| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
Apomorphine HCl hydrate acts primarily as a dopamine D2 receptor agonist in the central nervous system. It stimulates dopamine receptors in the nigrostriatal system, hypothalamus, limbic system, pituitary gland, and blood vessels. The compound also acts on D2 receptors in the chemoreceptor trigger zone (CTZ) in the medulla oblongata, stimulating the CTZ and exciting the vomiting center to produce emetic activity. Apomorphine is structurally related to dopamine.
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| ln Vitro |
In vitro, apomorphine hydrochloride demonstrates high binding affinity for dopamine D2 receptors. It acts as a direct dopamine receptor agonist. The compound shows activity at both central and peripheral dopamine receptors. Its emetic activity is mediated through stimulation of the chemoreceptor trigger zone. The in vitro potency of apomorphine at D2 receptors has been well characterized in radioligand binding assays using striatal membrane preparations.
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| ln Vivo |
In vivo, apomorphine hydrochloride reduces tremor, rigidity, and bradykinesia in patients receiving levodopa for Parkinson's disease. It enhances motor function by stimulating dopamine receptors in the nigrostriatal system. The compound induces vomiting through direct stimulation of the medullary chemoreceptor trigger zone. Its emetic effect is powerful and has been utilized in acute poisoning management. Apomorphine is used in the treatment of Parkinson's disease and erectile dysfunction.
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| Enzyme Assay |
General protocols for dopamine receptor binding assays use rat striatal membranes prepared by homogenization in 50 mM Tris-HCl buffer pH 7.4 containing 120 mM NaCl, 5 mM KCl, 2 mM CaCl2, and 1 mM MgCl2. Membranes are incubated with [3H]spiperone or [3H]raclopride (D2-selective ligands) and varying concentrations of apomorphine at 25°C for 30-60 minutes. Nonspecific binding is determined using 10 μM haloperidol. Bound ligand is separated by rapid filtration through GF/B filters and counted by scintillation. Ki values are calculated from competition curves using the Cheng-Prusoff equation.
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| Cell Assay |
General protocols for dopamine D2 receptor functional assays use cells expressing recombinant D2 receptors (e.g., CHO cells). Cells are seeded in 96-well plates and loaded with Fluo-4 or other calcium-sensitive dyes. Apomorphine is added at various concentrations, and intracellular calcium release is measured using a fluorescence plate reader. The EC50 for receptor activation is calculated from dose-response curves. Alternatively, cAMP accumulation assays measure inhibition of forskolin-stimulated cAMP production via D2 receptor-mediated Gi activation.
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| Animal Protocol |
General protocols for in vivo Parkinson's disease models use the 6-OHDA-lesioned rat model. Rats are unilaterally lesioned with 6-hydroxydopamine in the medial forebrain bundle. After recovery, apomorphine is administered subcutaneously at doses of 0.05-1.0 mg/kg, and rotational behavior (contralateral rotations) is quantified over 30-60 minutes. The number of rotations serves as a measure of dopamine receptor activation and motor response. ED50 values are calculated from dose-response data. Apomorphine-induced emesis is evaluated in dogs or ferrets.
