Page last updated: 2024-12-06

picenadol

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

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]

Cross-References

ID Source	ID
PubMed CID	53077
CHEMBL ID	2110973
SCHEMBL ID	488873
MeSH ID	M0107800

Synonyms (5)

Synonym
picenadol
3-[(3r,4s)-1,3-dimethyl-4-propylpiperidin-4-yl]phenol
SCHEMBL488873
Q7190610
CHEMBL2110973

Research Excerpts

Overview

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
"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

Effects

Excerpt	Reference	Relevance
"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

Dosage Studied

Excerpt	Relevance	Reference
"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

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

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]

Market Indicators

Research Demand Index: 18.98

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.

Metric	This Compound (vs All)
Research Demand Index	18.98 (24.57)
Research Supply Index	2.94 (2.92)
Research Growth Index	4.29 (4.65)
Search Engine Demand Index	15.26 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (18.98)

All Compounds (24.57)

Study Types

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]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
meperidine Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.. pethidine : A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain.	8.35	1	1	ethyl ester; piperidinecarboxylate ester; tertiary amino compound	antispasmodic drug; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic
methadone Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3). methadone : A racemate comprising equimolar amounts of dextromethadone and levomethadone. It is a opioid analgesic which is used as a painkiller and as a substitute for heroin in the treatment of heroin addiction.. 6-(dimethylamino)-4,4-diphenylheptan-3-one : A ketone that is heptan-3-one substituted by a dimethylamino group at position 6 and two phenyl groups at position 4.	1.96	1	0	benzenes; diarylmethane; ketone; tertiary amino compound
physostigmine Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.	1.96	1	0	carbamate ester; indole alkaloid	antidote to curare poisoning; EC 3.1.1.8 (cholinesterase) inhibitor; miotic
mr 2034 MR 2034: UM 1071 is active stereoisomer; 28 salts & isomers in Chemline; MR 2034 active isomer; MR 2035 less active isomer	1.96	1	0
pentazocine Pentazocine: The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)	1.96	1	0	benzazocine
buprenorphine Buprenorphine: A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.. buprenorphine : A morphinane alkaloid that is 7,8-dihydromorphine 6-O-methyl ether in which positions 6 and 14 are joined by a -CH2CH2- bridge, one of the hydrogens of the N-methyl group is substituted by cyclopropyl, and a hydrogen at position 7 is substituted by a 2-hydroxy-3,3-dimethylbutan-2-yl group. It is highly effective for the treatment of opioid use disorder and is also increasingly being used in the treatment of chronic pain.	1.96	1	0	morphinane alkaloid	delta-opioid receptor antagonist; kappa-opioid receptor antagonist; mu-opioid receptor agonist; opioid analgesic
codeine [no description available]	8.76	2	1	morphinane alkaloid; organic heteropentacyclic compound	antitussive; drug allergen; environmental contaminant; opioid analgesic; opioid receptor agonist; prodrug; xenobiotic
naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.	2.88	4	0	morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol	antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist
morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.	2.66	3	0	morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound	anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic
nalbuphine Nalbuphine: A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS.	1.96	1	0	organic heteropentacyclic compound	mu-opioid receptor antagonist; opioid analgesic
butorphanol Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.. butorphanol : Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is used as its (S,S)-tartaric acid salt for relief or moderate to severe pain.	1.96	1	0	morphinane alkaloid	antitussive; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic
morphinans Morphinans: Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.	1.96	1	0	isoquinoline alkaloid fundamental parent; morphinane alkaloid
scopolamine hydrobromide [no description available]	1.96	1	0
piperidines Piperidines: A family of hexahydropyridines.	6.14	12	3

Condition	Relationship Strength	Studies	Trials
Acute Post-operative Pain [description not available]	4.96	3	3
Pain, Postoperative Pain during the period after surgery.	4.96	3	3
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	3.35	1	1
Chemical Dependence [description not available]	1.97	1	0
Morphine Abuse [description not available]	2.37	2	0
Morphine Dependence Strong dependence, both physiological and emotional, upon morphine.	2.37	2	0
Substance-Related Disorders Disorders related to substance use or abuse.	1.97	1	0
Ache [description not available]	1.96	1	0
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	1.96	1	0
Drug Withdrawal Symptoms [description not available]	1.96	1	0
Substance Withdrawal Syndrome Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.	1.96	1	0

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