PZM21

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Structural formula
Structural formula of PZM21
General
Non-proprietary name PZM21
other names

1 - [(2 S ) -2- (Dimethylamino) -3- (4-hydroxyphenyl) propyl] -3 - [(2 S ) -1- (thiophen-3-yl) propan-2-yl] urea ( IUPAC )

Molecular formula C 19 H 27 N 3 O 2 S
External identifiers / databases
CAS number 1997387-43-5
PubChem 121596705
ChemSpider 58145207
Wikidata Q26306642
properties
Molar mass 361.50 g mol −1
safety instructions
GHS hazard labeling
no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

PZM21 is an experimental analgesic drug from the group of opioids , the application for the treatment of pain is explored. The substance is a functional selective μ- opioid receptor - agonist and has a similar analgesic potency and effectiveness as morphine .

As an analgesic, PZM21 is somewhat less potent than morphine or oliceridine , but it also has significantly fewer side effects: Constipation occurs less and respiratory depression is very low, even in very high doses. Likewise, no addiction could be proven so far. The findings to date are mainly based on the results of animal experiments; human trials are still pending.

The announcement of the results in Nature about PZM21 triggered a lot of echo in the press, as many hopes were aroused for a better treatment of pain with fewer side effects. PZM21 is an example of the successful application of active ingredient design : The researchers screened potential active ingredients using the so-called docking process, whereby substances were linked to the virtual binding site of a receptor in a computer model. A lead substance was selected from the most suitable molecules and its molecular structure was specifically optimized in terms of effectiveness.

Individual evidence

  1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
  2. ↑ Aashish Manglik, Henry Lin, Dipendra K. Aryal, John D. McCorvy, Daniela Dengler, Gregory Corder, Anat Levit, Ralf C. Kling, Viachaslau Bernat, Harald Hübner, Xi-Ping Huang, Maria F. Sassano, Patrick M. Giguère, Stefan Löber, null Da Duan, Grégory Scherrer, Brian K. Kobilka, Peter Gmeiner, Bryan L. Roth, Brian K. Shoichet: Structure-based discovery of opioid analgesics with reduced side effects . In: Nature . August 2016, p. 1-6 , doi : 10.1038 / nature19112 , PMID 27533032 .
  3. ↑ Peter Gmeiner: Painkillers without side effects , August 17, 2016, Friedrich-Alexander-Universität Erlangen-Nürnberg, reviewed on August 29, 2016.
  4. ↑ n-tv.de: New molecule can replace morphine , checked on August 29, 2016.
  5. ↑ Focus-online: Researchers find "ideal opioid" , reviewed on August 29, 2016.

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