Target Validation Information
TTD ID T67162
Target Name Dopamine D2 receptor (D2R)
Type of Target
Successful
Drug Potency against Target Amisulpride Drug Info IC50 = 21 nM
Aripiprazole Drug Info IC50 = 1.78 nM [79]
Bromocriptine Drug Info Ki = 12.2 nM [103]
Cabergoline Drug Info Ki = 0.62 nM [104]
Chlorpromazine Drug Info Ki = 50 nM [90]
Chlorprothixene Drug Info Ki = 3.9 nM [82]
Clozapine Drug Info Ki = 2.6 nM [102]
Dopamine Drug Info EC50 = 66.2 nM [93]
Ephedrine Drug Info Ki = 236 nM [93]
Fluphenazine Drug Info Ki = 14.0 nM [104]
Haloperidol Drug Info Ki = 2.6 nM [102]
Lisuride Drug Info Ki = 0.73 nM [103]
Loxapine Drug Info Ki = 50 nM [90]
Metoclopramide Drug Info IC50 = 483 nM [81]
Naphazoline Drug Info IC50 = 1100 nM/L [98]
Olanzapine Drug Info Ki = 50 nM [90]
Pergolide Drug Info Ki = 0.51 nM [103]
Phenoxybenzamine Drug Info IC50 = 100 nM [106]
Phentolamine Drug Info pKi = 7.46 [95]
Phenylephrine Drug Info pKi = 6320 nM
Pramipexole Drug Info Ki = 3.9 nM [80]
Pseudoephedrine Drug Info pKi = 4190 nM
Quetiapine Drug Info Ki = 8.1 nM [102]
Quinagolide Drug Info Ki = 0.52 nM
Risperidone Drug Info Ki = 0.2 nM [102]
Ropinirole Drug Info IC50 = 540 nM [112]
Sulpiride Drug Info IC50 = 10000 nM [92]
Thioridazine Drug Info Ki = 100 nM [104]
Tolazoline Drug Info IC50 = 390 nM [86]
Ziprasidone Drug Info IC50 = 0.42 nM [14]
Aplindore fumarate Drug Info IC50 = 2.82 nM [79]
Asenapine Drug Info Ki = 1.3 nM [100]
Bifeprunox Drug Info Ki = 64.6 nM [88]
Bifeprunox Drug Info Ki = 1.48 nM [88]
BIM23A760 Drug Info IC50 = 18.3 nM [101]
Blonanserin Drug Info Ki = 2020 nM [109]
Iloperidone Drug Info Ki = 110 nM [108]
Lurasidone hydrochloride Drug Info Ki = 1.68 nM [97]
Ocaperidone Drug Info Ki = 0.75 nM [85]
PD-158771 Drug Info Ki = 5.2 nM [113]
SLV-313 Drug Info Ki = 3.98 nM [91]
SSR-181507 Drug Info Ki = 0.84 nM [84]
1192U90 Drug Info Ki = 32 nM [110]
Drug Info Ki = 0.9 nM [27]
(+)-(1R,1'S)-berbamunine hydrochloride Drug Info IC50 = 300 nM
(+)-(1R,1'S)-thaligrisine hydrochloride Drug Info IC50 = 27 nM
(+)-BUTACLAMOL Drug Info Ki = 3.61 nM [13]
(+/-)-nantenine Drug Info Ki = 858 nM [46]
(-)-(1S,1'R)-O,O-dimethylgrisbine hydrochloride Drug Info IC50 = 1450 nM
(-)-3-(1-Propyl-piperidin-3-yl)-benzonitrile Drug Info Ki = 119 nM [68]
(4-Ethynyl-cyclohex-3-enyl)-dipropyl-amine Drug Info Ki = 250 nM [3]
(4-Quinolin-2-ylpiperazin-1-yl)acetic Acid Drug Info Ki = 919 nM [36]
(5-Methoxy-chroman-3-yl)-dipropyl-amine Drug Info IC50 = 50 nM [71]
(R)-(+)-coclaurine Drug Info IC50 = 130 nM [75]
(R)-(-)-10-methyl-11-hydroxyaporphine Drug Info Ki = 11500 nM [21]
(R)-(-)-11-hydroxy-N-n-propylnoraporphine Drug Info Ki = 28.5 nM [27]
(R)-(-)-2-methoxy-11-hydroxyaporphine Drug Info Ki = 235 nM [27]
(R)-(-)-2-methoxy-N-npropylnorapomorphine Drug Info Ki = 1.3 nM [27]
(R)-(-)-2-Methyl-apomorphine hydrochloride Drug Info Ki = 20.7 nM [28]
(R)-(-)-2-Phenyl-apomorphine hydrochloride Drug Info Ki = 11.7 nM [28]
(R)-(-)-N-ethyl-2-methoxy-11-hydroxynoraporphine Drug Info Ki = 28 nM [27]
(R)-(-)-N-propyl-2-methoxy-11-hydroxynoraporphine Drug Info Ki = 44 nM [27]
(S)-BULBOCAPNINE Drug Info IC50 = 14000 nM [20]
(S)-secoantioquine hydrochloride Drug Info IC50 = 10000 nM
(S)APOMORPHINE Drug Info Ki = 58.3 nM [43]
