TABLE 2

Interaction of TASP0433864 with a broad selection of other neurotransmitter targets

Results are expressed as the percent inhibition of control-specific binding by TASP0433864 at a concentration of 10 µM.

TargetSpeciesSourceLigand or Substrate% Inhibition at 10 µMIC50
µM
5-HT1BRatRat cerebral cortex[125I]P450 (+ 30 μM isoproterenol)
5-HT2AHumanHuman recombinant (HEK-293 cells)[3H]Ketanserin
5-HT2BHumanHuman recombinant (CHO cells)[3H]Mesulergine724.0
5-HT2CHumanHuman recombinant (HEK-293 cells)[3H]Mesulergine
5-HT3HumanHuman recombinant (CHO cells)[3H]BRL 43694
5-HT7HumanHuman recombinant (CHO cells)[3H]LSD
α1RatRat cerebral cortex[3H]Prazosin
α2AHumanHuman recombinant (CHO cells)[3H]RX 82100212
α2CHumanHuman recombinant (CHO cells)[3H]RX 821002
β1HumanHuman recombinant (HEK-293 cells)[3H](−)CGP 12177
β2HumanHuman recombinant (CHO cells)[3H](−)CGP 12177
D1HumanHuman recombinant (CHO cells)[3H]SCH 23390
D2LRatRat striatum[3H]Raclopride
M1HumanHuman recombinant (CHO cells)[3H]Pirenzepine
M2HumanHuman recombinant (CHO cells)[3H]AF-DX 384
M4HumanHuman recombinant (CHO cells)[3H]N-Methyl-scopolamine
AT1HumanHuman recombinant (HEK-293 cells)[125I][Sar1,Ile8]-AT-II
CCK1 (CCKA)HumanHuman recombinant (CHO cells)[125I]CCK-8s
ETAHumanHuman recombinant (CHO cells)[125I]Endothelin-1
GAL1HumanHuman recombinant (HEK-293 cells)[125I]Galanin
NK1HumanU-373MG cells (endogenous)[125I]BH-SP
NK2HumanHuman recombinant (CHO cells)[125I]NKA
A1HumanHuman recombinant (CHO cells)[3H]DPCPX17
CB1HumanHuman recombinant (CHO cells)[3H]CP-55,94015
μRatRat cerebral cortex[3H]DAMGO
δ2 (DOP)HumanHuman recombinant (CHO cells)[3H]DADLE
σ1HumanJurkat cells[3H]Pentazocine
P2XRatRat urinary bladder[3H]α,β-MeATP
P2YRatRat cerebral cortex[35S]dATPαS
EP1HumanHuman recombinant (HEK-293 cells)[3H]PGE2
CysLT1 (LTD4)HumanHuman recombinant (CHO cells)[3H]LTD4
GRHumanIM-9 cells (cytosol)[3H]Dexamethasone
AMPARatRat cerebral cortex[3H]AMPA13
KainateRatRat cerebral cortex[3H]Kainic acid27
NMDARatRat cerebral cortex[3H]CGP 39653
nACh α7HumanSH-SY5Y cells (endogenous)[125I]α-Bungarotoxin
BZD (central)RatRat cerebral cortex[3H]Flunitrazepam
BZD (peripheral)RatRat heart[3H]PK 11195
GABAA1HumanHuman recombinant (CHO cells)[3H]Muscimol
GABAB(1b)HumanHuman recombinant (CHO cells)[3H]CGP 54626
MAO-ARatRat cerebral cortex[3H]Ro 41-1049
MAO-BHumanHuman recombinantd-Luciferin derivative (4 μM)920.59
Ca2+ channel (L-type, dihydropyridine site)RatRat cerebral cortex[3H]Nitrendipine
KV channelRatRat cerebral cortex[125I]α-Dendrotoxin
SKCa channelRatRat cerebral cortex[125I]Apamin
Norepinephrine transporterHumanHuman recombinant (CHO cells)[3H]Nisoxetine
Dopamine transporterHumanHuman recombinant (CHO cells)[3H]BTCP13
Choline transporter (CHT1)HumanHuman recombinant (CHO cells)[3H]Hemicholinium-3
  • −, inhibition of less than 10%; A, adenosine receptor; AF-DX 384, N-[2-[2-[(dipropylamino)methyl]-1-piperidinyl]ethyl]-5,6-dihydro-6-oxo-11H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide; AMPA, 2-amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propanoic acid; AT, angiotensin receptor; AT-II, angiotensin II; BH-SP, Bolton Hunter-labelled substance P; BRL 43694, granisetron; BTCP, N-[1-(2-benzo(b)thiophenyl)cyclohexyl]piperidine; BZD, benzodiazepine receptor; CB, cannabinoid receptor; CCK, cholecystokinin receptor; CCK-8s, cholecystokinin-8s; (−)CGP 12177, (−)4-[3-(tert-butylamino)-2-hydroxypropoxy]-1,3-dihydrobenzimidazol-2-one; CGP 39653, d,l-(E)-2-amino-4-propyl-5-phosphono-3-pentenoic acid; CGP 54626, [S-(R*,R*)]-[3-[[1-(3,4-dichlorophenyl)ethyl]amino]-2-hydroxypropyl](cyclohexylmethyl) phosphinic acid; CHO, chinese hamster ovary; CP-55,940, 2-[(1R,2R,5R)-5-hydroxy-2-(3-hydroxypropyl) cyclohexyl]-5-(2-methyloctan-2-yl)phenol; CYP, cyanopindolol; CysLT, cysteinyl leukotriene receptor; DADLE, [d-Ala2, d-Leu5]enkephalin; DAMGO, [d-Ala2, NMe-Phe4, Gly-ol5]enkephalin; dATPαS, deoxyadenosine 5′(α-thio)triphosphate; DOP, δ-opioid receptor; DPCPX, 8-cyclopentyl-1,3-dipropylxanthine; EP, prostaglandin E receptor; ET, endothelin receptor; GAL, galanin receptor; GR, glucocorticoid receptor; HEK, human embryonic kidney; 5-HT, serotonin receptor; KV channel, voltage-gated potassium channel; LSD, lysergic acid diethylamide; LTD4, leukotriene D4; MAO, monoamine oxidase; α,β-MeATP, α,β-methyleneadenosine 5′-triphosphate; nACh, nicotinic acetylcholine receptor; NK, neurokinin receptor; NKA, neurokinin A; PGE2, prostaglandin E2; PK 11195, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide; Ro 41-1049, N-(2-aminoethyl)-5-(3-fluorophenyl)-4-thiazolecarboxamide; RX 821002, 2-(2,3-dihydro-2-methoxy-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole; SCH 23390, 7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine; SKCa channel, small conductance calcium-activated potassium channel.