Safety Pharmacology

Targets

We offer a qualitative and quantitative description of compound interactions with ion channels or GPC-receptor subtypes.

The table summarizes the available ion channels and GPC-receptor subtypes tested:

Ion channels	Assay	Preparation	Testing principle
hERG	Patch Clamp	hERG DUO cells	Reduction of tail current amplitudes
hERG	Papillary Muscle	Guinea pig	Increase in action potential duration
hERG	Langendorff Heart	Guinea pig or Rabbit	Increase of QT-intervals and QTc
Na+	Papillary Muscle	Guinea pig	Reduction of action potential amplitudes;    Decrease in muscle force
Ca2+	Papillary Muscle	Guinea pig	Reduction of action potential duration;      Decrease in muscle force
L-type Ca2+	Isolated Organs	Rabbit, aorta	Antagonism against KCl induced isometric contractions
GABA A	Isolated Organs	Guinea pig, ileum	Antagonism against muscimol-induced isometric contractions
Receptorsubtypes	Assay	Preparation	Testing principle
A1 Adenosine	Isolated Organs	Guinea pig, ileum	Antagonism against N6-CHA-induced reduction of twitch contraction amplitudes
A2A Adenosine	Isolated Organs	Rat, aorta	Antagonism against NECA-induced relaxation of isometric pre-contracted tissues by L-phenylephrine
A2B Adenosine	Isolated Organs	Guinea pig, aorta	Antagonism against NECA-induced relaxation of isometric pre-contracted tissues by L-phenylephrine
α1A Adrenoceptor	Isolated Organs	Rat, vas deferens	Antagonism against noradrenaline-induced isotonic contractions
α1B Adrenoceptor	Isolated Organs	Guinea pig, spleen	Antagonism against noradrenaline-induced isometric contractions
α1D Adrenoceptor	Isolated Organs	Rat, aorta	Antagonism against noradrenaline-induced isometric contractions
α2A Adrenoceptor	Isolated Organs	Rabbit, vas deferens	Antagonism against brimonidine-induced reduction of twitch contraction amplitudes
ß1 Adrenoceptor	Isolated Organs	Guinea pig, right atrium	Antagonism against isoprenaline-induced positive inotropy and chronotropy
ß2 Adrenoceptor	Isolated Organs	Guinea pig, trachea	Antagonism against isoprenaline-induced relaxation from isometric resting tension
D2 Dopamine	Isolated Organs	Mouse, vas deferens	Antagonism against dopamine-induced reduction of twitch contraction amplitudes
H1 Histamine	Isolated Organs	Guinea pig, ileum	Antagonism against histamine-induced isotonic contractions
H2 Histamine	Isolated Organs	Guinea pig, right atrium	Antagonism against histamine-induced positive inotropy and chronotropy
M1 Muscarinic Acetylcholine	Isolated Organs	Rabbit, vas deferens	Antagonism against McN-A-343-induced reduction of twitch contraction amplitudes
M2 Muscarinic Acetylcholine	Isolated Organs	Rabbit, vas deferens	Antagonism against carbachol-induced potentiation of twitch contraction amplitudes
M3 Muscarinic Acetylcholine	Isolated Organs	Guinea pig, gallbladder	Antagonism against Ach-induced isometric contractions
5-HT2B Serotonin	Isolated Organs	Rat, stomach fundus	Antagonism against 5-HT-induced isometric contractions