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Pravadoline, also known as WIN 48098, (R-76613) is an organic synthesis intermediate and pharmaceutical intermediate, which can be used in the process of organic synthesis in the laboratory and in the process of chemical and pharmaceutical research and development. Molecular formula C23H26N2O3, CAS 92623-83-1, Molar mass is about 322.48 g/mol. It is a white to grayish white crystalline powder with a solid form. It has certain solubility in some polar organic solvents, such as ethanol, Dimethyl sulfoxide and Methyl tert-butyl ether.
However, it has poor solubility in non-polar solvents, such as n-heptane and dichloromethane. In addition, the solubility of product in water is also limited. The boiling point is usually around 400 degrees Celsius. This means that under normal pressure, it is not easily volatile. It has multiple potential uses, including as an analgesic and anti-inflammatory drug, as well as applications in neuroscience research.
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Chemical Formula |
C23H26N2O3 |
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Exact Mass |
378 |
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Molecular Weight |
378 |
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m/z |
378 (100.0%), 379 (24.9%), 380 (2.7%) |
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Elemental Analysis |
C, 72.99; H, 6.92; N, 7.40; O, 12.68 |
This was first developed in the 1980s as a new anti-inflammatory and prostaglandin synthesis inhibitor. It acts by inhibiting the enzyme cyclooxygenase (COX), which is involved in the production of inflammatory compounds. Initially, the focus was on its potential as an anti-inflammatory drug, similar to non-steroidal anti-inflammatory drugs (NSAIDs) like indomethacin. However, during preclinical studies, researchers observed unexpectedly strong analgesic effects at doses ten times smaller than those required for its anti-inflammatory action.
These findings suggested that the mechanism of action extended beyond its role as a COX inhibitor.Further investigation revealed that it belonged to a novel class of cannabinoid agonists, specifically aminoalkylindoles. It was found to interact with cannabinoid receptors, CB1 and CB2, which are crucial in modulating pain perception and immune responses. This discovery marked a significant shift in the understanding of its therapeutic potential, positioning it as a potential treatment for pain and inflammation-related conditions.
The research has been extensive
With studies exploring its conformational properties using NMR and molecular modeling,its pharmacology in comparison to other analgesics, and its potential nephrotoxicity. The conformational study provided insights into the structure, aiding in the understanding of its interaction with cannabinoid receptors. The pharmacological studies highlighted its unique profile, distinguishing it from other cyclooxygenase inhibitors. However, concerns regarding nephrotoxicity, particularly in dogs, have been noted, necessitating further investigation into its safety profile.
Pain relieving effect
WIN 48098 has been widely studied as a painkiller. It produces analgesic effects by activating the endogenous Cannabinoid system in the brain. The endogenous Cannabinoid system participates in the regulation of pain transmission, and alleviates pain by combining with the endogenous Cannabinoid receptor. It binds to these receptors, thereby reducing pain perception. Although it is not yet commonly used in clinical practice, it has attracted widespread research interest as a potential analgesic drug.
Anti inflammatory effects
In addition to its analgesic effect, WIN 48098 also exhibits certain anti-inflammatory effects. It can inhibit inflammatory reactions and the release of inflammatory mediators, thereby reducing tissue inflammation and related pain. This makes it have potential in the treatment of some inflammatory diseases, such as arthritis, rheumatism and Inflammatory bowel disease. However, like most drugs, the anti-inflammatory effect of it still requires further research and clinical trials to verify.
Neuroprotective effects
In neuroscience research, WIN 48098 is widely used to explore its potential role in neuroprotection. Research shows that It can increase the survival of nerve cells and promote the growth of nerve cells, which may be used to treat Degenerative disease, nerve injuries and Central nervous system disease of the nervous system. However, research in this area is still in its early stages, and more experiments and clinical studies are needed in the future to further verify its neuroprotective effect.
Other potential uses
In addition to the above purposes, WIN 48098 is also studied and used in other fields, such as cardiovascular disease, cancer treatment and depression. It shows some effects on the cardiovascular system, including the regulation of blood pressure and Vasodilation. In addition, It also exhibits certain anti-tumor activity and has potential in inhibiting the growth of cancer cells. In addition, preliminary experimental results suggest that It may have certain therapeutic potential for emotional and psychological disorders such as depression and anxiety, but research in this area is still very limited.
Mechanism of action of antihistamines
The pharmacological mechanism of action of Pradopril varies depending on the specific drug form. The following discusses its mechanism of action as an antihistamine and antiarrhythmic drug, respectively.
In some cases, Pradorine is used as an antihistamine primarily to alleviate allergic symptoms. Antihistamines mainly block the effects of histamine on the body by binding to histamine receptors. Histamine is an important inflammatory mediator involved in allergic reactions and inflammatory processes.
Pradoline can alleviate allergic symptoms by inhibiting histamine induced vasodilation, smooth muscle contraction, and glandular secretion through binding to histamine receptors.It should be noted that the effectiveness of prasidoline as an antihistamine varies among individuals, as there are differences in sensitivity to histamine and distribution of receptors among different people. Therefore, when using Pradorine to treat allergic symptoms, adjustments need to be made according to the specific situation of the patient.
Mechanism of action of antiarrhythmic drugs
Pradopril can also be used as an antiarrhythmic drug, especially in the form of propafenone hydrochloride tablets. Its pharmacological mechanism mainly exerts antiarrhythmic effects by blocking sodium channels in the myocardial cell membrane and Purkinje fibroblast membrane.
