Quantitative in vitro and in vivo pharmacological profile of CE-178253, a potent and selective cannabinoid type 1 (CB1) Receptor Antagonist

Table 2 Receptors, ion channels, and uptake sites measured for CE-178253 binding activity

Receptors	Ion Channels/Regulatory sites	Uptake sites
Adenosine (A₁, A_2a, 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 (B_1,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-HT_1A, 5-HT_2A, 5-HT_2C, 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.