TABLE 4

Broad Cerep screen undertaken to determine the pharmacological activity of fenobam


Target

% Control (10 μM)

Target

% Control (10 μM)
A1 (h) 89.9 Opiate (nonsel) 114.8
A2A (h) 96.7 ORL1 (h) 101.4
A3 (h) 35.3 PCP 95.3
α1 (nonsel) 103.3 P2X 108.5
α2 (nonsel) 102.1 P2Y 95.8
β1 (h) 95.9 5-HT (nonsel) 94.1
β2 (h) 79.0 σ1 88.2
AT1 (h) 91.2 σ2 79.2
AT2 (h) 109.6 Glucocorticoid (h) 96.7
GABAA-BZD 97.6 Estrogen (h) 100.2
B1 108.5 Progesterone (h) 105.8
B2 (h) 102.1 Androgen (h) 108.0
CB1 (h) 95.0 TRH 90.6
CB2 (h) 100.5 V1 103.7
CCKA (h) 112.8 V2 (h) 109.4
CCKB (h) 84.8 Ca2+ L channel (DHP) 96.7
CRF1 106.9 Ca2+ L channel (dilt) 104.6
D1 (h) 100.0 Ca2+ L channel (verap) 150.9
D2 (h) 95.3 K+ ATP channel 136
D3 (h) 100.6 K+ V channel 103.6
D4.4 (h) 86.7 SK+ Ca2+ channel 97.9
ETA (h) 93.3 Na+ channel 88.9
ETB (h) 85.1 Cl channel 103.7
GABA (nonsel) 107.5 ADO transporter 99.6
AMPA 93.1 NE transporter (h) 99.9
Kainate 103.2 DA transporter (h) 98.2
NMDA 91.9 GABA transporter 104.7
Glycine (strych-sens) 126.2 Choline transporter 81.4
Glycine (strych-insens) 104.1 5-HT transporter (h) 101.2
H1 89.9 PDE I 100.3
H2 97.6 PDE II (h) 99.1
H3 89.8 PDE III (h) 95.9
I1 83.2 PDE IV (h) 93.4
I2 66.3 PDE V (h) 106.3
LTB4 (h) 99.0 PKC 96.0
LTD4 (h) 106.2 COMT 98.9
MC4 (h) 92.2 GABA transaminase 94.6
M (nonsel) 94.6 Glu. decarboxylase 105.7
NK1 (h) 102.2 MAO-A (h) 70.5
NK2 (h) 89.7 PNMT 88.9
NK3 (h) 104.1 TH 122.6
NPY (nonsel) 102.5 ATPase 97.4
N (neuronal)
119.4
Acetylcholinesterase (h)
98.5
  • h, human; nonsel, nonselective; NMDA, N-methyl-d-aspartate; AMPA, α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid; PDE, phosphodiesterase; PKC, protein kinase C; PNMT, phenylethanolamine-N-methyltransferase; MAO-A, monoamineoxidase-A; COMT, catechol-O-methyl transferase; LTB, leukotriene B; LTD, leukotriene D; NPY, neuropeptide Y; ET, endothelin; CRF, corticotrophin-releasing factor; CCK, cholecystokinin; CB, cannabinoid; 5-HT, serotonin; TRH, thyrotrophin-releasing factor; DHP, dihydropyridine; ADO, adenosine; NE, norepinephrine; DA, dopamine; TH, tyrosine hydroxylase; Dilt, diltiazem; Verap, verapamil; PCP, phencyclidine; P2X, purinergic 2X; P2Y, purinergic 2Y; BZD, benzodiazepine.