-
1
-
-
79957785934
-
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity
-
Banala A.K., Levy B.A., Khatri S.S., Furman C.A., Roof R.A., Mishra Y., Griffin S.A., Sibley D.R., Luedtke R.R., Newman A.H. N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity. J. Med. Chem. 2011, 54:3581-3594.
-
(2011)
J. Med. Chem.
, vol.54
, pp. 3581-3594
-
-
Banala, A.K.1
Levy, B.A.2
Khatri, S.S.3
Furman, C.A.4
Roof, R.A.5
Mishra, Y.6
Griffin, S.A.7
Sibley, D.R.8
Luedtke, R.R.9
Newman, A.H.10
-
2
-
-
79952032110
-
The physiology, signaling, and pharmacology of dopamine receptors
-
Beaulieu J.M., Gainetdinov R.R. The physiology, signaling, and pharmacology of dopamine receptors. Pharmacol. Rev. 2011, 63:182-217.
-
(2011)
Pharmacol. Rev.
, vol.63
, pp. 182-217
-
-
Beaulieu, J.M.1
Gainetdinov, R.R.2
-
3
-
-
84875921632
-
Modification of cocaine self-administration by buspirone (buspar(R)): potential involvement of D3 and D4 dopamine receptors
-
Bergman J., Roof R.A., Furman C.A., Conroy J.L., Mello N.K., Sibley D.R., Skolnick P. Modification of cocaine self-administration by buspirone (buspar(R)): potential involvement of D3 and D4 dopamine receptors. Int. J. Neuropsychopharmacol 2013, 16:445-458.
-
(2013)
Int. J. Neuropsychopharmacol
, vol.16
, pp. 445-458
-
-
Bergman, J.1
Roof, R.A.2
Furman, C.A.3
Conroy, J.L.4
Mello, N.K.5
Sibley, D.R.6
Skolnick, P.7
-
4
-
-
33748032418
-
The structural evolution of dopamine D3 receptor ligands: structure-activity relationships and selected neuropharmacological aspects
-
Boeckler F., Gmeiner P. The structural evolution of dopamine D3 receptor ligands: structure-activity relationships and selected neuropharmacological aspects. Pharmacol. Ther. 2006, 112:281-333.
-
(2006)
Pharmacol. Ther.
, vol.112
, pp. 281-333
-
-
Boeckler, F.1
Gmeiner, P.2
-
5
-
-
0015861774
-
Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction
-
Cheng Y., Prusoff W.H. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 1973, 22:3099-3108.
-
(1973)
Biochem. Pharmacol.
, vol.22
, pp. 3099-3108
-
-
Cheng, Y.1
Prusoff, W.H.2
-
6
-
-
78449305788
-
Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist
-
Chien E.Y., Liu W., Zhao Q., Katritch V., Han G.W., Hanson M.A., Shi L., Newman A.H., Javitch J.A., Cherezov V., Stevens R.C. Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist. Science 2010, 330:1091-1095.
-
(2010)
Science
, vol.330
, pp. 1091-1095
-
-
Chien, E.Y.1
Liu, W.2
Zhao, Q.3
Katritch, V.4
Han, G.W.5
Hanson, M.A.6
Shi, L.7
Newman, A.H.8
Javitch, J.A.9
Cherezov, V.10
Stevens, R.C.11
-
7
-
-
0036258990
-
G protein-coupled receptor allosterism and complexing
-
Christopoulos A., Kenakin T. G protein-coupled receptor allosterism and complexing. Pharmacol. Rev. 2002, 54:323-374.
-
(2002)
Pharmacol. Rev.
, vol.54
, pp. 323-374
-
-
Christopoulos, A.1
Kenakin, T.2
-
8
-
-
84880591671
-
D1-D2 dopamine receptor synergy promotes calcium signaling via multiple mechanisms
-
Chun L.S., Free R.B., Doyle T.B., Huang X.P., Rankin M.L., Sibley D.R. D1-D2 dopamine receptor synergy promotes calcium signaling via multiple mechanisms. Mol. Pharmacol. 2013, 84:190-200.
-
(2013)
Mol. Pharmacol.
, vol.84
, pp. 190-200
-
-
Chun, L.S.1
Free, R.B.2
Doyle, T.B.3
Huang, X.P.4
Rankin, M.L.5
Sibley, D.R.6
-
9
-
-
58149193205
-
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nature reviews
-
Conn P.J., Christopoulos A., Lindsley C.W. Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nature reviews. Drug Discovery 2009, 8:41-54.
-
(2009)
Drug Discovery
, vol.8
, pp. 41-54
-
-
Conn, P.J.1
Christopoulos, A.2
Lindsley, C.W.3
-
10
-
-
13444287717
-
Novel heterocyclic trans olefin analogues of N-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor
-
Grundt P., Carlson E.E., Cao J., Bennett C.J., McElveen E., Taylor M., Luedtke R.R., Newman A.H. Novel heterocyclic trans olefin analogues of N-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor. J. Med. Chem. 2005, 48:839-848.
-
(2005)
J. Med. Chem.
, vol.48
, pp. 839-848
-
-
Grundt, P.1
Carlson, E.E.2
Cao, J.3
Bennett, C.J.4
McElveen, E.5
Taylor, M.6
Luedtke, R.R.7
Newman, A.H.8
-
11
-
-
34548138905
-
Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents
-
Grundt P., Prevatt K.M., Cao J., Taylor M., Floresca C.Z., Choi J.K., Jenkins B.G., Luedtke R.R., Newman A.H. Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents. J. Med. Chem. 2007, 50:4135-4146.
-
(2007)
J. Med. Chem.
, vol.50
, pp. 4135-4146
-
-
Grundt, P.1
Prevatt, K.M.2
Cao, J.3
Taylor, M.4
Floresca, C.Z.5
Choi, J.K.6
Jenkins, B.G.7
Luedtke, R.R.8
Newman, A.H.9
-
12
-
-
77949300041
-
Current perspectives on selective dopamine D(3) receptor antagonists as pharmacotherapeutics for addictions and related disorders
-
Heidbreder C.A., Newman A.H. Current perspectives on selective dopamine D(3) receptor antagonists as pharmacotherapeutics for addictions and related disorders. Ann. N. Y. Acad. Sci. 2010, 1187:4-34.
-
(2010)
Ann. N. Y. Acad. Sci.
, vol.1187
, pp. 4-34
-
-
Heidbreder, C.A.1
Newman, A.H.2
-
13
-
-
21544439847
-
Dopamine D3 receptor antagonists as therapeutic agents
-
Joyce J.N., Millan M.J. Dopamine D3 receptor antagonists as therapeutic agents. Drug Discovery Today 2005, 10:917-925.
-
(2005)
Drug Discovery Today
, vol.10
, pp. 917-925
-
-
Joyce, J.N.1
Millan, M.J.2
-
14
-
-
84893175454
-
Beyond small-molecule SAR: using the dopamine D3 receptor crystal structure to guide drug design
-
Keck T.M., Burzynski C., Shi L., Newman A.H. Beyond small-molecule SAR: using the dopamine D3 receptor crystal structure to guide drug design. Adv. Pharmacol. 2014, 69:267-300.
-
(2014)
Adv. Pharmacol.
, vol.69
, pp. 267-300
-
-
Keck, T.M.1
Burzynski, C.2
Shi, L.3
Newman, A.H.4
-
15
-
-
78149496159
-
Allosteric modulation of G protein-coupled receptors: a pharmacological perspective
-
Keov P., Sexton P.M., Christopoulos A. Allosteric modulation of G protein-coupled receptors: a pharmacological perspective. Neuropharmacology 2011, 60:24-35.
-
(2011)
Neuropharmacology
, vol.60
, pp. 24-35
-
-
Keov, P.1
Sexton, P.M.2
Christopoulos, A.3
-
16
-
-
84883172335
-
Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M(1) muscarinic acetylcholine receptor
-
Keov P., Valant C., Devine S.M., Lane J.R., Scammells P.J., Sexton P.M., Christopoulos A. Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M(1) muscarinic acetylcholine receptor. Mol. Pharmacol. 2013, 84:425-437.
-
(2013)
Mol. Pharmacol.
, vol.84
, pp. 425-437
-
-
Keov, P.1
Valant, C.2
Devine, S.M.3
Lane, J.R.4
Scammells, P.J.5
Sexton, P.M.6
Christopoulos, A.7
-
17
-
-
67349158011
-
Evaluation of the D3 dopamine receptor selective antagonist PG01037 on L-dopa-dependent abnormal involuntary movements in rats
-
Kumar R., Riddle L., Griffin S.A., Grundt P., Newman A.H., Luedtke R.R. Evaluation of the D3 dopamine receptor selective antagonist PG01037 on L-dopa-dependent abnormal involuntary movements in rats. Neuropharmacology 2009, 56:944-955.
-
(2009)
Neuropharmacology
, vol.56
, pp. 944-955
-
-
Kumar, R.1
Riddle, L.2
Griffin, S.A.3
Grundt, P.4
Newman, A.H.5
Luedtke, R.R.6
-
18
-
-
84876525643
-
Regulation of G protein-coupled receptors by allosteric ligands
-
Lane J.R., Abdul-Ridha A., Canals M. Regulation of G protein-coupled receptors by allosteric ligands. ACS Chem. Neurosci. 2013, 4:527-534.
-
(2013)
ACS Chem. Neurosci.
, vol.4
, pp. 527-534
-
-
Lane, J.R.1
Abdul-Ridha, A.2
Canals, M.3
-
19
-
-
84906306554
-
A new mechanism of allostery in a G protein-coupled receptor dimer
-
Lane J.R., Donthamsetti P., Shonberg J., Draper-Joyce C.J., Dentry S., Michino M., Shi L., Scammells P.J., Capuano B., Sexton P.M., Javitch J.A., Christopoulos A. A new mechanism of allostery in a G protein-coupled receptor dimer. Nat Chem Biol. 2014, 10(9):745-752.
-
(2014)
Nat Chem Biol.
, vol.10
, Issue.9
, pp. 745-752
-
-
Lane, J.R.1
Donthamsetti, P.2
Shonberg, J.3
Draper-Joyce, C.J.4
Dentry, S.5
Michino, M.6
Shi, L.7
Scammells, P.J.8
Capuano, B.9
Sexton, P.M.10
Javitch, J.A.11
Christopoulos, A.12
-
21
-
-
79952454207
-
Recent advances in the search for D3- and D4-selective drugs: probes, models and candidates
-
Lober S., Hubner H., Tschammer N., Gmeiner P. Recent advances in the search for D3- and D4-selective drugs: probes, models and candidates. Trends Pharmacol. Sci. 2011, 32:148-157.
-
(2011)
Trends Pharmacol. Sci.
, vol.32
, pp. 148-157
-
-
Lober, S.1
Hubner, H.2
Tschammer, N.3
Gmeiner, P.4
-
22
-
-
33847122495
-
Allosteric modulation of G protein-coupled receptors
-
May L.T., Leach K., Sexton P.M., Christopoulos A. Allosteric modulation of G protein-coupled receptors. Ann. Rev. Pharmacol. Toxicol. 2007, 47:1-51.
-
(2007)
Ann. Rev. Pharmacol. Toxicol.
, vol.47
, pp. 1-51
-
-
May, L.T.1
Leach, K.2
Sexton, P.M.3
Christopoulos, A.4
-
23
-
-
84874027543
-
Dopamine D3 receptor antagonists: a patent review (2007-2012)
-
Micheli F., Heidbreder C. Dopamine D3 receptor antagonists: a patent review (2007-2012). Expert Opin. Ther. Patents 2013, 23:363-381.
-
(2013)
Expert Opin. Ther. Patents
, vol.23
, pp. 363-381
-
-
Micheli, F.1
Heidbreder, C.2
-
24
-
-
84888863473
-
A single glycine in extracellular loop 1 is the critical determinant for pharmacological specificity of dopamine D2 and D3 receptors
-
Michino M., Donthamsetti P., Beuming T., Banala A., Duan L., Roux T., Han Y., Trinquet E., Newman A.H., Javitch J.A., Shi L. A single glycine in extracellular loop 1 is the critical determinant for pharmacological specificity of dopamine D2 and D3 receptors. Mol. Pharmacol. 2013, 84:854-864.
-
(2013)
Mol. Pharmacol.
, vol.84
, pp. 854-864
-
-
Michino, M.1
Donthamsetti, P.2
Beuming, T.3
Banala, A.4
Duan, L.5
Roux, T.6
Han, Y.7
Trinquet, E.8
Newman, A.H.9
Javitch, J.A.10
Shi, L.11
-
25
-
-
6844250767
-
Dopamine receptors: from structure to function
-
Missale C., Nash S.R., Robinson S.W., Jaber M., Caron M.G. Dopamine receptors: from structure to function. Physiol. Rev. 1998, 78:189-225.
-
(1998)
Physiol. Rev.
, vol.78
, pp. 189-225
-
-
Missale, C.1
Nash, S.R.2
Robinson, S.W.3
Jaber, M.4
Caron, M.G.5
-
26
-
-
84871446904
-
Occupancy of brain dopamine D3 receptors and drug craving: a translational approach
-
(official publication of the American College of Neuropsychopharmacology)
-
Mugnaini M., Iavarone L., Cavallini P., Griffante C., Oliosi B., Savoia C., Beaver J., Rabiner E.A., Micheli F., Heidbreder C., Andorn A., Merlo Pich E., Bani M. Occupancy of brain dopamine D3 receptors and drug craving: a translational approach. Neuropsychopharmacology 2013, 38:302-312. (official publication of the American College of Neuropsychopharmacology).
-
(2013)
Neuropsychopharmacology
, vol.38
, pp. 302-312
-
-
Mugnaini, M.1
Iavarone, L.2
Cavallini, P.3
Griffante, C.4
Oliosi, B.5
Savoia, C.6
Beaver, J.7
Rabiner, E.A.8
Micheli, F.9
Heidbreder, C.10
Andorn, A.11
Merlo Pich, E.12
Bani, M.13
-
27
-
-
84864938692
-
Molecular determinants of selectivity and efficacy at the dopamine D3 receptor
-
Newman A.H., Beuming T., Banala A.K., Donthamsetti P., Pongetti K., LaBounty A., Levy B., Cao J., Michino M., Luedtke R.R., Javitch J.A., Shi L. Molecular determinants of selectivity and efficacy at the dopamine D3 receptor. J. Med. Chem. 2012, 55:6689-6699.
-
(2012)
J. Med. Chem.
, vol.55
, pp. 6689-6699
-
-
Newman, A.H.1
Beuming, T.2
Banala, A.K.3
Donthamsetti, P.4
Pongetti, K.5
LaBounty, A.6
Levy, B.7
Cao, J.8
Michino, M.9
Luedtke, R.R.10
Javitch, J.A.11
Shi, L.12
-
28
-
-
84865513282
-
Medication discovery for addiction: translating the dopamine D3 receptor hypothesis
-
Newman A.H., Blaylock B.L., Nader M.A., Bergman J., Sibley D.R., Skolnick P. Medication discovery for addiction: translating the dopamine D3 receptor hypothesis. Biochem. Pharmacol. 2012, 84:882-890.
-
(2012)
Biochem. Pharmacol.
, vol.84
, pp. 882-890
-
-
Newman, A.H.1
Blaylock, B.L.2
Nader, M.A.3
Bergman, J.4
Sibley, D.R.5
Skolnick, P.6
-
29
-
-
0038548068
-
N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists
-
Newman A.H., Cao J., Bennett C.J., Robarge M.J., Freeman R.A., Luedtke R.R. N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists. Bioorg. Med. Chem. Lett. 2003, 13:2179-2183.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 2179-2183
-
-
Newman, A.H.1
Cao, J.2
Bennett, C.J.3
Robarge, M.J.4
Freeman, R.A.5
Luedtke, R.R.6
-
30
-
-
65249161020
-
N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists
-
Newman A.H., Grundt P., Cyriac G., Deschamps J.R., Taylor M., Kumar R., Ho D., Luedtke R.R. N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists. J. Med.Chem. 2009, 52:2559-2570.
-
(2009)
J. Med.Chem.
, vol.52
, pp. 2559-2570
-
-
Newman, A.H.1
Grundt, P.2
Cyriac, G.3
Deschamps, J.R.4
Taylor, M.5
Kumar, R.6
Ho, D.7
Luedtke, R.R.8
-
31
-
-
78650804442
-
Evaluation of the D3 dopamine receptor selective agonist/partial agonist PG01042 on L-dopa dependent animal involuntary movements in rats
-
Riddle L.R., Kumar R., Griffin S.A., Grundt P., Newman A.H., Luedtke R.R. Evaluation of the D3 dopamine receptor selective agonist/partial agonist PG01042 on L-dopa dependent animal involuntary movements in rats. Neuropharmacology 2011, 60:284-294.
-
(2011)
Neuropharmacology
, vol.60
, pp. 284-294
-
-
Riddle, L.R.1
Kumar, R.2
Griffin, S.A.3
Grundt, P.4
Newman, A.H.5
Luedtke, R.R.6
-
32
-
-
70349820514
-
Pharmacotherapy of addictive disorders
-
Ross S., Peselow E. Pharmacotherapy of addictive disorders. Clin. Neuropharmacol. 2009, 32:277-289.
-
(2009)
Clin. Neuropharmacol.
, vol.32
, pp. 277-289
-
-
Ross, S.1
Peselow, E.2
-
34
-
-
77958134183
-
The tetrahydroisoquinoline derivative SB269,652 is an allosteric antagonist at dopamine D3 and D2 receptors
-
Silvano E., Millan M.J., Mannoury la Cour C., Han Y., Duan L., Griffin S.A., Luedtke R.R., Aloisi G., Rossi M., Zazzeroni F., Javitch J.A., Maggio R. The tetrahydroisoquinoline derivative SB269,652 is an allosteric antagonist at dopamine D3 and D2 receptors. Mol. Pharmacol. 2010, 78:925-934.
-
(2010)
Mol. Pharmacol.
, vol.78
, pp. 925-934
-
-
Silvano, E.1
Millan, M.J.2
Mannoury la Cour, C.3
Han, Y.4
Duan, L.5
Griffin, S.A.6
Luedtke, R.R.7
Aloisi, G.8
Rossi, M.9
Zazzeroni, F.10
Javitch, J.A.11
Maggio, R.12
-
35
-
-
57649170953
-
A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand
-
Valant C., Gregory K.J., Hall N.E., Scammells P.J., Lew M.J., Sexton P.M., Christopoulos A. A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand. J. Biol. Chem. 2008, 283:29312-29321.
-
(2008)
J. Biol. Chem.
, vol.283
, pp. 29312-29321
-
-
Valant, C.1
Gregory, K.J.2
Hall, N.E.3
Scammells, P.J.4
Lew, M.J.5
Sexton, P.M.6
Christopoulos, A.7
-
36
-
-
84896987724
-
Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist
-
Valant C., May L.T., Aurelio L., Chuo C.H., White P.J., Baltos J.A., Sexton P.M., Scammells P.J., Christopoulos A. Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Proc. Natl. Acad. Sci. U.S.A. 2014, 111:4614-4619.
-
(2014)
Proc. Natl. Acad. Sci. U.S.A.
, vol.111
, pp. 4614-4619
-
-
Valant, C.1
May, L.T.2
Aurelio, L.3
Chuo, C.H.4
White, P.J.5
Baltos, J.A.6
Sexton, P.M.7
Scammells, P.J.8
Christopoulos, A.9
-
37
-
-
84855879360
-
The best of both worlds? Bitopic orthosteric/allosteric ligands of g protein-coupled receptors
-
Valant C., Robert Lane J., Sexton P.M., Christopoulos A. The best of both worlds? Bitopic orthosteric/allosteric ligands of g protein-coupled receptors. Annu. Rev. Pharmacol. Toxicol. 2012, 52:153-178.
-
(2012)
Annu. Rev. Pharmacol. Toxicol.
, vol.52
, pp. 153-178
-
-
Valant, C.1
Robert Lane, J.2
Sexton, P.M.3
Christopoulos, A.4
-
38
-
-
67650489125
-
Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs
-
Valant C., Sexton P.M., Christopoulos A. Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs. Mol. Intervent. 2009, 9:125-135.
-
(2009)
Mol. Intervent.
, vol.9
, pp. 125-135
-
-
Valant, C.1
Sexton, P.M.2
Christopoulos, A.3
-
39
-
-
84881271660
-
Emerging paradigms in GPCR allostery: implications for drug discovery. Nature reviews
-
Wootten D., Christopoulos A., Sexton P.M. Emerging paradigms in GPCR allostery: implications for drug discovery. Nature reviews. Drug Discovery 2013, 12:630-644.
-
(2013)
Drug Discovery
, vol.12
, pp. 630-644
-
-
Wootten, D.1
Christopoulos, A.2
Sexton, P.M.3
|