(S,R)-antioquine hydrochloride Drug Info IC50 = 3180 nM
(S,R)-isotetrandrine hydrochloride Drug Info IC50 = 670 nM
(S,R)-pseudoxandrine hydrochloride Drug Info IC50 = 16200 nM
(S,S)-oxandrine hydrochloride Drug Info IC50 = 2760 nM
1,2,3,7,12,12a-hexahydro-1-aza-pleiadene-5,6-diol Drug Info Ki = 8000 nM [20]
1,2-Bis-[R-(-)-apomorphine-2'-oxy]ethane Drug Info Ki = 345 nM [29]
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane Drug Info Ki = 11 nM [49]
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane Drug Info Ki = 27 nM [49]
1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane Drug Info Ki = 159 nM [49]
1,6-bis(4-m-tolylpiperazin-1-yl)hexane Drug Info Ki = 70 nM [49]
1,6-bis(4-phenylpiperazin-1-yl)hexane Drug Info Ki = 1 nM [49]
1-(3-Hydroxyphenyl)-4-propylpiperazine Drug Info Ki = 69 nM [48]
1-(4-(1H-pyrazol-1-yl)benzyl)-4-phenylpiperazine Drug Info Ki = 2400 nM [18]
1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one Drug Info Ki = 286 nM [22]
1-(benzyloxy)-2-(2-phenylethyl)benzene Drug Info Ki = 5000 nM [19]
1-(benzyloxy)-2-[2-(3-methoxyphenyl)ethyl]benzene Drug Info Ki = 5000 nM [19]
1-Aminomethyl-3-cyclohexyl-isochroman-5,6-diol Drug Info Ki = 1120 nM [30]
1-Aminomethyl-isochroman-5,6-diol Drug Info Ki = 4610 nM [45]
1-Benzyl-4-(2-ethynyl-pyrrol-1-yl)-piperidine Drug Info Ki = 6300 nM [2]
1-Benzyl-4-(2-iodo-pyrrol-1-yl)-piperidine Drug Info Ki = 5300 nM [2]
1-Benzyl-4-(2-oxazol-5-yl-pyrrol-1-yl)-piperidine Drug Info Ki = 320 nM [2]
1-Benzyl-4-(3-hydroxyphenyl)piperidine Drug Info Ki = 35 nM [48]
1-Benzyl-4-(3-oxazol-5-yl-pyrrol-1-yl)-piperidine Drug Info Ki = 3200 nM [2]
1-Benzyl-4-pyrrol-1-yl-piperidine Drug Info Ki = 9800 nM [2]
1-Benzyl-4-[3-(methylsulfonyl)phenyl]piperazine Drug Info Ki = 431 nM [48]
1-Benzyl-4-[3-(methylsulfonyl)phenyl]piperidine Drug Info Ki = 392 nM [48]
1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine Drug Info IC50 = 1500 nM [61]
1-Methyl-1,2,3,4-tetrahydro-isoquinoline-6,7-diol Drug Info Ki = 5400 nM
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine Drug Info Ki = 151 nM
1-Propyl-3-m-tolyl-piperidine hydrochloride Drug Info Ki = 15900 nM [6]
1-Propyl-3-o-tolyl-piperidine hydrochloride Drug Info Ki = 1510 nM [6]
1-Propyl-3-p-tolyl-piperidine hydrochloride Drug Info Ki = 13800 nM [6]
1-[(3-methoxybenzyl)oxy]-2-(2-phenylethyl)benzene Drug Info Ki = 5000 nM [19]
1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine Drug Info Ki = 1015 nM [9]
1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine Drug Info Ki = 1006 nM [9]
1-[3-(Methylsulfonyl)phenyl]-4-propylpiperazine Drug Info Ki = 664 nM [48]
2,3-Dihydro-1H-indol-5-ol Drug Info Ki = 9400 nM
2-(4-Dipropylamino-cyclohexylidene)-malononitrile Drug Info Ki = 15000 nM [3]
2-methoxyapomorphine Drug Info Ki = 74 nM [29]
2-Methyl-8-phenyl-1,2,3,4-tetrahydro-isoquinoline Drug Info IC50 = 27 nM [63]
2-{[2-(2-phenylethyl)phenoxy]methyl}pyridine Drug Info Ki = 5000 nM [19]
2-{[R-(-)-Apomorphine-2'-oxy]ethoxy}-ethanol Drug Info Ki = 587 nM [29]
3,8-dibromoboldine Drug Info IC50 = 1910 nM [4]
3-(1-Propyl-pyrrolidin-3-yl)-phenol Drug Info Ki = 68 nM
3-(2,3-Dimethyl-phenyl)-1-propyl-piperidine Drug Info Ki = 4900 nM [76]
