Page last updated: 2024-12-08
ly 106737
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
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Research Growth
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Description
LY 106737: RN given refers to (cis(+-)-isomer); structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 134131 |
| CHEMBL ID | 319536 |
| MeSH ID | M0176035 |
Synonyms (14)
| Synonym |
|---|
| 82970-72-7 |
| CHEMBL319536 , |
| (+)-n-phenethyl trans-3(r),4(r)-dimethyl-4-(3-hydroxyphenyl)piperidine |
| n-phenethyltrans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine |
| 3-((3r,4r)-3,4-dimethyl-1-phenethyl-piperidin-4-yl)-phenol |
| bdbm50045767 |
| 3-(3,4-dimethyl-1-phenethyl-piperidin-4-yl)-phenol |
| 3-(trans-3,4-dimethyl-1-phenethylpiperidin-4-yl)phenol |
| phenol, 3-(3,4-dimethyl-1-(2-phenylethyl)-4-piperidinyl)-, cis-(+-)- |
| ly-106737 |
| ly 106737 |
| 3-[(3r,4r)-3,4-dimethyl-1-(2-phenylethyl)piperidin-4-yl]phenol |
| 3-[3,4-dimethyl-1-(2-phenylethyl)piperidin-4-yl]phenol |
| DTXSID801003031 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (6)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0015 | 0.0000 | 0.3845 | 8.6000 | AID224574 |
| Mu-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 0.0016 | 0.0001 | 0.8133 | 10.0000 | AID150821; AID260389; AID274396; AID274417 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.0018 | 0.0000 | 0.4197 | 10.0000 | AID150990; AID152067; AID260386; AID274390; AID274411 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 0.0330 | 0.0000 | 0.5978 | 9.9300 | AID148251; AID260388; AID274392; AID274413 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0520 | 0.0000 | 0.2018 | 6.4240 | AID149274; AID223587 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 0.0255 | 0.0000 | 0.3624 | 10.0000 | AID148019; AID148251; AID148709; AID260387; AID274391; AID274412 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0015 | 0.0000 | 0.2786 | 9.0000 | AID224574 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (52)
Molecular Functions (12)
Ceullar Components (23)
Bioassays (25)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID274396 | Antagonist activity assessed as inhibition of loperamide-stimulated [35S]GTPgammaS binding to human mu opioid receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists. |
| AID274390 | Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists. |
| AID260388 | Displacement of [3H]diprenorphine from human cloned delta opioid receptor | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Synthesis and structure-activity relationships of a new series of 2alpha-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as mu-selective opioid antagonists. |
| AID274417 | Antagonist activity against human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of loperamide-stimulated [35S]GTP-gamma-S binding | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists. |
| AID223591 | Tested for the antagonism of kappa opioid receptor diuresis at a dose of 0.08 mg/kg subcutaneously | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors. |
| AID223587 | Binding affinity towards kappa-opioid receptor by displacement of [3H]-EKC at from guinea pig cortical tissue | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors. |
| AID224574 | Binding affinity was determined against Mu opioid receptor using [3H]-Naltrexone as radioligand | 1998 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22 | N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists. |
| AID260386 | Displacement of [3H]diprenorphine from human cloned mu opioid receptor | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Synthesis and structure-activity relationships of a new series of 2alpha-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as mu-selective opioid antagonists. |
| AID148019 | Binding affinity at cloned human kappa opioid receptor by [3H]diprenorphine displacement. | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists. |
| AID274391 | Displacement of [3H]diprenorphine from human cloned kappa opioid receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists. |
| AID149274 | Binding affinity was determined against Opioid receptor kappa 1 using [3H]ethylketocyclazocine as radioligand | 1998 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22 | N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists. |
| AID148251 | Concentration required to inhibit the binding of the non-selective opioid antagonist, [3H]diprenorphine, to cloned human delta opioid receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists. |
| AID260389 | Inhibition of loperamide-stimulated [35S]GTP-gamma-S binding to membranes containing mu opioid receptor | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Synthesis and structure-activity relationships of a new series of 2alpha-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as mu-selective opioid antagonists. |
| AID148709 | Binding affinity against Opioid receptor kappa 1 using [3H]ethylketocyclazocine as radioligand. | 1998 | Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21 | N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists. |
| AID224718 | Binding affinity towards mu opioid receptor by displacement of [3H]NAL from rat brain homogenates | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors. |
| AID223589 | Antagonism of opioid analgesia using a mouse writhing model to block U-50,488 (2.5 mg/kg) induced kappa-opioid receptor subcutaneously | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors. |
| AID274411 | Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists. |
| AID274412 | Displacement of [3H]diprenorphine from human cloned kappa opioid receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists. |
| AID152067 | Binding affinity against Opioid receptor mu 1 using [3H]naloxone as radioligand. | 1998 | Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21 | N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists. |
| AID274392 | Displacement of [3H]diprenorphine from human cloned delta opioid receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists. |
| AID260387 | Displacement of [3H]diprenorphine from human cloned kappa opioid receptor | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Synthesis and structure-activity relationships of a new series of 2alpha-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as mu-selective opioid antagonists. |
| AID274413 | Displacement of [3H]diprenorphine from human cloned delta opioid receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists. |
| AID150821 | Concentration required to inhibit agonist (loperamide) stimulated [35S]GTP-gamma-S, binding to membranes containing the cloned human mu opioid receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists. |
| AID150990 | Inhibition of binding of the non-selective opioid antagonist, [3H]diprenorphine, to cloned human mu opioid receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists. |
| AID224715 | Antagonism of opioid analgesia using a mouse writhing model to block morphine (2.5 mg/kg) induced mu-opioid receptor (subcutaneously dosed) | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (8)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (50.00) | 18.2507 |
| 2000's | 4 (50.00) | 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: 12.16
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 weak demand-to-supply ratio for research on this compound.
| This Compound (12.16) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 8 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||