | |
| 5 mM | 0.7047 mL | 3.5237 mL | 7.0475 mL | |
| 10 mM | 0.3524 mL | 1.7619 mL | 3.5237 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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