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| ADME/Pharmacokinetics |
Apomorphine HCl hydrate has a rapid onset of action with a short duration of effect due to extensive first-pass metabolism. The compound is administered subcutaneously, sublingually, or via injection for Parkinson's disease management. The bioavailability of oral apomorphine is poor, necessitating parenteral administration. Metabolism occurs primarily in the liver via conjugation and oxidation. The elimination half-life is approximately 40 minutes. The compound crosses the blood-brain barrier readily, consistent with its central nervous system effects.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation There is currently no information regarding the use of apomorphine during lactation. If a mother needs to use apomorphine, this is not a reason to stop breastfeeding. However, apomorphine inhibits the release of prolactin in animals and may interfere with the establishment of lactation. Especially when breastfeeding newborns or premature infants, other medications should be preferred. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information found as of the revision date. Apomorphine hydrochloride has a well-documented toxicity profile. Common adverse effects include nausea, vomiting, and orthostatic hypotension. Its powerful emetic effect limits its use in some patients. CNS effects include drowsiness, dizziness, and confusion. At high doses, respiratory depression may occur. The compound should be used with caution in patients with cardiovascular disease or those taking antihypertensive medications. Contraindications include severe cardiovascular disease and known hypersensitivity. |
| Additional Infomation |
Apomorphine hydrochloride is the hydrochloride form of apomorphine, a derivative of morphine. It is a non-ergot dopamine agonist with high selectivity for dopamine D2, D3, D4, and D5 receptors. Apomorphine hydrochloride exerts its effects by stimulating dopamine receptors in the substantia nigra-striatal system, hypothalamus, limbic system, pituitary gland, and blood vessels. This can enhance motor function, inhibit prolactin release, and induce vasodilation and behavioral changes. Apomorphine hydrochloride is used to treat Parkinson's disease and erectile dysfunction. Additionally, apomorphine hydrochloride acts on chemoreceptor trigger zones and can be used as a centrally acting emetic for drug overdose. Morphine, a dopamine D2 receptor agonist, is a potent emetic and has been used to treat acute poisoning. It has also been used for the diagnosis and treatment of Parkinson's disease, but its adverse effects limit its application.
See also: Apomorphine (contains the active ingredient)...View more... Drug Indications Treatment of erectile dysfunction in men, i.e., the inability to achieve or maintain an erection sufficient for satisfactory sexual intercourse. Uprima requires sexual stimulation to be effective. Treatment of erectile dysfunction in men, i.e., the inability to achieve or maintain an erection sufficient for satisfactory sexual intercourse. Taluvian requires sexual stimulation to be effective. Treatment of erectile dysfunction in men, i.e., the inability to achieve or maintain an erection sufficient for satisfactory sexual intercourse. Ixense requires sexual stimulation to be effective. Apomorphine HCl hydrate is approved for the treatment of Parkinson's disease (subcutaneous injection) and for the treatment of male erectile dysfunction. It is also used as a central emetic in the treatment of drug overdose. The compound is available as a hydrochloride hemihydrate salt. It is classified as a dopamine receptor agonist. Clinical use is limited by its adverse effect profile, particularly nausea and vomiting. Regulatory approvals vary by country and indication. |
| Molecular Formula |
C34H38CL2N2O5
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|---|---|
| Molecular Weight |
625.587
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| Exact Mass |
321.113
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| CAS # |
41372-20-7
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| Related CAS # |
58-00-4;314-19-2 (HCl);41372-20-7 (HCl hydrate);41035-30-7 (S-isomer HCl); 39478-62-1 (S-isomer);
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| PubChem CID |
107882
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.299 g/cm3
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| Boiling Point |
473.4ºC at 760 mmHg
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| Melting Point |
285-287 °C(lit.)
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| Flash Point |
268.8ºC
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| LogP |
3.525
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
43
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| Complexity |
374
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CN1CCC2=C3C(=CC=C2)C4=C(C=CC(=C4O)O)C[C@H]31.CN1CCC2=C3C(=CC=C2)C4=C(C=CC(=C4O)O)C[C@H]31.Cl.Cl.O
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| InChi Key |
CXWQXGNFZLHLHQ-DPFCLETOSA-N
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| InChi Code |
InChI=1S/2C17H17NO2.2ClH.H2O/c2*1-18-8-7-10-3-2-4-12-15(10)13(18)9-11-5-6-14(19)17(20)16(11)12/h2*2-6,13,19-20H,7-9H2,1H32*1H1H2/t2*13-/m11.../s1
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| Chemical Name |
(R)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol hydrochloride hemihydrate
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| Synonyms |
Apomorphine HydrochlorideApomorphine HClAPL-130277TAK-251TAK251TAK 251APL130277APL 130277KW-6500KW 6500KW6500ND-0701ND 0701ND0701Apomorphine HCl hydrate Apmorphine hydrochloride hemihydrate ApokynVR-004VR 004VR004VR-040VR 040VR040
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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 | 1.5985 mL | 7.9925 mL | 15.9849 mL | |
| 5 mM | 0.3197 mL | 1.5985 mL | 3.1970 mL | |
| 10 mM | 0.1598 mL | 0.7992 mL | 1.5985 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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