TABLE 1

Target radiolabeled ligands inhibited or stimulated by ≥10% by 10 μM (5.57 μg/ml) omadacycline

TargetSource% inhibition or stimulationa
Adrenergic α1BRat15
Adrenergic α1DHuman14
Adrenergic β1Human11
Adrenergic β2Human−12
Bradykinin β1Human11
Calcium channel L type, benzothiazepineRat12
Calcium channel L type, dihydropyridineRat18
Dopamine D3Human12
GABAa, agonist siteRat14
Glutamate, kainiteRat14
Glutamate, N-methyl-d-aspartate, glycineRat14
Histamine H2Guinea pig19
M2Human82
M3Human13
Neuropeptide Y1Human11
Nicotinic acetylcholine, centralRat−18
Phorbol esterMouse14
5-Hydroxytriptamine, 5-HT1AHuman10
Sodium channel, site 2Rat19
  • a Positive values represent inhibition, and negative values represent stimulation.