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Table 1 Pharmacological agents used for reverse microdialysis

From: Redundant Gs-coupled serotonin receptors regulate amyloid-β metabolism in vivo

Compound Target IC50 or Ki Rev MD Concentration Dosage Across MD Membrane Selectivity Limit Reference
Agonists       
Ipsapirone 5-HT1AR 10 nM 1 μM 100 nM 58 nMa [59]
WAY161503 5-HT2CR 4 nM 400 nM 40 nM 233 nM [60]
ML10302 5-HT4R 4 nM 400 nM 40 nM 700 nM [61]
ST1936 5-HT6R 13 nM 1.3 μM 130 nM 168 nM [62]
AS19 5-HT7R 0.83 nM 83 nM 8.3 nM 6.6 nMb [63]
Antagonists       
GR113808 5-HT4R 0.02 nM 100 nM 10 nM 10 μM [64]
SB258719 5-HT7R 31.6 nM 3.16 μM 316 nM 316 nM [68]
Inhibitors       
GM6001 ADAM/MMP 0.5 nM-27 nM 2.5 μM 250 nM NA [66]
KT5720 PKA 60 nM 6 μM 600 nM 2 μM [67]
PKI14-22 PKA 36 nM 3.6 μM 360 nM 15 μM [65]
  1. All agents were chosen for their selectivity for their targets as assayed in previous literature. We used the Ki and IC50 values to determine necessary concentrations of each compound (reverse microdialysis (Rev MD) concentration). We assumed only 10 % of the drug would cross the membrane (Dosage Across MD membrane), and this amount of the compound would be further diluted in the brain ISF. The selectivity limit is the concentration above which each compound begins stimulating off-target receptors
  2. aIpsapirone has been shown to stimulate bovine α-adrenergic receptors at 58 nM in vitro [59]
  3. bAS19 can stimulate 5-HT1DR at 6.6 nM concentrations in vitro [63]. However, expression of this receptor is absent in adult mouse hippocampus [14], so effects of its stimulation should be neglible
  4. Abbreviations: 5-HTR serotonin receptor, ADAM a disintegrin and metallopeptidase domain, MMP matrix metallopeptidase, PKA protein kinase A