An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. ##-Carbolines are a novel class of potent mixed CB1/CB2 agonists characterized by attractive physicochemical properties including high aqueous solubility. Optimization of the series has led to the discovery of 29, which has oral activity in a rat inflammatory pain model and limited brain exposure at analgesic doses, consistent with a lower risk of CNS-mediated tolerability issues. ..more
Tested Compound:
Description:
Title: ##-Carbolines: a novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration.
Abstract: An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. ##-Carbolines are a novel class of potent mixed CB1/CB2 agonists characterized by attractive physicochemical properties including high aqueous solubility. Optimization of the series has led to the discovery of 29, which has oral activity in a rat inflammatory pain model and limited brain exposure at analgesic doses, consistent with a lower risk of CNS-mediated tolerability issues.
(PMID: 22284817)
Abstract: An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. ##-Carbolines are a novel class of potent mixed CB1/CB2 agonists characterized by attractive physicochemical properties including high aqueous solubility. Optimization of the series has led to the discovery of 29, which has oral activity in a rat inflammatory pain model and limited brain exposure at analgesic doses, consistent with a lower risk of CNS-mediated tolerability issues.
(PMID: 22284817)
Comment
Putative Target:
ChEMBL Target ID: 80249
Target Type: CELL-LINE
Cell Line: MDCK
Tissue: Kidney cells
Pref Name: MDCK
Organism: Canis lupus familiaris
Tax ID: 9615
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
ChEMBL Target ID: 80249
Target Type: CELL-LINE
Cell Line: MDCK
Tissue: Kidney cells
Pref Name: MDCK
Organism: Canis lupus familiaris
Tax ID: 9615
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment
ChEMBL Assay Type: ADMET
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Assay Data Source: Scientific Literature
Result Definitions
| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | Ratio activity comment | Ratio activity comment | String | |||
| 2 | Ratio standard flag | Ratio standard flag |  | Integer | ||
| 3 | Ratio qualifier | Ratio qualifier | String | |||
| 4 | Ratio published value | Ratio published value | | Float | ||
| 5 | Ratio standard value | Ratio standard value | | Float |
Data Table (Concise)
PageFrom: