TABLE 1

Binding selectivity profile of TC-1698 Data are mean percent inhibition of control binding (or activity) for duplicate determinations. No data denotes less than 25% change in binding at 10 μM TC-1698. For all non-nicotinic receptors tested, TC-1698 had an IC50 > 1 μM.


Binding Site

Radioligand

Inhibition (Percentage at 10 μM)
Acetylcholinesterase Acetylthiocholine
Adenosine, nonselective [3H]NECA
Adrenergic α1 (rat cortex) [3H]MeOxy-prazocin
Adrenergic α2 (rat cortex) [3H]RX-821002
Adrenergic β nonselective [3H]DHA
Angiotensin AT1 (human) [125I]-(Sar1-Ile8) angiotensin
Angiotensin AT2 [125I]Tyr4-angiotensin II
Calcium channel, type L [3H]Nitrendipine
Bradykinin, BK2 [3H]Bradykinin
Calcium channel, type N [3H]contoxin GVIA
Cholecystokinin, CCK1 (CCKA) [125I]CCK-8
Cholecystokinin, CCK2 (CCKB) [125I]CCK-8
Choline acetyltransferase [14C]-Acetyl Coenzyme
Glutamic acid decarboxylase [14C]-Glutamic Acid
Corticotropin-releasing factor [3H]-Tyr0-oCRF
Dopamine D3 (rat recombinant) [3H]Spiperone
Dopamine transporter [3H]-WIN 35,428
Endothelin ET-A (Human) [125I]-Endothelin1
Endothelin ET-B (Human) [125I]-Endothelin1
GABA (rat cortex) [3H]-GABA
Estrogen [125I] 3,17B-Estradiol, 16a
GABA-A, BDZ, α1, central [3H]-Flunitrazepam
GABA-B transporter (rat cortex) [3H]-CGP 5462A
Galanin, nonselective [125I] Galanin
Glycine (rat spinal cord) [3H]-Strychnine
Histamine H1 periph. (guinea pig lung) [3H]-Pyrilamine
Histamine H1 [3H]-Pyrilamine
Histamine H2 [3H]-Pyrilamine 39
Histamine H3 [3H]-Pyrilamine 60
Leukotriene B4, LTB4 [3H]-LTB4
Leukotriene D4, LTD4 [3H]-LTD4
Melatonin ML1 (chicken brain) [125I]-Iodomelatonin
Monoamine oxidase A, peripheral [14C]-5HT
Monoamine oxidase B, peripheral [14C]phenylethylamine
Muscarinic, M1 (human recombinant) [3H]-QNB
Muscarinic, M2 (human recombinant) [3H]-QNB 46
Muscarinic, nonselective central [3H]-QNB
Muscarinic, nonselective, peripheral [3H]-QNB
Neurokinin, NK1 [3H]-SP
Neurokinin, NK2 (human recombinant) [3H]-NKA
Neurokinin, NK3 (NKB) [3H]-Eledoisin
Nicotinic (rat cortex) [3H]-Cytisine 104
Norepinephrine transporter (rat cortex) [3H]-Nisoxetine
NOS (neuronal-binding) [3H]-NOARG
Opioids (rat cortex) [3H]-Naloxone
Oxytocin (rat uterus) [3H]-oxytocin
Platelet-activating factor, PAF Hexadecyl-[3H]-acetyl-PAF
Potassium KATP channels (rat cortex) [3H]-Glibenclamide
Potassium KVI channels (rat cortex) [125I]-Apamin
Potassium KVS channels (rat cortex) [125I]-Charybdotoxin
Serotonin transporter [3H]-Citalopram, N-methyl
Serotonin, nonselective [125I]-LSD
Sigma (rat cortex) [3H]-DTG 35
Sodium channels site 2 (rat cortex) [3H]-Batrachotoxin
Testosterone (cytosolic) [3H]-Methyltrienolone
Thromboxane A2 (Human) [3H]-SQ 29,548
Thyrotropin-releasing hormone, TRH [3H]-(3MeHis2)TRH
Vasoactive intestinal peptide [125I]-VIP
Vasopressin V1 (rat aortic A7r5 cells)
[3H]-AVP