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 Compounds:
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: 102178
Target Type: SUBCELLULAR
Pref Name: Liver microsomes
Organism: Rattus norvegicus
Tax ID: 10116
Confidence: Target assigned is subcellular fraction
Relationship Type: Subcellular target assigned
ChEMBL Target ID: 102178
Target Type: SUBCELLULAR
Pref Name: Liver microsomes
Organism: Rattus norvegicus
Tax ID: 10116
Confidence: Target assigned is subcellular fraction
Relationship Type: Subcellular 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 | Stabilty activity comment | Stabilty activity comment | String | |||
| 2 | Stabilty standard flag | Stabilty standard flag |  | Integer | ||
| 3 | Stabilty qualifier | Stabilty qualifier | String | |||
| 4 | Stabilty published value | Stabilty published value | | Float | microL/min/mg | |
| 5 | Stabilty standard value | Stabilty standard value | | Float | microL/min/mg |
Data Table (Concise)
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