3-(2,3-Dimethyl-phenyl)-piperidine Drug Info Ki = 16000 nM [76]
3-(2,4-Dimethyl-phenyl)-1-propyl-piperidine Drug Info Ki = 17000 nM [76]
3-(2,5-Dimethyl-phenyl)-1-propyl-piperidine Drug Info Ki = 540 nM [76]
3-(2,6-Dimethyl-phenyl)-1-propyl-piperidine Drug Info Ki = 156 nM [76]
3-(2-Benzylamino-ethoxy)-phenol Drug Info Ki = 101 nM [1]
3-(3,4-Dimethyl-phenyl)-1-propyl-piperidine Drug Info Ki = 4990 nM [76]
3-(3,4-Dimethyl-phenyl)-piperidine Drug Info Ki = 19000 nM [76]
3-(3,5-Dimethyl-phenyl)-1-propyl-piperidine Drug Info Ki = 1300 nM [76]
3-(3,5-Dimethyl-phenyl)-piperidine Drug Info Ki = 240 nM [76]
3-(4-Benzyl-piperazin-1-yl)-phenol Drug Info Ki = 5.5 nM [78]
3-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one Drug Info Ki = 1093 nM [13]
3-(4-Methyl-piperidin-1-ylmethyl)-1H-indole Drug Info Ki = 5500 nM [70]
3-(4-Phenyl-piperazin-1-ylmethyl)-1H-indole Drug Info Ki = 120 nM [70]
3-(4-Phenyl-piperidin-1-ylmethyl)-1H-indole Drug Info Ki = 110 nM [70]
3-(N-propylpiperidin-4-yl)phenol Drug Info Ki = 349 nM [48]
3-(Octahydro-quinolizin-1-yl)-phenol Drug Info IC50 = 13000 nM [40]
3-(Octahydro-quinolizin-3-yl)-phenol Drug Info IC50 = 7900 nM [40]
3-bromoboldine Drug Info IC50 = 1050 nM [4]
3-Butyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol Drug Info IC50 = 12000 nM [8]
3-Chloroboldine Drug Info IC50 = 720 nM [4]
3-Cyclohexyl-1-propyl-piperidine hydrochloride Drug Info Ki = 14400 nM [6]
3-Ethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol Drug Info IC50 = 14000 nM [8]
3-Iodoboldine Drug Info IC50 = 96 nM [4]
3-Naphthalen-1-yl-1-propyl-pyrrolidine Drug Info Ki = 71 nM
3-Naphthalen-1-yl-pyrrolidine Drug Info Ki = 264 nM
3-Phenyl-1-propyl-piperidine hydrochloride Drug Info Ki = 10800 nM [6]
3-Phenyl-1-propyl-pyrrolidine Drug Info Ki = 625 nM
3-Phenyl-pyrrolidine Drug Info IC50 = 486 nM
3-{[2-(2-phenylethyl)phenoxy]methyl}pyridine Drug Info Ki = 5000 nM [19]
4-(2-Benzylamino-ethoxy)-1,3-dihydro-indol-2-one Drug Info Ki = 11.4 nM [1]
4-(4-Benzyl-piperazin-1-yl)-1H-benzoimidazole Drug Info Ki = 9.7 nM [78]
4-(4-Benzyl-piperazin-1-yl)-1H-indole Drug Info Ki = 3.2 nM [78]
4-(4-Benzyl-piperazin-1-yl)-5-chloro-1H-indole Drug Info Ki = 9.1 nM [78]
4-(4-Benzyl-piperazin-1-yl)-7-bromo-1H-indole Drug Info Ki = 26.8 nM [78]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [51]
4-Benzyl-1-chroman-2-ylmethyl-piperidine Drug Info Ki = 924 nM [13]
4-Benzyl-1-chroman-3-ylmethyl-piperidine Drug Info Ki = 2493 nM [13]
4-Benzyl-1-indan-2-ylmethyl-piperidine Drug Info Ki = 575 nM [13]
5-OH-DPAT Drug Info Ki = 58.8 nM [47]
7-(2-Amino-ethyl)-4-hydroxy-3H-benzothiazol-2-one Drug Info IC50 = 2000 nM [58]
7-(2-Dipropylamino-ethyl)-3H-benzothiazol-2-one Drug Info IC50 = 1000 nM [58]
A-437203 Drug Info Ki = 351 nM [17]
A-68930 Drug Info Ki = 807 nM [45]
A-690344 Drug Info Ki = 320 nM [17]
A-706149 Drug Info Ki = 246 nM [16]
A-80426 Drug Info Ki = 52 nM [14]
ANOLOBINE Drug Info IC50 = 15000 nM [20]
ANONAINE Drug Info IC50 = 19000 nM [20]
Azaperone Drug Info Ki = 52 nM [65]
Benzyl-[2-(1H-indazol-4-yloxy)-ethyl]-amine Drug Info Ki = 35.9 nM [1]
Benzyl-[2-(1H-indol-4-yloxy)-ethyl]-amine Drug Info Ki = 39.3 nM [1]
Bis-{[R-(-)-apomorphine-2-oxy]ethyl} ether Drug Info Ki = 17158 nM [29]
BOLDINE Drug Info IC50 = 520 nM [4]
BP-897 Drug Info Ki = 162 nM [12]
BRL-25594 Drug Info Ki = 0.28 nM [7]
CLEBOPRIDE Drug Info Ki = 11.9 nM [7]
D-189 Drug Info Ki = 1835 nM [31]
D-190 Drug Info Ki = 189 nM [31]
D-192 Drug Info Ki = 813 nM [31]
D-193 Drug Info Ki = 915 nM [31]
D-203 Drug Info Ki = 769 nM [31]
D-210 Drug Info Ki = 166 nM [31]
D-218 Drug Info Ki = 81.2 nM [31]
D-219 Drug Info Ki = 68.4 nM [31]
D-220 Drug Info Ki = 34.9 nM [31]
D-264 Drug Info Ki = 264 nM [37]
D-315 Drug Info Ki = 40.6 nM [50]
D-366 Drug Info Ki = 47.5 nM [47]
Ecopipam Drug Info Ki = 514 nM [56]
Ethyl-(4,5,6,7-tetrahydro-2H-indazol-5-yl)-amine Drug Info IC50 = 11600 nM [54]
ETICLOPRIDE Drug Info Ki = 0.12 nM [41]
Etoloxamine Drug Info Ki = 2024 nM [9]
FLUANISONE Drug Info Ki = 2.9 nM [57]
FLUMEZAPINE Drug Info IC50 = 20 nM [55]
FLUTROLINE Drug Info IC50 = 14 nM [60]
GLAUCINE Drug Info Ki = 2800 nM [20]
IBZM Drug Info Ki = 0.43 nM [67]
IODOPRIDE Drug Info Ki = 3 nM [67]
IODOSULPIRIDE Drug Info Ki = 1.5 nM [67]
ISOCLOZAPINE Drug Info IC50 = 13 nM [74]
ISOLOXAPINE Drug Info IC50 = 2480 nM [62]
L-741626 Drug Info Ki = 10 nM
Levacecarnine hci Drug Info Ki = 1272 nM [25]
MAZAPERTINE Drug Info Ki = 2.2 nM [66]
MCL-515 Drug Info Ki = 18.9 nM [35]
MCL-516 Drug Info Ki = 192 nM [35]
N-(4-Dipropylaminobutyl)-4-biphenylcarboxamide Drug Info Ki = 8800 nM [33]
N-Benzyl-4-(2-diphenyl)-1-piperazinehexanamide Drug Info Ki = 503 nM [32]
N-Ethyl-2-methylnorapomorphine hydrochloride Drug Info Ki = 115 nM [38]
N-Ethyl-2-phenylnorapomorphine hydrochloride Drug Info Ki = 14 nM [38]
N-Propyl-2-methylnorapomorphine hydrochloride Drug Info Ki = 9.2 nM [38]
N-Propyl-2-phenylnorapomorphine hydrochloride Drug Info Ki = 192 nM [38]
NLX-101 Drug Info Ki = 15000 nM [53]
NOR-ROEFRACTINE Drug Info IC50 = 5000 nM [75]
OCTOCLOTHEPIN Drug Info Ki = 0.67 nM [52]
PD-128483 Drug Info IC50 = 2920 nM
PD-135111 Drug Info IC50 = 436 nM
PD-135146 Drug Info IC50 = 2430 nM
PD-135188 Drug Info IC50 = 352 nM
PD-135222 Drug Info IC50 = 1180 nM
PD-135385 Drug Info IC50 = 412 nM
PD-135478 Drug Info IC50 = 600 nM
PD-135540 Drug Info IC50 = 128 nM
PD-137789 Drug Info IC50 = 704 nM
PD-137821 Drug Info IC50 = 545 nM
PD-168077 Drug Info Ki = 18300 nM [6]
PD-172938 Drug Info Ki = 5882 nM [77]
PD-172939 Drug Info Ki = 2748 nM [77]
PG-01037 Drug Info IC50 = 80.9 nM [24]
Phenyltoloxamine Drug Info Ki = 2740 nM [9]
Preclamol Drug Info IC50 = 3400 nM [40]
Pridopidine Drug Info Ki = 7521 nM [48]
Propyl-(4,5,6,7-tetrahydro-2H-indazol-5-yl)-amine Drug Info IC50 = 15200 nM [54]
PUKATEINE Drug Info IC50 = 600 nM [20]
QUINPIROLE Drug Info Ki = 1500 nM [76]
Ro-21-7767 Drug Info IC50 = 121 nM [64]
ROXINDOLE Drug Info IC50 = 5.6 nM [11]
RWJ-25730 Drug Info Ki = 0.8 nM [66]
SB-258719 Drug Info Ki = 3981 nM [5]
SB-269970 Drug Info Ki = 316 nM [5]
SB-271046 Drug Info Ki = 460 nM [26]
SCH-24518 Drug Info Ki = 676 nM [59]
SK&F-89626 Drug Info IC50 = 285 nM [42]
SKF-89124A Drug Info IC50 = 530 nM [58]
SLV-314 Drug Info Ki = 6.9 nM [15]
SNAP-94847 Drug Info Ki = 7400 nM [23]
STEPHOLIDINE Drug Info Ki = 974 nM [44]
Sumanirole Drug Info Ki = 9 nM [72]
TIOSPIRONE Drug Info Ki = 0.58 nM [69]
UH-232 Drug Info Ki = 15 nM
UH-301 Drug Info Ki = 400 nM [73]
WAY-208466 Drug Info IC50 < 5000 nM [39]
[2-(1H-Benzoimidazol-4-yloxy)-ethyl]-benzyl-amine Drug Info Ki = 128 nM [1]
[3H]7-OH-DPAT Drug Info Ki = 311 nM [34]
[3H]N-methylspiperone Drug Info Ki = 0.118 nM [10]
[3H]spiperone Drug Info Ki = 0.42 nM [13]
[R-(-)-Apomorphine-2-yl]-(2'-hydroxy-ethyl)ether Drug Info Ki = 347 nM [29]
Action against Disease Model Acetophenazine Drug Info AR competitive ligand binding assays, demonstrated competition for [3H]mibolerone binding Ki: 800 nM [96]
Clozapine Drug Info We examined the feasibility of coupling the 5-HT(6) receptor to a Ca(2+) signaling read-out using a chimeric G-protein, comprising of G(alphaq) with the C-terminal five amino acids from G(alphas), to facilitate assays on the fluorometric imaging plate reader (FLIPR). Using a transient transfection assay in h uMan embryonic kidney (HEK) cells, Ca(2+) signaling in response to serotonin (5-HT) was facilitated by co-transfection of the 5-HT(6) receptor with the G(alphaq)/G(alphas) chimera, but not with the 5-HT(6) receptor alone or with a similar chimera incorporating the C-terminal five amino acids of G(alphai3). A series of agonist concentration-response curves were constructed using the 5-HT(6)-G(alphaq)/G(alphas) signaling assay generating the following rank order ofagonist potency; 5-methoxytryptamine (EC(50), 9 nM)=5-HT (12 nM)=2-methyl 5-HT (13 nM)>tryptamine (86 nM)=5-carboxamidotryptamine (5-CT) (119 nM)>>lisuride (>1 microM). In comparison, essentially identical EC(50) values were observed for the stimulation of cAMP acc uMulation with the same compounds; 5-methoxytryptamine (EC(50), 6 nM)=5-HT (6 nM)=2-methyl 5-HT (15 nM)>tryptamine (91 nM)=5-CT (153 nM)>lisuride (>350 nM). Clozapine and SB 271046 both produced a concentration-dependent antagonism of the 5-HT-stimulated Ca(2+) response with IC(50) values of 45 and 11 nM, respectively. In contrast,aripiprazole, a recently launched atypical anti-psychotic with a novel mechanism of action described as a dopamine/serotonin stabilizer, was essentially devoid of 5-HT(6) receptor antagonist activity. Our results demonstrate that a FLIPR-based Ca(2+) signaling assay is a feasible approach to the functional characterization of 5-HT(6) receptor ligands. Moreover, the equivalent coupling efficiency,as indexed by agonist potency, observed using this system compared with the native coupling assay to cAMP suggests that the C-terminal five amino acids of G(alphas) are the major determinant for the receptor/G-protein interaction of the 5-HT(6) receptor subtype. [83]
Domperidone Drug Info HERG-Lite monitors the expression of hERG at the cell surface in two different stable mammalian cell lines. One cell line acts as a biosensor for drugs that inhibit hERG trafficking, while the other predicts hERG blockers based on their ability to act as pharmacological chaperones. In this study, we have validated the HERG-Lite assay using a panel of 100 drugs: 50 hERG blockers and 50 nonblockers.HERG-Lite correctly predicted hERG risk for all 100 test compounds with no false positives or negatives. All 50 hERG blockers were detected as drugs with hERG risk in the HERG-Lite assay, and fell into two classes: B (for blocker) and C (for complex; block and trafficking inhibition). [89]
Droperidol Drug Info HERG-Lite monitors the expression of hERG at the cell surface in two different stable mammalian cell lines. One cell line acts as a biosensor for drugs that inhibit hERG trafficking, while the other predicts hERG blockers based on their ability to act as pharmacological chaperones. In this study, we have validated the HERG-Lite assay using a panel of 100 drugs: 50 hERG blockers and 50 nonblockers.HERG-Lite correctly predicted hERG risk for all 100 test compounds with no false positives or negatives. All 50 hERG blockers were detected as drugs with hERG risk in the HERG-Lite assay, and fell into two classes: B (for blocker) and C (for complex; block and trafficking inhibition). [89]
Fluspirilene Drug Info HERG-Lite monitors the expression of hERG at the cell surface in two different stable mammalian cell lines. One cell line acts as a biosensor for drugs that inhibit hERG trafficking, while the other predicts hERG blockers based on their ability to act as pharmacological chaperones. In this study, we have validated the HERG-Lite assay using a panel of 100 drugs: 50 hERG blockers and 50 nonblockers.IC50 on hERG: 3nM [89]
Haloperidol Drug Info HERG-Lite monitors the expression of hERG at the cell surface in two different stable mammalian cell lines. One cell line acts as a biosensor for drugs that inhibit hERG trafficking, while the other predicts hERG blockers based on their ability to act as pharmacological chaperones. In this study, we have validated the HERG-Lite assay using a panel of 100 drugs: 50 hERG blockers and 50 nonblockers.IC50 on hERG: 19nM [89]
Lisuride Drug Info In primary cerebellar granule cell model(D1) EC50: 530 nM [111]
Olanzapine Drug Info DHA transport was inhibited in cells of neuronal/glial and blood cell origin but in detail on B-lymphoblastoids. IC50: 15000 nM [87]
Phentolamine Drug Info In rat aorta at 27.5 ???C, the IC50 value of phentolamine against 0.1 |?m of phenylephrine: 8.8 nM. [94]
Pimozide Drug Info HERG-Lite monitors the expression of hERG at the cell surface in two different stable mammalian cell lines. One cell line acts as a biosensor for drugs that inhibit hERG trafficking, while the other predicts hERG blockers based on their ability to act as pharmacological chaperones. In this study, we have validated the HERG-Lite assay using a panel of 100 drugs: 50 hERG blockers and 50 nonblockers.IC50 on hERG: 1nM [89]
Pramipexole Drug Info To determine whether antiparkinson dopamine agonists preferentially act on the high-affinity or the low-affinity states of dopamine D1 and D2 receptors, the agonist potencies were obtained by competition against [(3)H]SCH23390 for D1(High) and D1(Low), and against [(3)H]domperidone for D2(High) and D2(Low). N-propylnorapomorphine and cabergoline were the most potent at D2(High), with dissociation constants of 0.18 and 0.36 nM, respectively. Other agonists had D2(High)K(i) values of 0.52 nM for quinagolide, 0.6 nM for (+)PHNO, 0.9 for bromocriptine, 1.8 nM for apomorphine, 2.4 nM for pergolide, 3 nM for quinpirole, and 6.2 nM for lergotrile. There was