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| 5mg |
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| Other Sizes |
| Targets |
The primary targets of Quinelorane hydrochloride are the dopamine D2 and D3 receptors, which are G protein-coupled receptors that play key roles in the regulation of movement, reward, cognition, and neuroendocrine function. Quinelorane hydrochloride acts as a full agonist at these receptors, exhibiting Ki values of 5.7 nM for D2 and 3.4 nM for D3 in radioligand binding assays. As a full agonist, it inhibits adenylate cyclase activity, leading to reduced cyclic AMP (cAMP) production. The compound provides a balanced D2/D3 profile, making it useful for studying the contributions of these receptors.
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| ln Vitro |
Quinelorane hydrochloride demonstrates potent in vitro agonist activity at dopamine D2 and D3 receptors, with Ki values of 5.7 nM and 3.4 nM, respectively. It is a full agonist that inhibits adenylate cyclase activity, leading to reduced cAMP production. The compound is used as a high-potency reference standard for behavioral and neurochemical studies. It shows superior potency in hypothermia and prepulse inhibition assays.
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| ln Vivo |
Quinelorane diHClide (LY163502; 0.003, 0.01 mg/kg; sc) can inhibit GABA efflux. 0.01 mg/kg has a substantial effect in male Wistar rats (300 g), whereas the effect at 0.003 mg/kg is not significant [1]. Qunelorane diHClide (0.032, 0.32, 3.2, 5.6 mg/kg; IP) substantially and dose-dependently enhances locomotor activity in Sprague Dawley rats. There was no main influence of sex and sex interaction [1]. Qunelorane diHClide significantly lowers activity in male and female inbred strains FVB/NJ, BALB/cJ, BALB/cByJ, C57BL/6J, Swiss Webster, A/J, DBA/2J, 129S1/SvImJ and 129S6/SvEvTac mice [ 1] .
Quinelorane hydrochloride reduces ventral pallidal GABA efflux at a dose of 0.01 mg/kg. It is used in behavioral pharmacology and neurochemistry studies to investigate the role of dopamine D2 and D3 receptors in various physiological and pathological processes. However, specific in vivo efficacy data beyond these observations are not extensively detailed in the available literature. |
| Enzyme Assay |
In vitro receptor binding assays for Quinelorane hydrochloride typically involve measuring its displacement of a radiolabeled dopamine receptor ligand from membrane preparations expressing D2 or D3 receptors. The receptor is incubated with a radiolabeled ligand (e.g., [³H]-spiperone or [³H]-7-OH-DPAT) in the presence of varying concentrations of the compound. The Ki values are calculated from competition binding curves, with Quinelorane hydrochloride showing Ki values of 5.7 nM for D2 and 3.4 nM for D3.
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| Cell Assay |
Cellular assays for Quinelorane hydrochloride are performed in cells expressing dopamine D2 or D3 receptors. The compound's agonist activity is assessed by measuring its ability to activate receptor-mediated signaling pathways, such as inhibition of cAMP production. Cells are treated with Quinelorane hydrochloride, and cAMP levels are measured. The compound's potency and efficacy as a D2/D3 agonist are determined from concentration-response curves.
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| Animal Protocol |
In vivo animal studies with Quinelorane hydrochloride have been performed to evaluate its effects on dopaminergic signaling and behavior. The compound reduces ventral pallidal GABA efflux at a dose of 0.01 mg/kg. It is also used in behavioral assays such as hypothermia and prepulse inhibition to study the role of D2/D3 receptors. However, specific protocols are not extensively detailed in the available literature.
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| ADME/Pharmacokinetics |
Quinelorane hydrochloride has a molecular weight of 319.27 and a molecular formula of C14H22N4·2HCl. It is soluble in DMSO and has high water solubility (up to 25 mM). The compound is stable when stored at room temperature in a desiccated environment. However, detailed pharmacokinetic parameters such as absorption, distribution, metabolism, excretion, half-life, and bioavailability are not extensively reported.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for Quinelorane hydrochloride are not extensively reported. The compound is classified as a research-use-only chemical and is not intended for human consumption. As a dopamine receptor agonist, it may have effects on various physiological processes that could contribute to toxicity at high concentrations. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
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| References |
[1]. Ying Qu, et al. Quinelorane, a dopamine D3/D2 receptor agonist, reduces prepulse inhibition of startle and ventral pallidal GABA efflux: time course studies. Pharmacol Biochem Behav. 2008 Oct;90(4):686-90.
[2]. Morgane Thomsen, et al. Psychomotor stimulation by dopamine D₁-like but not D₂-like agonists in most mouse strains. Exp Clin Psychopharmacol. 2011 Oct;19(5):342-60. |
| Additional Infomation |
Quinelorane hydrochloride is a research-grade compound not approved for clinical use. Its primary application is as a pharmacological tool for studying dopamine D2 and D3 receptors. The compound is widely used in neuropharmacological research to study dopaminergic signaling, receptor dynamics, and their implications in neurological and psychiatric disorders such as Parkinson's disease, schizophrenia, and drug addiction. Its balanced D2/D3 profile makes it a valuable tool for teasing apart the contributions of these receptors.
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| Molecular Formula |
C14H24CL2N4
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| Molecular Weight |
319.273160934448
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| Exact Mass |
318.138
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| CAS # |
97548-97-5
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| PubChem CID |
68728
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
438.5ºC at 760 mmHg
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| Flash Point |
219ºC
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| LogP |
3.771
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
283
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C(N1CCC[C@@H]2CC3N=C(N)N=CC=3C[C@@H]12)CC.Cl
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| InChi Key |
WDEMLQIGYYLRRX-OWVUFADGSA-N
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| InChi Code |
InChI=1S/C14H22N4.2ClH/c1-2-5-18-6-3-4-10-7-12-11(8-13(10)18)9-16-14(15)17-12;;/h9-10,13H,2-8H2,1H3,(H2,15,16,17);2*1H/t10-,13-;;/m1../s1
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| Chemical Name |
(5aR,9aR)-6-propyl-5a,7,8,9,9a,10-hexahydro-5H-pyrido[2,3-g]quinazolin-2-amine;dihydrochloride
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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) |
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 | 3.1321 mL | 15.6607 mL | 31.3215 mL | |
| 5 mM | 0.6264 mL | 3.1321 mL | 6.2643 mL | |
| 10 mM | 0.3132 mL | 1.5661 mL | 3.1321 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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