| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Dopamine D2 autoreceptors and postsynaptic D2 receptors. Preclamol is a centrally acting dopamine receptor agonist with selectivity for autoreceptors. It acts as a full agonist at presynaptic dopamine autoreceptors (inhibiting dopamine synthesis and release) while exhibiting weak partial agonism or antagonism at postsynaptic D2 receptors.
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| ln Vitro |
In vitro, Preclamol acts as a dopamine receptor agonist with selectivity for autoreceptors. Its activity profile involves inhibiting DOPA accumulation in striatal and accumbens tissue slices, a functional measure of autoreceptor activation. This effect confirms its ability to inhibit dopamine synthesis in a relevant brain tissue model.
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| ln Vivo |
In vivo, Preclamol has been shown to inhibit DOPA accumulation in the striatum, nucleus accumbens, and medial prefrontal cortex of rodents. This demonstrates its ability to activate dopamine autoreceptors in a living brain, leading to a rapid reduction in dopamine synthesis. It has also been used to stimulate growth hormone (GH) release in humans.
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| Enzyme Assay |
The non-cellular protocol for determining binding affinity uses radioligand competition assays. Membrane preparations from cells expressing human D2 or D3 receptors are incubated with [3H]spiperone or [3H]raclopride with increasing concentrations of Preclamol. After filtration, radioactivity is counted, and Ki values are calculated.
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| Cell Assay |
To assess functional autoreceptor activity, a synaptosomal preparation from rat striatum is used. Synaptosomes are pre-incubated with Preclamol, then stimulated with potassium to depolarize the membrane. The amount of [3H]dopamine released is measured. A decrease in stimulated dopamine release indicates successful autoreceptor activation and inhibition of exocytosis.
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| Animal Protocol |
In a classic in vivo protocol, male rats are administered Preclamol via subcutaneous injection. After 30-60 min, the animals are euthanized, and brain regions (striatum, nucleus accumbens) are dissected. The accumulation of L-DOPA is measured by HPLC-ECD following inhibition of aromatic amino acid decarboxylase (AADC) to quantify the rate of dopamine synthesis.
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| ADME/Pharmacokinetics |
In humans, pharmacokinetic analysis after intramuscular injection of 30-40 mg showed blood levels between 200-500 pmoles/ml. The drug's half-life is 2-2.5 hours. Growth hormone (GH) levels were elevated in a linear fashion up to the 30 mg dose, providing a pharmacodynamic readout of its central activity.
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| Toxicity/Toxicokinetics |
In Phase I clinical trials in male schizophrenic volunteers, Preclamol was administered intramuscularly in a single rising dose design and was found to be safe. No severe adverse effects were reported, suggesting it is a safe drug for studying dopamine autoreceptor function in humans.
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| References | |
| Additional Infomation |
Preclamol hydrochloride ((-)-3-PPP) is the enantiomer of (R)-Preclamol ((+)-3-PPP). These two enantiomers have distinct pharmacological profiles; while both activate autoreceptors, (+)-3-PPP is a weak partial agonist/antagonist at postsynaptic sites, whereas (-)-3-PPP is a more potent full agonist at autoreceptors. This pair is invaluable for dissecting the functional roles of pre- vs. postsynaptic dopamine receptors.
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| Molecular Formula |
C14H22CLNO
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|---|---|
| Molecular Weight |
255.78
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| Exact Mass |
255.139
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| CAS # |
88768-67-6
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| Related CAS # |
(R)-Preclamol hydrochloride;89874-80-6;(R)-Preclamol;85976-54-1
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| PubChem CID |
11957669
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| Appearance |
White to light yellow solid powder
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| Boiling Point |
342.2ºC at 760 mmHg
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| Flash Point |
158ºC
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| LogP |
3.721
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
17
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| Complexity |
207
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCCN1CCC[C@H](C1)C2=CC(=CC=C2)O.Cl
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| InChi Key |
NRHUDETYKUBQJT-BTQNPOSSSA-N
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| InChi Code |
InChI=1S/C14H21NO.ClH/c1-2-8-15-9-4-6-13(11-15)12-5-3-7-14(16)10-12;/h3,5,7,10,13,16H,2,4,6,8-9,11H2,1H3;1H/t13-;/m1./s1
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| Chemical Name |
3-[(3S)-1-propylpiperidin-3-yl]phenol;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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: 50 mg/mL (195.48 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 | 3.9096 mL | 19.5480 mL | 39.0961 mL | |
| 5 mM | 0.7819 mL | 3.9096 mL | 7.8192 mL | |
| 10 mM | 0.3910 mL | 1.9548 mL | 3.9096 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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