a clear correlation between the K(i) values at D2(High) and their therapeutic concentrations in the plasma water, as derived from the known concentrations after correction for the fraction bound to the h uMan plasma proteins. The data suggest that D2(High) is the primary and common target for the antiparkinson actionof dopamine agonists. Bromocriptine, cabergoline, lergotrile, pergolide, and pramipexole had no affinity for D1(High), consistent with the clinical observations that the D2-selective bromocriptine and pramipexole elicit low levels of dyskinesia. [99]
Remoxipride Drug Info The novel substituted benzamide, remoxipride, preferentially blocked apomorphine-induced hyperactivity with weak effects on stereotypies. The potency of remoxipride was about 50times higher than that of sulpiride. Remoxipride caused a weak, atypical form of catalepsy and showed a high separation between the ED50 for blockade of apomorphine-induced hyperactivity and the ED50for induction of catalepsy (ratio 24). Remoxipride was shown to be a selective dopamine D2 receptor antagonist since it displaced [3H]spiperone (IC50 = 1570 nM) but not [3H]flupentixol (IC50 greater than 100 000 nM) in rat striat uM, and did not inhibit striatal DA-sensitive adenylate cyclase in vitro (IC50 greater than 100 000 nM). Remoxipride is a potent antagonist of D2 receptors showing a dose-dependent blockade of [3H]spiperone and [3H]n-propylnorapomorphine in vivo binding with a potency equal to that of chlorpromazine. In contrast to haloperidol, remoxipride caused a preferential blockade of in vivo [3H]spierone binding in the mesolimbic DA rich areas and the substantia nigra with much less effect in the striat uM. In addition, remoxipride produced a preferential increase of DA utilization following synthesis inhibition in the olfactory tubercle. Only minor changes in NA and 5-HT metabolism were observed while HVA and DOPAC levels were markedly elevated. Taken together, these results indicate that remoxipride is a potent, selective D2 receptor blocking agent with a preferential action in mesolimbic and extrastriatal dopamine-containing neurons. [107]
Risperidone Drug Info IC50 on serotonin-induced 32P-phosphatidic acid formation in h uMan blood platelets: 0.5 nM [105]
Thioridazine Drug Info HERG-Lite monitors the expression of hERG at the cell surface in two different stable mammalian cell lines. One cell line acts as a biosensor for drugs that inhibit hERG trafficking, while the other predicts hERG blockers based on their ability to act as pharmacological chaperones. In this study, we have validated the HERG-Lite assay using a panel of 100 drugs: 50 hERG blockers and 50 nonblockers.HERG-Lite correctly predicted hERG risk for all 100 test compounds with no false positives or negatives. All 50 hERG blockers were detected as drugs with hERG risk in the HERG-Lite assay, and fell into two classes: B (for blocker) and C (for complex; block and trafficking inhibition). [89]
Thiothixene Drug Info cls-Thiothixene Inhibitionn of [ 3 H]rauwolscine ([ 3 H]RAUW) specific binding to a2-receptor sites m bovine caudate nucleus IC50: 640 nM
References
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