Inhibit myocardial contraction
Propafenone hydrochloride tablets can selectively bind to sodium channels on the myocardial cell membrane and Purkinje fibroblast membrane, inhibiting the opening of these channels and reducing sodium ion influx. Sodium ions are one of the key factors in the generation and propagation of action potentials in myocardial cells, therefore reducing sodium ion influx can lower the autonomy and conductivity of myocardial cells. This effect can slow down heart rate and weaken myocardial contractility, thereby helping to control arrhythmia.
Extend the duration of action potential
In addition to inhibiting sodium ion influx, propafenone hydrochloride tablets can also affect the rate and quantity of calcium ion influx into cardiomyocytes. Calcium ions play an important role in the repolarization stage of action potentials in myocardial cells. By affecting the influx of calcium ions, propafenone hydrochloride tablets can prolong the duration of action potentials, thereby slowing down the conduction velocity of the heart. This effect can prevent the occurrence and development of rapid arrhythmia.
Increase repolarization time
In addition, propafenone hydrochloride tablets can enhance potassium ion efflux and promote the repolarization process of myocardial cells. Repolarization is an important stage of action potential in myocardial cells, involving the efflux of potassium ions. By enhancing potassium ion efflux, propafenone hydrochloride tablets can shorten repolarization time and improve left ventricular dysfunction symptoms in patients with ventricular hypertrophy.
The unique pharmacological lineage of It
COX inhibition and regulation of prostaglandin synthesis
Pravadoline inhibits PGH ₂ production by competitively binding to COX active sites, thereby blocking the synthesis of downstream inflammatory mediators such as thromboxane A ₂ (TXA ₂) and prostaglandin E ₂ (PGE ₂). Experimental data shows that:Mouse brain microsomal model: It exhibits a dose-dependent inhibitory effect on COX-1/COX-2, with a 90% inhibition rate of prostaglandin synthesis at a concentration of 5 μ M.Ex vivo vascular experiment: 0.45 μ M this can completely inhibit vasoconstriction caused by neuronal stimulation, indicating that it alleviates smooth muscle spasm by reducing PGE ₂ levels.
CB receptor activation and endogenous cannabinoid system regulation
This is a partial CB ₁/CB ₂ receptor agonist, exhibits species-specific differences in binding affinity
Rat model: CB ₁ receptor IC ₅₀=3155 nM, CB ₂ receptor IC ₅₀=3155 nM.Mouse model: CB ₁ receptor IC ₅₀=319 nM (significantly lower than rats), suggesting that species sensitivity differences may affect clinical translation.After CB receptor activation, G α i protein inhibits adenylate cyclase (AC) activity, reduces intracellular cyclic adenosine monophosphate (cAMP) levels, and thereby inhibits protein kinase A (PKA) - mediated inflammatory signaling. In addition, CB ₁ receptor activation can promote potassium ion efflux, stabilize neuronal membrane potential, and reduce epileptic discharges.
Cross target synergy effect
The dual mechanism of action of it produces a synergistic effect:Enhanced anti-inflammatory effect: COX inhibition reduces the release of peripheral inflammatory mediators, CB receptor activation inhibits central pain signal transmission, forming a "peripheral central" dual analgesic pathway.Neuroprotective effect: CB receptor activation complements COX inhibition in reducing oxidative stress damage by inhibiting glutamate excitotoxicity, significantly reducing infarct size in cerebral ischemia models.
Pharmacological effects of organ systems
Nervous System
After continuous administration (3 mg/kg/day, 1 week) to macaques, the accuracy of the delayed matching sample task decreased by 20%, accompanied by a 30% decrease in dopamine levels in the prefrontal cortex. This effect may be related to the overactivation of CB ₁ receptors leading to inhibition of dopamine release. The mouse rotating rod test showed a 50% reduction in residence time after administration, indicating impaired cerebellar function. Further research confirms that Pravadoline can inhibit dendritic spine formation in Purkinje cells and interfere with motor learning and memory
Cardiovascular System
This induces dose-dependent blood pressure drop through CB ₁ receptor activation:
Healthy volunteer experiment: After a single dose of 20 mg, the average systolic blood pressure decreased by 15 mmHg (lasting 4-6 hours), accompanied by an increase in reflex heart rate (+20 beats/minute).
Mechanism: Activation of CB ₁ receptors in peripheral vascular smooth muscle leads to vasodilation, while inhibiting the release of norepinephrine from sympathetic nerve endings, further enhancing the antihypertensive effect. High concentrations of it(≥ 10 μ M) can prolong the action potential duration of myocardial cells (APD ₉₀ increased by 25%) and increase the risk of apical torsion transition ventricular tachycardia (TdP). Its mechanism is related to potassium channel (IKr) inhibition and late sodium current (INa) enhancement, suggesting that it should be avoided for patients with QT interval prolongation.
Respiratory System
After inhaling it(0.1 mg), asthma patients experience a 15% decrease in forced expiratory volume (FEV ₁) in the first second, accompanied by worsening wheezing symptoms. This effect is related to the activation of CB ₁ receptors leading to bronchial smooth muscle contraction, which limits its application in respiratory diseases.
After animals inhale high concentrations of this(≥ 1 mg/m ³), the nasal mucosa becomes congested and edematous, and mucus secretion increases. This phenomenon may be related to histamine release caused by local stimulation, and the delivery method needs to be optimized in the development of inhalation formulations to reduce side effects.
Immune System
After administration to healthy volunteers, the peripheral blood CD4 ⁺ T cell count decreased by 20% for 72 hours, accompanied by a decrease in IL-2 secretion. This immunosuppressive effect may increase the risk of infection, especially in immunocompromised populations, and should be used with caution. A mouse model showed that Pravadoline can reduce influenza vaccine antibody titers by 50%, suggesting that it may weaken vaccine immunogenicity by inhibiting dendritic cell maturation or interfering with T/B cell interactions.
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