1,259
edits
Changes
Jump to navigation
Jump to search
Line 43:
Line 43: − + − *'''Do they cross the blood brain barrier?'''+ − **'''Search [https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL63354/ ChEMBL]+ + + + + + + + + + + + + + + + + +
→Mechanisms of Anesthesia
**Sevoflurane binds to '''K<sub>v</sub>1.2''' w/ EC<sub>50</sub> of 0.0097 mM.
**Sevoflurane binds to '''K<sub>v</sub>1.2''' w/ EC<sub>50</sub> of 0.0097 mM.
*'''Are there pharmacological agents with receptor specificity? When given together with "promiscuous" anesthetics, what happens? For instance, is propofol equally effective when given with a specific HCN1 receptor inhibitor? What about a GABA<sub>A</sub>R inhibitor?'''
*'''Are there pharmacological agents with effects opposite of anesthetics and with receptor specificity? Do they cross the blood brain barrier? Search [https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL63354/ ChEMBL]. When given together with "promiscuous" anesthetics, what happens? For instance, is propofol equally effective when given with a specific HCN1 receptor inhibitor? What about a GABA<sub>A</sub>R inhibitor?'''
{| class="wikitable sortable"
|+ Caption text
|-
! Receptor !! Anesthetic Antagonist !! Off-Target Effects? !! Crosses BBB !! Approved for Humans
|-
| α1β2γ2 GABA<sub>A</sub>R || methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM) || Example || Example || Example
|-
| HCN1 || Example || Example || Example || Example
|-
| α4β4 nAChR || Example || Example || Example || Example
|-
| GluN1/N2C NMDAR || Example || Example || Example || Example
|-
| α<sub>2A</sub> AR || Example || Example || Example || Example
|-
| M<sub>3</sub> mAChR || Example || Example || Example || Example
|-
| K<sub>v</sub>1.2 || Example || Example || Example || Example
|}
*'''Are there genetic KO/KD or optogenetic tools available for location-specific inducible receptor knockdowns?'''
*'''Are there genetic KO/KD or optogenetic tools available for location-specific inducible receptor knockdowns?'''
**'''Is the receptor, its components, or homologues of the gene expressed in different model organisms? What is the sequence similarity with human?'''
**'''Is the receptor, its components, or homologues of the gene expressed in different model organisms? What is the sequence similarity with human?'''