Table 2.
Receptors, ion channels, and uptake sites measured for CE-178253 binding activity
| Receptors | Ion Channels/Regulatory sites | Uptake sites |
|---|---|---|
| Adenosine (A1, A2a, A3) | Calcium channels: | Choline |
| Adrenergic (α1, α2, β1, β2) | L-type DHP | Dopamine |
| Angiotensin-II (AT1, AT2) | L-type (diltiazem) | GABA |
| Benzodiazepine | L-type (verapamil) | 5-HT |
| Bradykinin (B1,B2) | N-type | Norepinephrine |
| Dopamine (D1, D2, D3, D4) | ||
| GABA (non-selective) | Functional Assays | |
| Glutamate (AMPA, kainate, NMDA) | GPR55 (no activity at 10 μM) | |
| Histamine (H1, H2, H3) | TRPV1 (11% inhibition at 10 μM) | |
| 5-Hydroxytryptamine (5-HT1A, 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT7) | ||
| Melanocortin (MC4) | ||
| Muscarinic (M1, M2, M3, M4) | ||
| Nicotinic (neuronal, muscle) | ||
| Opiate (delta, kappa, mu) | ||
| Platelet activating factor | ||
| Steroid (glucocorticoid) | ||
| Tachykinin (NK1) | ||
| Thyroid hormone | ||
| Vasopressin (V1, V2) |
Inhibition CE-178253 was evaluated for inhibition of binding to the following receptors, channels and sites at 1 μM concentration (except where noted). CE-178253 did not inhibit binding by > 50% at any site noted in the panel.