TABLE 2

Pharmacological selectivity profile of BCTC (10 μM)


Target

Radioligand

Percentage of Inhibition
Neurotransmitter-related
    Adenosine, nonselective [3H]NECA -2.70
    Adrenergic, α1, nonselective [3H]7-MeOxy-Prazocin 1.69
    Adrenergic, α2, nonselective [3H]RX 821002 11.05
    Adrenergic, β, nonselective [3H]DHA 15.51
    Dopamine transporter [3H]WIN-35,428 -13.73
    Dopamine, nonselective [3H]Spiperone 13.13
    GABA A, agonist site [3H]GABA 14.71
    GABA A, benzodiazepine, α1, central [3H]Flunitrazepam -4.05
    GABA-B [3H]CGP 54626A 17.41
    Glutamate, AMPA site [3H]AMPA -14.53
    Glutamate, kainate site [3H]kainic acid 5.74
    Glutamate, NMDA agonist site [3H]CGP 39653 26.52
    Glutamate, NMDA, glycine (Strychnine-insens site) [3H]MDL-105,519 -9.76
    Glycine, strychnine-sensitive [3H]Strychnine 35.70
    Histamine, H1 [3H]Pyrilamine 37.10
    Histamine, H2 [125I]Aminopotentidine 6.46
    Histamine, H3 [3H]N-α-Me-histamine 6.57
    Melatonin [125I]2-lodomelatonin 4.34
    Muscarinic, M1 [3H]Scopolamine,N-methyl 16.32
    Muscarinic, M2 [3H]Scopolamine,N-methyl 6.88
    Muscarinic, nonselective, central [3H]QNB 7.02
    Muscarinic, nonselective, peripheral [3H]QNB -3.06
    Nicotinic (α-bungarotoxin-insensitive) [3H]Epibatidine 3.96
    Norepinephrine transporter [3H]Nisoxetine 13.20
    Opiate, nonselective [3H]Naloxone 85.85
    Serotonin transporter [3H]Citralopram,N-methyl -20.27
    Serotonin, nonselective [3H]LSD 4.78
    Sigma, nonselective [3H]DTG 8.05
Steroids
    Estrogen [125I]3, 17β-estradiol, 16α 12.87
    Testosterone (cytosolic) [3H]Methyltrienolone -7.04
Ion Channels
    Calcium channel, type L (dihydropyridine site) [3H]Nitrendipine 8.63
    Calcium channel, type N [125I]Conotoxin-GVIA 4.43
    Potassium channel, ATP-sensitive [3H]Glibenclamide 1.40
    Potassium channel, Ca2+ Act., VI [125I]Apamin 18.55
    Potassium channel, Ca2+ Act., VS [125I]Charybdotoxin 7.95
    Sodium, site 1 [3H]Saxitoxin 1.50
    Sodium, site 2 [3H]Batrachotoxin A 20-α-benzo 24.02
Second Messengers
    NOS (neuronal-binding) [3H]NOARG -8.55
Prostaglandins
    Leukotriene B4, LTB4 [3H]LTB4 14.28
    Leukotriene D4, LTD4 [3H]LTD4 28.00
    Thromboxane A2 [3H]SQ 29,548 -2.35
Growth Factors/Hormones
    Corticotropin-releasing factor [125I]Tyr0-oCRF 5.52
    Oxytocin [3H]Oxytocin -21.82
    Platelet-activating factor [3H]Hexadecyl, PAF -2.87
    Thyrotropin-releasing hormone [3H](3-Methyl-His2)-TRH -16.67
Brain/Gut Peptides
    Angiotensin II, AT1 [125I](Sar1-Ile8)-Angiotensin 11.12
    Angiotensin II, AT2 [125I](Tyr4)-Angiotensin II 29.72
    Bradykinin, BK2 [3H]Bradykinin 13.35
    Cholecystokinin, CCK1 (CCKA) [125I]CCK-8 16.81
    Cholecystokinin, CCK2 (CCKB) [125I]CCK-8 -2.06
    Endothelin, ET-A [125I]Endothelin-1 8.28
    Endothelin, ET-B [125I]Endothelin-1 28.39
    Galanin [125I]Galanin -10.65
    Neurokinin, NK1 [3H]Substance P -3.11
    Neurokinin, NK2 (NKA) [125I]NKA -9.72
    Neurokinin, NK3 (NKB) [125I]Eledoisin 14.56
    Vasoactive intestinal peptide, nonselective [125I]VIP 16.84
    Vasopressin 1 [3H]Vasopressin-1 antagonist 8.35
Enzymes
    Acetylcholinesterase Acetylthiocholine 2.38
    Choline Acetyltransferase [14C]Acetyl coenzyme 12.39
    Glutamic acid decarboxylase [14C]Glutamic acid -14.78
    Monoamine oxidase A, peripheral [14C]5HT -1.25
    Monoamine oxidase B, peripheral
[14C]Phenylethylamine
5.24