Page last updated: 2024-12-08
cns 5161
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
CNS 5161: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 192711 |
| CHEMBL ID | 41306 |
| SCHEMBL ID | 499356 |
| MeSH ID | M0442548 |
Synonyms (19)
| Synonym |
|---|
| 160754-76-7 |
| cns5161 |
| cns-5161 |
| CHEMBL41306 , |
| cns 5161 |
| n''-(2-chloro-5-methylsulfanyl-phenyl)-n-methyl-n-(3-methylsulfanyl-phenyl)-guanidine |
| bdbm50096974 |
| 2-(2-chloro-5-methylsulfanylphenyl)-1-methyl-1-(3-methylsulfanylphenyl)guanidine |
| guanidine, n'-(2-chloro-5-(methylthio)phenyl)-n-methyl-n-(3-(methylthio)phenyl)- |
| unii-58s83m36v6 |
| 58s83m36v6 , |
| DB05824 |
| SCHEMBL499356 |
| DTXSID20166975 |
| AKOS027382365 |
| Q27095700 |
| cns5161;cns 5161 |
| 3-(2-chloro-5-(methylthio)phenyl)-1-methyl-1-(3-(methylthio)phenyl)guanidine |
| cns-5161,n-(2-chloro-5-methylsulfanyl-phenyl)-n-methyl-n-(3-methylsulfanyl-phenyl)-guanidine |
Research Excerpts
Overview
CNS 5161 is a novel NMDA ion-channel antagonist. It interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
| Excerpt | Reference | Relevance |
|---|---|---|
| "CNS 5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate." | ( Early clinical experience with the novel NMDA receptor antagonist CNS 5161. Bradford, AP; Fischer, J; Lees, KR; Walters, MR, 2002) | 1.27 |
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " All adverse events to study drug, blood pressure, heart rate, ECG, drug level and clinical laboratory values were monitored." | ( Dose escalating safety study of CNS 5161 HCl, a new neuronal glutamate receptor antagonist (NMDA) for the treatment of neuropathic pain. Forst, T; Marcus, P; Pfützner, A; Schütte, K; Smith, T, 2007) | 0.62 |
| " The most common adverse events were hypertension, headache and mild visual disorders." | ( Dose escalating safety study of CNS 5161 HCl, a new neuronal glutamate receptor antagonist (NMDA) for the treatment of neuropathic pain. Forst, T; Marcus, P; Pfützner, A; Schütte, K; Smith, T, 2007) | 0.62 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " A dose escalation design was adopted and the volunteers were stratified into eight dosage groups, ranging from 30 microg to 2000 microg." | ( Early clinical experience with the novel NMDA receptor antagonist CNS 5161. Bradford, AP; Fischer, J; Lees, KR; Walters, MR, 2002) | 0.55 |
| " A dose dependent rise in systolic, mean arterial and diastolic blood pressure was seen in subsequent dosage groups, reaching 23/19 mmHg." | ( Early clinical experience with the novel NMDA receptor antagonist CNS 5161. Bradford, AP; Fischer, J; Lees, KR; Walters, MR, 2002) | 0.55 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (10)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Glutamate receptor ionotropic, NMDA 2D | Homo sapiens (human) | Ki | 0.0019 | 0.0012 | 0.7025 | 6.0000 | AID143453 |
| Glutamate receptor ionotropic, NMDA 3B | Homo sapiens (human) | Ki | 0.0019 | 0.0012 | 0.7025 | 6.0000 | AID143453 |
| Sodium channel protein type 1 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 1.7500 | 0.0023 | 2.8296 | 9.0000 | AID146732 |
| Glutamate receptor ionotropic, NMDA 1 | Homo sapiens (human) | Ki | 0.0019 | 0.0012 | 0.4824 | 6.0000 | AID143453 |
| Glutamate receptor ionotropic, NMDA 2A | Homo sapiens (human) | Ki | 0.0019 | 0.0012 | 0.6205 | 6.0000 | AID143453 |
| Glutamate receptor ionotropic, NMDA 2B | Homo sapiens (human) | Ki | 0.0019 | 0.0012 | 0.3268 | 6.0000 | AID143453 |
| Glutamate receptor ionotropic, NMDA 2C | Homo sapiens (human) | Ki | 0.0019 | 0.0012 | 0.7025 | 6.0000 | AID143453 |
| Glutamate receptor ionotropic, NMDA 3A | Homo sapiens (human) | Ki | 0.0019 | 0.0012 | 0.7025 | 6.0000 | AID143453 |
| Sodium channel protein type 2 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 1.7500 | 0.0000 | 3.7401 | 10.0000 | AID146732 |
| Sodium channel protein type 3 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 1.7500 | 0.0053 | 2.8085 | 9.0000 | AID146732 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (82)
Molecular Functions (24)
Ceullar Components (39)
Bioassays (11)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID188219 | Compound was tested in hypoxia -ischemia reduction model for percent reduction in lesion volume at the dose 4 mg/kg (iv) | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788. |
| AID178880 | Compound was tested in rotarod motor assay and the effective intravenous dose required to fall from the rod was reported. | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788. |
| AID233151 | Lowest effective intravenous dose required to observe the behavioral effects (excitation) | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788. |
| AID146731 | Cardiac sodium channel blocking activity by [14C]guanidinium flux assay | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788. |
| AID189394 | Tested in rat middle cerebral artery occlusion model (MACO model) and percent reduction in total lesion volume at the dose of 1.5 mg/kg (combination ip and iv) | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788. |
| AID132239 | Effective dose required to block the audiogenic seizures. | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788. |
| AID26784 | Partition coefficient (logP) | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Synthesis and in vitro evaluation of N,N'-diphenyl and N-naphthyl-N'-phenylguanidines as N-methyl-D-aspartate receptor ion-channel ligands. |
| AID145330 | In vitro binding to N-methyl-D-aspartate glutamate receptor using [3H]MK-801 (1 nM) and rat brain membrane suspensions | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Synthesis and in vitro evaluation of N,N'-diphenyl and N-naphthyl-N'-phenylguanidines as N-methyl-D-aspartate receptor ion-channel ligands. |
| AID146732 | Neuronal sodium channel blocking activity by [14C]guanidinium flux assay | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788. |
| AID143453 | In vitro displacement of [3H]MK-801 from N-methyl-D-aspartate glutamate receptor | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788. |
| AID493017 | Wombat Data for BeliefDocking | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (9)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (55.56) | 29.6817 |
| 2010's | 4 (44.44) | 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: 11.97
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 (11.97) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (11.11%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 8 (88.89%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||