| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
dopamine[1]
(R)-Preclamol is an agonist at dopamine receptors (D2 family) but displays functional selectivity, acting as an agonist at presynaptic dopamine autoreceptors while exhibiting antagonist or partial agonist properties at postsynaptic receptors. It also acts as an agonist at sigma receptors. This profile defines its utility as a research tool. |
|---|---|
| ln Vitro |
In vitro, (R)-Preclamol (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.
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| ln Vivo |
In vivo, (R)-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 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 (R)-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 (R)-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 (R)-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, (R)-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 |
[1]. Hjorth S, et al. Central dopamine receptor agonist and antagonist actions of the enantiomers of 3-PPP.
[2]. Arnt J, et al. Dopamine receptor agonistic and antagonistic effects of 3-PPP enantiomers. Psychopharmacology (Berl). 1983;81(3):199-207. |
| Additional Infomation |
(R)-Preclamol is distinguished by its stereoselective pharmacology. Its enantiomer, (S)-Preclamol ((-)-3-PPP), has a completely different profile, acting as a full antagonist at postsynaptic receptors while also activating autoreceptors. This pair of enantiomers provides a powerful tool for dissecting the functional roles of pre- vs. postsynaptic dopamine receptors in animal models of schizophrenia and Parkinson‘s disease.
|
| Molecular Formula |
C14H21NO
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|---|---|
| Molecular Weight |
219.32
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| Exact Mass |
219.162
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| CAS # |
85976-54-1
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| Related CAS # |
Preclamol hydrochloride;88768-67-6;(R)-Preclamol hydrochloride;89874-80-6
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| PubChem CID |
202478
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.919
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
16
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| Complexity |
207
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(N1CCC[C@H](C2C=CC=C(O)C=2)C1)CC
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| InChi Key |
HTSNFXAICLXZMA-ZDUSSCGKSA-N
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| InChi Code |
InChI=1S/C14H21NO/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/t13-/m0/s1
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| Chemical Name |
3-[(3R)-1-propylpiperidin-3-yl]phenol
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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: 100 mg/mL (455.95 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.5595 mL | 22.7977 mL | 45.5955 mL | |
| 5 mM | 0.9119 mL | 4.5595 mL | 9.1191 mL | |
| 10 mM | 0.4560 mL | 2.2798 mL | 4.5595 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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