Release date: 2014-07-23
Paracetamol is one of the most common drugs, with only 27 billion tablets sold in 2009 (average 4 per person on Earth). Although paracetamol has a long history, its mechanism of action has not been conclusive. An early statement was that paracetamol inhibited COX like aspirin, so inhibition of prostaglandin biosynthesis led to anti-inflammatory and fever-reducing. Later, the pioneer of COX research, Nobel laureate JohnVane believed that paracetamol worked by inhibiting central COX. But later found that the dog may be the case, but it does not apply to people. Now the COX school believes that paracetamol can effectively inhibit COX only under certain physiological conditions.
Recent studies have shown that paracetamol or its metabolites can act as an analgesic effect with other pain-related receptors and ion channels in the central nervous system. For example, the hot targets of the pharmaceutical industry, such as cannabinoid receptor, 5HT3 receptor, and TRPV/TRPA channel, can be regulated by paracetamol. It has also been suggested that paracetamol is associated with opioid receptors. C&EN consulted five experts in this field. Some people think that this question is basically clear. Some people think that we still understand it very comprehensively.
The target proteins mentioned above have all been cloned and can be expressed in vitro. The pharmaceutical industry has also screened and optimized a myriad of compounds that are much more complex than paracetamol. These compounds are much better for the activity of these targets, the selectivity for other proteins, or the pharmacological and toxicological properties than paracetamol, but No one can be listed as a drug. Does this mean that the current drug discovery system is wrong (of course, these targets may also have nothing to do with pain relief)?
There is no doubt that it is difficult to find drugs such as aspirin and paracetamol in the current R&D system, but this does not mean that the paracetamol method is a better development system. Last Friday's article talked about the importance of lead quality. Aspirin and paracetamol are basically not optimized, that is, the quality of the lead is very high, almost a drug. This can be said to be a gift from God. This kind of example is actually in many other fields. For example, if it is necessary to design a substance with a solid density lower than the liquid density according to the principle of molecular mechanics, if we do not know the existence of water, it may take a lot of manpower and material resources to invent this peculiar substance. Perhaps because of our lack of knowledge and ability, God put the most important things in the most conspicuous place.
But gifts are not received every day, and more often we have to work hard to find useful things. The paracetamol story only shows that the current optimization system still relies on the quality of the lead, but maintaining a large pharmaceutical industry still requires a complex and complete research and development system, because in most cases high-quality lead must be obtained through a large number of scientists.
Source: US and Chinese medicine source
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