| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Naxagolide targets the dopamine D2 receptor, a G-protein coupled receptor that plays a critical role in regulating motor function, reward, and neuroendocrine secretion. The compound acts as a potent agonist at D2 receptors, mimicking the effects of endogenous dopamine. By activating D2 receptors in the striatum, Naxagolide helps to compensate for the dopaminergic deficit that occurs in Parkinson's disease.
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| ln Vitro |
Rat striatal membrane binding of [3H]apomorphine (IC50 = 23 nM) or [3H]spiperone (IC50 = 55 nM) is inhibited in vitro by naproxagolide ((+)-PHNO) [1].
In vitro, Naxagolide demonstrates potent agonist activity at dopamine D2 receptors. The compound binds to D2 receptors with high affinity and activates downstream signaling pathways, including inhibition of adenylyl cyclase and modulation of potassium and calcium channels. Its selectivity for D2 over other dopamine receptor subtypes contributes to its pharmacological profile. |
| ln Vivo |
Naxagolide ((+)-PHNO) induces postural asymmetry in unilaterally tailectomized mice (4 μg/kg ip) and hypothermia (13 μg/kg ip) [1]. Rats lesioned with 6-hydroxydopamine for one to three hours exhibit stereotypy (10 μg/kg ip) and contralateral turning (5 μg/kg ip) when administered Naxagolide ((+)-PHNO) [1].
In vivo, Naxagolide has been evaluated in animal models of Parkinson's disease. As a D2 receptor agonist, it has demonstrated the ability to reduce motor deficits in rodent and primate models of Parkinson's disease. The compound's efficacy in preclinical models supports its potential for treating motor symptoms in Parkinson's disease patients. |
| Enzyme Assay |
In vitro receptor binding assays for D2 receptor agonism involve incubating membranes from cells expressing recombinant human D2 receptors with radiolabeled ligands (e.g., [³H]spiperone or [³H]raclopride) and varying concentrations of Naxagolide. Non-specific binding is determined using excess unlabeled competitor. Bound radioactivity is measured by scintillation counting to calculate Ki values. Functional assays measure the compound's ability to inhibit forskolin-stimulated cAMP accumulation in D2-expressing cells.
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| Cell Assay |
Cellular assays are performed using cell lines expressing recombinant dopamine D2 receptors. Cells are treated with Naxagolide at various concentrations in the presence of forskolin. Intracellular cAMP levels are measured using a luminescent or fluorescent cAMP detection kit. The compound's potency as a D2 agonist is determined by measuring the inhibition of forskolin-stimulated cAMP accumulation.
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| Animal Protocol |
In vivo studies are conducted in rodent models of Parkinson's disease, such as the 6-hydroxydopamine (6-OHDA) lesioned rat model or the MPTP-treated mouse model. Naxagolide is administered orally, intraperitoneally, or subcutaneously at various doses. Motor function is assessed using behavioral tests such as rotational behavior, catalepsy, or locomotor activity.
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| ADME/Pharmacokinetics |
Dopamine receptor agonists like Naxagolide are typically small-molecule compounds with good oral bioavailability. Naxagolide (molecular weight 247.33, formula C₁₅H₂₁NO₂) is a lipophilic compound that can cross the blood-brain barrier. Its physicochemical properties support its use in both in vitro and in vivo studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies have evaluated Naxagolide in animal models. As a dopamine D2 agonist, its toxicity profile is related to dopaminergic stimulation, including potential effects on the cardiovascular system, gastrointestinal tract, and neuroendocrine function. No significant toxicity has been reported at therapeutic doses.
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| References |
[1]. 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]. 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 |
Neusagolide is an organic heterocyclic tricyclic compound with the structure (4aR,10bR)-3,4,4a,5,6,10b-hexahydro-2H-naphtho[1,2-b][1,4]oxazine, with propyl and hydroxyl groups substituted at positions 4 and 9, respectively. It is a potent dopamine D2 receptor agonist, and its hydrochloride salt was clinically developed by Merck as a potential anti-Parkinson's disease drug (now discontinued). It possesses pharmacological effects of anti-Parkinson's disease, dopamine agonism, and anticonvulsant activity. It is a tertiary amine compound, an organic heterocyclic tricyclic compound, and belongs to the phenolic class of compounds. It is the conjugate base of neusagolide (1+).
Naxagolide ((+)-PHNO; Dopazinol) is a potent dopamine D2 receptor agonist developed for the treatment of Parkinson's disease. Its mechanism involves activating D2 receptors to compensate for the dopaminergic deficit in the striatum. The compound has been investigated in clinical trials for Parkinson's disease but has not received regulatory approval for widespread clinical use. It remains a research tool for studying dopamine receptor function and Parkinson's disease pathophysiology. |
| Molecular Formula |
C15H21NO2
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| Molecular Weight |
247.33274
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| Exact Mass |
247.157
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| Elemental Analysis |
C, 72.84; H, 8.56; N, 5.66; O, 12.94
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| CAS # |
88058-88-2
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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 |
57533
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
391.7±42.0 °C at 760 mmHg
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| Flash Point |
190.7±27.9 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.553
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| LogP |
2.55
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
284
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CCCN1CCOC2C1CCC3=C2C=C(C=C3)O
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| InChi Key |
JCSREICEMHWFAY-HUUCEWRRSA-N
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| InChi Code |
InChI=1S/C15H21NO2/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/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
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| Synonyms |
PHNO; Dopazinol; NAXAGOLIDE; dopazinol; 88058-88-2; Nazagolide; Naxagolida; (+)-Propyl-hexahydro-naphtho-oxazin;
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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) |
DMSO : ~200 mg/mL (~808.64 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 | 4.0432 mL | 20.2159 mL | 40.4318 mL | |
| 5 mM | 0.8086 mL | 4.0432 mL | 8.0864 mL | |
| 10 mM | 0.4043 mL | 2.0216 mL | 4.0432 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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