Picenadol is a synthetic opioid analgesic that is structurally related to pentazocine. It acts as an agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. Picenadol has been studied for its potential to provide analgesia with fewer side effects than other opioids. It has shown efficacy in treating moderate to severe pain, but its use has been limited by concerns about its potential for abuse. Research on picenadol has focused on understanding its pharmacokinetic and pharmacodynamic properties, as well as its clinical efficacy and safety. Further studies are needed to fully evaluate its potential as a safe and effective analgesic.'
picenadol: racemic mixture of D-optical isomer (LY 97435) exhibiting potent morphine-like agonist activity & L-optical isomer (LY 97436) exhibiting nalorphine-like activity; RN given refers to parent cpd(trans)-(+-)-isomer; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
ID Source | ID |
---|---|
PubMed CID | 53077 |
CHEMBL ID | 2110973 |
SCHEMBL ID | 488873 |
MeSH ID | M0107800 |
Synonym |
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picenadol |
3-[(3r,4s)-1,3-dimethyl-4-propylpiperidin-4-yl]phenol |
SCHEMBL488873 |
Q7190610 |
CHEMBL2110973 |
Picenadol (LY 150720) is a racemic mixture of an N-methyl-4-phenylpiperidine derivative, with agonist-antagonist opiate properties. It is currently under clinical evaluation.
Excerpt | Reference | Relevance |
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"Picenadol (LY 150720) is a racemic mixture of an N-methyl-4-phenylpiperidine derivative, with agonist-antagonist opiate properties. " | ( Picenadol (LY 150720) compared with meperidine and placebo for relief of post-cesarean section pain: a randomized double-blind study. Sherline, DM, 1983) | 3.15 |
"Picenadol is a unique opioid mixed agonist-antagonist analgesic currently under clinical evaluation. " | ( Picenadol. Cantrell, BE; Hynes, MD; Leander, JD; Mendelsohn, LG; Nickander, R; Smits, SE; Zimmerman, DM, 1985) | 3.15 |
Excerpt | Reference | Relevance |
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"Picenadol itself has weak antagonist activity, whereas the antagonist potency of the l-isomer is approx." | ( Picenadol. Cantrell, BE; Hynes, MD; Leander, JD; Mendelsohn, LG; Nickander, R; Smits, SE; Zimmerman, DM, 1985) | 2.43 |
Excerpt | Relevance | Reference |
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"0 mg/kg); dose-response curves for LY136596 were shifted to the right in a parallel manner by increasing doses of LY136595." | ( Quantitative analysis of the interaction between the agonist and antagonist isomers of picenadol (LY150720) on electric shock titration in the squirrel monkey. Carter, RB; Dykstra, LA, 1984) | 0.49 |
"Randomized, double-blind, parallel, dose-response study." | ( Picenadol in a large multicenter dental pain study. Brunelle, RL; Cooper, SA; Desjardins, PJ; Gallegos, LT; Gaston, GW; George, RE; Goldstein, DJ; Jeffers, GE; Reynolds, DC, ) | 1.57 |
" This comparison suggests that 25 mg of picenadol is a more acceptable dosage since both 25 and 50 mg were effective dosages." | ( Intramuscular picenadol in patients with postoperative pain. Brunelle, RL; George, RE; Goldstein, DJ; Zimmerman, DM, 1993) | 0.91 |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 10 (83.33) | 18.7374 |
1990's | 2 (16.67) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 0 (0.00) | 24.3611 |
2020's | 0 (0.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (18.98) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 4 (28.57%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 10 (71.43%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |