Quinpirole is a non-peptide dopamine D2 receptor agonist that is used in research to study the role of dopamine in various physiological processes, including movement, reward, and cognition. It is a synthetic compound that was first developed in the 1980s. Quinpirole is known to have high affinity for dopamine D2 receptors, particularly the D2 subtype. It can cross the blood-brain barrier and exert its effects on the central nervous system. Quinpirole has been used to investigate the role of dopamine in movement disorders such as Parkinson's disease and Huntington's disease. It has also been studied in animal models of addiction and schizophrenia. Quinpirole is a valuable tool in neuroscience research due to its high selectivity for dopamine receptors and its ability to mimic the effects of dopamine. Studies using quinpirole have provided insights into the mechanisms of action of dopamine and the role of dopamine in various neurological and psychiatric disorders.'
Quinpirole: A dopamine D2/D3 receptor agonist. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
quinpirole : A pyrazoloquinoline that is (4aR,8aR)-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrazolo[3,4-g]quinoline substituted by a propyl group at position 5. It acts as a dopamine agonist. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 54562 |
| CHEMBL ID | 240773 |
| CHEBI ID | 75401 |
| SCHEMBL ID | 50905 |
| SCHEMBL ID | 11048143 |
| MeSH ID | M0028678 |
| Synonym |
|---|
| BRD-K26548821-001-01-8 |
| BRD-K26548821-003-03-0 |
| gtpl2 |
| (4ar,8ar)-5-propyl-1,4,4a,6,7,8,8a,9-octahydropyrido[2,3-f]indazole |
| PRESTWICK3_001093 |
| BIOMOL-NT_000014 |
| LOPAC0_000990 |
| BPBIO1_001284 |
| 1h-pyrazolo(3,4-g)quinoline, 4,4a,5,6,7,8,8a,9-octahydro-5-propyl-, (4ar-trans)- |
| (4ar-trans)-4,4a,5,6,7,8,8a,9-octahydro-5-propyl-1h-pyrazolo(3,4-g)quinoline |
| 1h-pyrazolo(3,4-g)quinoline, 4,4a,5,6,7,8,8a,9-octahydro-5-propyl-, dihydrochloride, (e)-, (+-)- |
| quinpirole [inn] |
| quinpirolum [latin] |
| quinpirol [spanish] |
| trans-(+-)-5-propyl-4,4a,5,6,7,8,8a,9-octahydro-1h-pyrazolo(3,4-g)quinoline dihydrochloride |
| ly 156258 |
| tocris-1061 |
| cas-85760-74-3 |
| lopac-q-102 |
| NCGC00024974-01 |
| NCGC00015866-01 |
| NCGC00015866-02 |
| NCGC00016954-01 |
| lopac-q-111 |
| PRESTWICK2_001093 |
| LOPAC0_001030 |
| BSPBIO_001166 |
| AB00514646 |
| quinpirole |
| SPBIO_003053 |
| PRESTWICK0_001093 |
| PRESTWICK1_001093 |
| BPBIO1_001169 |
| 85760-74-3 |
| HMS2089L17 |
| NCGC00016954-06 |
| NCGC00016954-07 |
| CHEMBL240773 , |
| (4ar,8ar)-5-propyl-1,4,4a,6,7,8,8a,9-octahydropyrazolo[3,4-g]quinoline |
| chebi:75401 , |
| bdbm50018958 |
| NCGC00016954-05 |
| A841444 |
| unii-20op60125t |
| 20op60125t , |
| 80373-22-4 |
| quinpirol |
| quinpirolum |
| 74196-92-2 |
| (4ar,8ar)-5-propyl-4,4a,5,6,7,8,8a,9-octahydro-1h-pyrazolo[3,4-g]quinoline |
| CCG-205070 |
| bdbm84637 |
| cas_85760-74-3 |
| quinpirole,(-) |
| nsc_54562 |
| NCGC00016954-02 |
| NCGC00016954-08 |
| AKOS015895855 |
| quinpirole [who-dd] |
| (-)-(4ar,8ar)-4,4a,5,6,7,8,8a,9-octahydro-5-propyl-1h-pyrazolo(3,4-g)quinoline |
| SCHEMBL50905 |
| SCHEMBL11048143 |
| DTXSID9048229 |
| (4as,8as)-5-propyl-1,4,4a,6,7,8,8a,9-octahydropyrazolo[3,4-g]quinolinedihydrochloride |
| Q253187 |
| SDCCGSBI-0050963.P003 |
| NCGC00016954-17 |
| quinpirol-(-) |
Quinpirole is a dopamine agonist with high affinity for the D2 and D3 dopamine receptor subtypes. While ropinirole exhibits selectivity toward D2, D3, and D4 receptors.
Quinpirole (LY 171555) has been reported to have a 113-fold greater affinity for dopamine D3 receptors than for D2 receptors. It is a selective D2 dopamine agonist. A recent report has indicated that it may have high affinity for a novel dopamine binding site called D3.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Quinpirole (LY 171555) has also been reported to have a 113-fold greater affinity for dopamine D3 receptors than for D2 receptors." | ( Effects of putative dopamine D3 receptor agonists, 7-OH-DPAT, and quinpirole, on yawning, stereotypy, and body temperature in rats. Furukawa, T; Kurashima, M; Nagashima, M; Shirakawa, K; Yamada, K, 1995) | 1.25 |
| "Quinpirole has been reported to be a selective D2 dopamine agonist; however, a recent report has indicated that it may have high affinity for a novel dopamine binding site which has been termed D3." | ( Autoradiographic localization of [3H]quinpirole binding to dopamine D2 and D3 receptors in rat brain. Gackenheimer, SL; Gehlert, DR; Schaus, J; Seeman, P, 1992) | 1.28 |
Quinpirole did not produce any effect in isolated uterus from oestrogenized rats even when it is contracted by KCl (37 mM) It did not enhance contractile responses to acetylcholine and carbachol, but in high concentrations induced contractions.
| Excerpt | Reference | Relevance |
|---|---|---|
| "1. Quinpirole did not produce any effect in isolated uterus from oestrogenized rats even when it is contracted by KCl (37 mM). " | ( Response to dopamine agonists of the rat isolated uterus. Berenguer, A; Estañ, L; Martinez-Mir, I; Morales-Olivas, FJ; Rubio, E, 1993) | 0.91 |
| "Quinpirole did not inhibit monoamine oxidase-A or monoamine oxidase-B activity and had low affinity (200 nM) for sigma site(s)." | ( Monoamine oxidase inhibitors inhibit [3H]quinpirole binding in rat striatal membranes. DeSouza, EB; Grigoriadis, DE; Levant, B, 1993) | 1.27 |
| "Quinpirole did not enhance contractile responses to acetylcholine and carbachol, but in high concentrations induced contractions in unstimulated preparations." | ( Influence of the DA2-receptor agonist quinpirole on the guinea pig ileum. Guenaneche, F; Lefebvre, RA, 1990) | 1.27 |
| "Quinpirole failed to inhibit the stimulation of TH elicited by dibutyryl cyclic AMP (2 mM), which acts independently of adenylate cyclase." | ( Involvement of adenylate cyclase inhibition in dopamine autoreceptor regulation of tyrosine hydroxylase in rat nucleus accumbens. Olianas, MC; Onali, P, 1989) | 1 |
Quinpirole-treated rats organized and updated their progression primarily according to the proximal layout of landmarks, but did so with excessive repetitions compared with saline- treated rats. Treatment with quin pirole (2 mg/kg/day) decreased the size of colonic lesions in rats with iodoacetamide-ind.
Clonidine and the slightly alpha 1-selective agonist ST587, but not ST91, produced marked stimulation when combined with the selective D2 agonist quinpirole. The drugs were studied alone and in combination with cocaine for their effects on locomotor activity in non-habituated mice.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Clonidine and the slightly alpha 1-selective agonist ST587, but not ST91, an alpha-agonist which does not readily cross the blood brain barrier, produced marked stimulation when combined with the selective D2 agonist quinpirole." | ( Alpha 1 (but not alpha 2)-adrenoceptor agonists in combination with the dopamine D2 agonist quinpirole produce locomotor stimulation in dopamine-depleted mice. Edis, LE; Eshel, G; Jackson, DM; Kelder, D; Ross, SB, 1990) | 0.68 |
| " Furthermore, the data indicate that in normal rats D-1 receptors are functionally relevant since D-1 agonists facilitate the expression of oral stereotyped behaviour after combination with a D-2 agonist." | ( Dopamine D-1 receptor agonists combined with the selective D-2 agonist quinpirole facilitate the expression of oral stereotyped behaviour in rats. Arnt, J; Hyttel, J; Perregaard, J, 1987) | 0.51 |
| " Unlike clozapine, neither the selective 5-HT2 receptor antagonist, ritanserin, nor the dopamine D2 receptor antagonists, haloperidol and remoxipride, caused locomotor activation when given alone or in combination with SKF38393." | ( Why does clozapine stimulate the motor activity of reserpine-pretreated rats when combined with a dopamine D1 receptor agonist? Bengtsson, A; Jackson, DM; Malmberg, A; Mohell, N, 1995) | 0.29 |
| " The drugs 7-OH-DPAT, quinpirole and RU24213 were studied alone and in combination with cocaine for their effects on locomotor activity in non-habituated mice." | ( Dopamine 'D2-like' receptor agonists in combination with cocaine: absence of interactive effects on locomotor activity. Reggers, J; Terry, P; Tirelli, E, 1997) | 0.61 |
| "The aim of this study was to explore effects on anxiety-like behavior of the D2 dopamine receptor agonist, quinpirole and of the D2 dopamine receptor antagonist, sulpiride given alone or in combination with a low dose of 17β-estradiol (17β-E2) to ovariectomized (OVX) rats." | ( Anxiolytic-like effect of quinpirole in combination with a low dose of 17β-estradiol in ovariectomized rats. Fedotova, J, 2013) | 0.9 |
| "This report compares the effects on medial forebrain bundle self-stimulation of injecting into either the sublenticular central extended amygdala (SLEAc) or nucleus accumbens shell (NAcS) the D1 dopamine receptor blocker SCH23390 or the D2 dopamine receptor agonist quinpirole alone or in combination with the AMPA glutamate receptor blocker NBQX." | ( Comparison of the effects on brain stimulation reward of D1 blockade or D2 stimulation combined with AMPA blockade in the extended amygdala and nucleus accumbens. Kuehn, L; Schmid, E; Stoehr, M; Waraczynski, M; Zwifelhofer, W, 2015) | 0.6 |
The goal of the present investigation was to study a full dose-response of quinpirole in production of species-specific 50 kHz ultrasonic vocalizations in rats. The maximal inhibition in response to the highest dose was significantly greater. When rats had free access to high-fat chow (discrimination training was suspended), the quin pirole discrimination dose- response curve shifted leftward.
| Excerpt | Relevance | Reference |
|---|---|---|
| "Akin to receptor inactivation with phenoxybenzamine (PBZ) (1 microM, 1 hr), treatment of anterior pituitary cells with 17 beta-estradiol (10 nM, 3 days) right-shifted the dose-response curve for inhibition of prolactin (PRL) secretion by the full agonist R-(-)-N-n-propylnorapomorphine (NPA) and reduced the maximal effect [EC50 (pM) and percent maximal effect: control, 25." | ( Comparative effects of receptor inactivation, 17 beta-estradiol and pertussis toxin on dopaminergic inhibition of prolactin secretion in vitro. Bohmaker, K; Diamond, J; Lieu, HD; Meller, E; Puza, T, 1992) | 0.28 |
| " Thus, both the locomotor activating and inhibiting effects of quinpirole are found in both the nucleus accumbens and the dorsal striatum, but the differing dose-response relationships indicate that the mechanisms are not the same in these two brain regions." | ( Effects of intracerebral quinpirole on locomotion in rats. Cottrell, GA; Meyer, ME; Potter, T; Van Hartesveldt, C, 1992) | 0.83 |
| " The dose-response relation for LY171555 was bell-shaped, with a maximal effect being obtained with 10(-9) M) LY171555." | ( Opposing effects of dopamine D2 receptor stimulation on the spontaneous and the electrically evoked release of [3H]GABA on rat prefrontal cortex slices. Besson, MJ; Penit-Soria, J; Rétaux, S, 1991) | 0.28 |
| " Compared to WKY, the dose-response curve for the inhibition of dopamine release by quinpirole was shifted to the left in SHR and the maximal inhibition in response to the highest dose was significantly greater." | ( Effect of the dopamine D2 receptor agonist quinpirole on the in vivo release of dopamine in the caudate nucleus of hypertensive rats. De Jong, W; De Lang, H; Linthorst, AC; Versteeg, DH, 1991) | 0.77 |
| " The administration of SKF 30 min before QUIN had no effect on the QUIN dose-response function in either group of rats." | ( Evaluation of the interaction between D1 and D2 receptors in a drug discrimination paradigm. Sutherland, JV; Williams, JE; Woolverton, WL, 1990) | 0.28 |
| " Dose-response curves for each drug were shifted to the left in the MPTP-treated mice, suggesting behavioral supersensitivity." | ( Dopamine receptors and sensorimotor behavior in MPTP-treated mice. Bruno, JP; Hadjiconstantinou, M; Weihmuller, FB, 1990) | 0.28 |
| "05) shifted the SKF dose-response function to the left, suggesting that stimulation of D2 receptors can potentiate a behavioral effect mediated by D1 receptors." | ( The D2 agonist quinpirole potentiates the discriminative stimulus effects of the D1 agonist SKF 38393. Williams, JE; Woolverton, WL, 1990) | 0.63 |
| " The dose-response curves for both agonists were shifted to the left in the hypothyroid rats compared to water-treated controls." | ( The hypothyroid rat as a model of increased sensitivity to dopamine receptor agonists. Cameron, DL; Crocker, AD, 1990) | 0.28 |
| " We sought to determine whether daily versus weekly dosing of haloperidol for 3 weeks produced distinct effects on DA, dihydroxyphenylacetic acid (DOPAC), and homovanillic acid (HVA) concentrations in multiple brain areas." | ( Sensitization versus tolerance to the dopamine turnover-elevating effects of haloperidol: the effect of regular/intermittent dosing. Barnes, DE; Bellows, EP; Csernansky, JG; Lombrozo, L, 1990) | 0.28 |
| " DA was less potent than VIP, and stimulated cyclase activity with a monophasic dose-response curve." | ( Interactions between vasoactive intestinal peptide and dopamine in the rabbit retina: stimulation of a common adenylate cyclase. Lam, DM; Pachter, JA, 1986) | 0.27 |
| " SCH23390 (3-30 nmol), a selective D-1 DA receptor antagonist, caused a progressive parallel shift to the right in the dose-response curve for DA-induced pancreatic secretion without changes in the maximal response." | ( Do D-1 dopamine receptors mediate dopamine-induced pancreatic exocrine secretion in anesthetized dogs? Chiba, S; Horiuchi, A; Iwatsuki, K; Yonekura, H, 1989) | 0.28 |
| " Pretreatment with sulpiride (200 mg/kg) produced a parallel, 40-fold shift to the right of the dose-response curve for NPA." | ( Hypothermia in mice: D2 dopamine receptor mediation and absence of spare receptors. Hizami, R; Kreuter, L; Meller, E, 1989) | 0.28 |
| "0 mg/kg) produced dose-dependent rightward shifts of the (+/-)BAY k 8644 dose-response curve." | ( Modification of the behavioral effects of (+/-)BAY k 8644, cocaine and d-amphetamine by L-type calcium channel blockers in squirrel monkeys. Barrett, JE; Rosenzweig-Lipson, S, 1995) | 0.29 |
| " A dose-response effect was observed related to alertness, indifference, and locomotion." | ( Behavioral effects evoked by SKF 38393 and LY 171555 in adult cats. Gomez, A; Motles, E; Tetas, M, 1995) | 0.29 |
| "025 mg/kg quinpirole from distilled water, a dose-response curve and time course of the quinpirole discriminative stimulus were determined." | ( D2-specific discriminative stimuli: parameters, blocking, and rebound. Barrett, RJ; Caul, WF; Huffman, EM; Jones, JR; Strand, EJ, 1995) | 0.69 |
| " Pretreatment also shifted to the right the dose-response function for DALA intra-accumbens." | ( Mesoaccumbens dopamine-opiate interactions in the control over behaviour by a conditioned reinforcer. Everitt, BJ; Phillips, GD; Robbins, TW, 1994) | 0.29 |
| "Methylphenidate (MPD) increased in rats the incidence of sniffing, rearing and locomotion, and this along dose-response curves that had an inverted U-shape; at 40 mg/kg, MPD exclusively induced stereotyped gnawing, which was inhibited by neuroleptics." | ( Inhibition of methylphenidate-induced behaviors in rats: differences among neuroleptics. Colpaert, FC; Koek, W, 1993) | 0.29 |
| "A within-subject dose-response analysis was conducted by locally perfusing increasing concentrations (0." | ( The development of D2 autoreceptor-mediated modulation of K(+)-evoked dopamine release in the neostriatum. Andersen, SL; Gazzara, RA, 1994) | 0.29 |
| " The dose-response curves of intravenously administered apomorphine on the spontaneous activity of NSDA neurons were shifted to the right in animals exposed to a liquid diet containing 17." | ( The effects of in utero ethanol administration on the electrophysiological activity of rat nigrostriatal dopaminergic neurons. Chiodo, LA; Shen, RY, 1993) | 0.29 |
| " SCH23390 (3-30 nmol), a selective D-1 DA receptor antagonist, caused a progressive parallel shift to the right in the dose-response curve for DA-induced pancreatic secretion without changes in the maximal response." | ( D-1 dopamine receptors mediate dopamine-induced pancreatic exocrine secretion in anesthetized dogs. Chiba, S; Horiuchi, A; Iwatsuki, K; Ren, LM, 1995) | 0.29 |
| " Increasing the number of pulses to 2 or 4 pulses at 50 Hz resulted in a shift of the quinpirole dose-response curve to the right in all regions and in the rostral pole, a significant reduction in the maximum inhibition of dopamine overflow to both stimulation parameters." | ( Influences of neuronal uptake and D2 autoreceptors on regulation of extracellular dopamine in the core, shell and rostral pole of the rat nucleus accumbens. Kruk, ZL; Wieczorek, W, 1995) | 0.51 |
| " Following systemic (intraperitoneal) administration of apomorphine (a dopamine receptor D1/D2 mixed agonist), SKF 38393 (D1 > D3 > D2 agonist), LY 17155 or quinpirole (D3 > D2 and D1) agonist), haloperidol (a DA-D2 antagonist), and clonidine (noradrenaline receptor alpha 2 agonist), the ICSS response rates evoked from LH-MFB and VTA-SN were compared with vehicle or saline-treated animals on the basis of dose-response functions." | ( Dose-response functions of apomorphine, SKF 38393, LY 171555, haloperidol and clonidine on the self-stimulation evoked from lateral hypothalamus and ventral tegmentum. Desiraju, T; Raju, TR; Singh, J, 1996) | 0.49 |
| " Following a 7-day withdrawal period, we examined the effects of these two dosing regimens on: (1) baseline dopamine efflux and uptake following single-pulse electrical stimulation, (2) inhibition of uptake by cocaine; and (3) inhibition of efflux by autoreceptor activation." | ( Effects of intermittent and continuous cocaine administration on dopamine release and uptake regulation in the striatum: in vitro voltammetric assessment. Ellinwood, EH; Jones, SR; Lee, TH; Wightman, RM, 1996) | 0.29 |
| " The dissimilarity in dose-response curve of WAY-100635 on punished and unpunished behaviour poses questions about the mediation of these effects." | ( Effects of 5-HT1A receptor ligands in a modified Geller-Seifter conflict model in the rat. Gommans, J; Hijzen, TH; Joordens, RJ; King, CM; Maes, RA; Olivier, B, 1997) | 0.3 |
| "5 mg/kg, twice weekly) or saline injections in either the home cage environment, an alternate environment or the testing environment (activity monitors), followed by a dose-response test for the expression of sensitization in the activity monitors." | ( Locomotor sensitization to quinpirole: environment-modulated increase in efficacy and context-dependent increase in potency. Allan, M; Szechtman, H; Szumlinski, KK; Talangbayan, H; Tracey, A, 1997) | 0.59 |
| " The shift to the left in the dose-response curve of quinpirole in isolated A/J mice indicated that D2-like dopamine receptor functions can be altered by social experience." | ( D2-like dopamine receptor mediation of social-emotional reactivity in a mouse model of anxiety: strain and experience effects. Gariépy, JL; Gendreau, PL; Lewis, MH; Petitto, JM, 1998) | 0.55 |
| " The dose-response curve obtained from the denervated striatum showed a shift to the right." | ( Loss of regulation by presynaptic dopamine D2 receptors of exogenous L-DOPA-derived dopamine release in the dopaminergic denervated striatum. Kannari, K; Maeda, T; Matsunaga, M; Suda, T, 1999) | 0.3 |
| " Thus, the inhibitory dose-response effects of a D2-preferring [sulpride], a D3-preferring [U 99194A] and combination of varying doses of these antagonists [sulpride + U 99194A] were evaluated on the ability of the cited agonists to produce vomiting." | ( The role of D2 and D3 dopamine receptors in the mediation of emesis in Cryptotis parva (the least shrew). Ahmad, B; Darmani, NA; Zhao, W, 1999) | 0.3 |
| " It is suggested that these cocaine dosing regimes cause differential and dynamic changes in dopamine autoreceptor sensitivity during the early withdrawal phase." | ( Altered sensitivity of dopamine autoreceptors in rat accumbens 1 and 7 days after intermittent or continuous cocaine withdrawal. Davidson, C; Ellinwood, EH; Lee, TH, 2000) | 0.31 |
| " Selective adenosine A(2A) receptor antagonists, such as KW-6002, may be one means of reducing the dosage of L-DOPA used in treating Parkinson's disease and are potentially a novel approach to treating the illness both as monotherapy and in combination with dopaminergic drugs." | ( Combined use of the adenosine A(2A) antagonist KW-6002 with L-DOPA or with selective D1 or D2 dopamine agonists increases antiparkinsonian activity but not dyskinesia in MPTP-treated monkeys. Jackson, MJ; Jenner, P; Kanda, T; Kase, H; Kuwana, Y; Nakamura, J; Pearce, RK; Smith, LA, 2000) | 0.31 |
| " Furthermore, the inhibitory effects on striatal nerve cell firing rate by the D1 receptor agonist SKF 81297 were not different in noninnervated or reinnervated areas of the striatum compared to the control side as seen from the dose-response curves." | ( Fetal ventral mesencephalic grafts functionally reduce the dopamine D2 receptor supersensitivity in partially dopamine reinnervated host striatum. Andbjer, B; Fuxe, K; Kehr, J; Strömberg, I, 2000) | 0.31 |
| "0 mg/kg; n=7-10/dose) in two dose-response tests for locomotor sensitization, conducted at 3 and 15 days following the cessation of chronic treatment." | ( Locomotor sensitization to quinpirole in rats: effects of drug abstinence and sex. Goodwill, AM; Szechtman, H; Szumlinski, KK, 2000) | 0.6 |
| " Compared to males, female rats displayed greater locomotor responding to QNP, both during chronic treatment and on the dose-response tests for sensitization." | ( Locomotor sensitization to quinpirole in rats: effects of drug abstinence and sex. Goodwill, AM; Szechtman, H; Szumlinski, KK, 2000) | 0.6 |
| " Daily dosing with A-77636 rapidly produced complete tolerance, as previously observed, whereas coadministration of the D2 agonist quinpirole plus A-77636 failed to either delay or prevent tolerance." | ( Dinapsoline: characterization of a D1 dopamine receptor agonist in a rat model of Parkinson's disease. Gulwadi, AG; Korpinen, CD; Mailman, RB; Nichols, DE; Sit, SY; Taber, MT, 2001) | 0.52 |
| " The present study was designed to determine the extent to which D2/3 receptor activation and blockade can modulate morphine-induced locomotion using a novel cumulative dosing procedure in Swiss-Webster mice." | ( The modulatory actions of dopamine D2/3 agonists and antagonists on the locomotor-activating effects of morphine and caffeine in mice. Beardsley, PM; Cook, CD, 2003) | 0.32 |
| " The objectives of this study were to determine (1) the dose-response effects for the self-administration of EtOH into the VTA of male Wistar rats, and (2) the involvement of VTA DA neurons in the reinforcing actions of EtOH within the VTA." | ( Intracranial self-administration of ethanol within the ventral tegmental area of male Wistar rats: evidence for involvement of dopamine neurons. Bell, RL; Kuc, KA; McBride, WJ; Melendez, RI; Murphy, JM; Rodd, ZA; Zhang, Y, 2004) | 0.32 |
| " Following chronic treatment, a full dose-response profile was determined to assess the presence of sensitization." | ( Presynaptic stimulation and development of locomotor sensitization to the dopamine agonist quinpirole. Gormley, S; Lomanowska, A; Szechtman, H, 2004) | 0.54 |
| "We compared two different methamphetamine dosing regimens and found distinct long-term behavioral and neurochemical changes." | ( Acute and chronic continuous methamphetamine have different long-term behavioral and neurochemical consequences. Davidson, C; Ellinwood, EH; Lee, TH, 2005) | 0.33 |
| " The action of these drugs is dosing time-dependent; in fruit flies, behavioral response to quinpirole shows a marked circadian variability." | ( Diurnal rhythms in quinpirole-induced locomotor behaviors and striatal D2/D3 receptor levels in mice. Akhisaroglu, M; Kurtuncu, M; Manev, H; Uz, T, 2005) | 0.88 |
| " Following chronic treatment, dose-response profiles to QNP were obtained to assess the expression of sensitization; the effect of U69593 on locomotor activity in animals already sensitized to QNP was also assessed." | ( Kappa-opioid agonist U69593 potentiates locomotor sensitization to the D2/D3 agonist quinpirole: pre- and postsynaptic mechanisms. Bisnaire, L; Graham, D; Hayton, S; Perreault, ML; Simms, J; Szechtman, H, 2006) | 0.56 |
| " Both the anorectic response on the first day of dosing and the tolerant response on the subsequent days were attenuated." | ( Hypothalamic neuropeptide Y (NPY) and the attenuation of hyperphagia in streptozotocin diabetic rats treated with dopamine D1/D2 agonists. Kuo, DY, 2006) | 0.33 |
| " When given in combination with cocaine, CJB 090 but not NGB 2904 attenuated the discriminative stimulus effects of cocaine, shifting the cocaine dose-response curve to the right." | ( Effects of two novel D3-selective compounds, NGB 2904 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-9H-fluorene-2-carboxamide] and CJB 090 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide], on the reinforcing and discrimin Claytor, R; Martelle, JL; Nader, MA; Newman, AH; Reboussin, BA; Ross, JT, 2007) | 0.34 |
| " drug injection, combining heroin with cocaine shifted the heroin dose-response function leftward, and isobolographic analysis indicated that the combined effects were dose-additive." | ( Modulation of heroin and cocaine self-administration by dopamine D1- and D2-like receptor agonists in rhesus monkeys. Platt, DM; Rowlett, JK; Spealman, RD; Yao, WD, 2007) | 0.34 |
| "0 mg/kg was more effective at shifting to the right the pramipexole dose-response curve in pramipexole-trained rats, while 32 mg/kg of the selective D3 antagonist PG01037 had little effect." | ( The discriminative stimulus effects of dopamine D2- and D3-preferring agonists in rats. Greedy, B; Grundt, P; Husbands, SM; Koffarnus, MN; Newman, AH; Woods, JH, 2009) | 0.35 |
| " The discriminative stimulus effects of quinpirole were attenuated by the D3 receptor-selective antagonist N-{4-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-trans-but-2-enyl}-4-pyridine-2-yl-benzamide HCl (PG01037) and the nonselective D3/D2 receptor antagonist raclopride, but not by the D2 receptor-selective antagonist 3-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]methyl-1H-indole (L-741,626); the potencies of PG01037 and raclopride to antagonize this effect of quinpirole paralleled their potencies to antagonize the ascending limb of the quinpirole yawning dose-response curve (thought to be mediated by D3 receptors)." | ( Dopamine D3 receptors mediate the discriminative stimulus effects of quinpirole in free-feeding rats. Baladi, MG; France, CP; Newman, AH, 2010) | 0.86 |
| " Seven to ten days after sensitization was complete, microdialysis of the NAcc core was performed using a cumulative dosing regimen of amphetamine (0." | ( Neonatal quinpirole treatment enhances locomotor activation and dopamine release in the nucleus accumbens core in response to amphetamine treatment in adulthood. Brown, RW; Cope, ZA; Huggins, KN; Noel, DM; Roane, DS; Sheppard, AB, 2010) | 0.78 |
| " When rats had free access to high-fat chow (discrimination training was suspended), the quinpirole discrimination dose-response curve shifted leftward, possibly indicating enhanced sensitivity at D3 receptors." | ( Eating high-fat chow increases the sensitivity of rats to quinpirole-induced discriminative stimulus effects and yawning. Baladi, MG; France, CP, 2010) | 0.83 |
| "In rats gaining weight with restricted or free access to high-fat chow, both limbs of the quinpirole yawning dose-response curve (0." | ( Influence of body weight and type of chow on the sensitivity of rats to the behavioral effects of the direct-acting dopamine-receptor agonist quinpirole. Baladi, MG; France, CP; Newman, AH, 2011) | 0.79 |
| " Male Sprague-Dawley rats (n=6/group) had free access to water or 10% sucrose and quinpirole dose-response curves (yawning and hypothermia) were generated weekly for 8 weeks." | ( Drinking sucrose enhances quinpirole-induced yawning in rats. Baladi, MG; France, CP; Newman, AH; Thomas, YM, 2011) | 0.9 |
| "The goal of the present investigation was to study a full dose-response of quinpirole in production of species-specific 50 kHz ultrasonic vocalizations in rats, and to study involvement of D2 and D3 dopamine receptors in this response." | ( Quinpirole-induced 50 kHz ultrasonic vocalization in the rat: role of D2 and D3 dopamine receptors. Brudzynski, SM; Komadoski, M; St Pierre, J, 2012) | 2.05 |
| " Following a 2-day drug-free period, dose-response curves for hyperactivity produced by MDMA (2." | ( Repeated exposure to MDMA and amphetamine: sensitization, cross-sensitization, and response to dopamine D₁- and D₂-like agonists. Bradbury, S; Gittings, D; Schenk, S, 2012) | 0.38 |
| " We then performed a dose-response study to test for chloro-APB-induced restoration of righting during continuous isoflurane anesthesia." | ( Activation of D1 dopamine receptors induces emergence from isoflurane general anesthesia. Brown, EN; Chemali, JJ; Solt, K; Taylor, NE, 2013) | 0.39 |
| " Restricting access to high fat or standard chow shifted the DOM-induced head twitch dose-response curve to the right and shifted the quinpirole-induced yawning dose-response curve downward in both groups of rats." | ( Restricted access to standard or high fat chow alters sensitivity of rats to the 5-HT(2A/2C) receptor agonist 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane. France, CP; Serafine, KM, 2014) | 0.61 |
| "Animal work on the behavioral effects of antipsychotic treatment suggests that different dosing regimens could affect drug sensitivity differently, with an intermittent treatment regimen tending to cause a sensitization effect, while a continuous treatment causing a tolerance." | ( Differential effects of intermittent versus continuous haloperidol treatment throughout adolescence on haloperidol sensitization and social behavior in adulthood. Gao, J; Li, M, 2014) | 0.4 |
| " Dose-response curves (0." | ( Drinking sucrose or saccharin enhances sensitivity of rats to quinpirole-induced yawning. Bentley, TA; France, CP; Kilborn, DJ; Koek, W; Serafine, KM, 2015) | 0.66 |
| " leftward shift of the quinpirole dose-response curve) than rats eating standard chow to yawning induced by quinpirole." | ( Dietary supplementation with fish oil prevents high fat diet-induced enhancement of sensitivity to the behavioral effects of quinpirole. Hernandez-Casner, C; Ramos, J; Serafine, KM, 2017) | 0.97 |
| " resulted in a leftward shift of the ascending limb of the dose-response curve)." | ( Dietary supplementation with fish oil reverses high fat diet-induced enhanced sensitivity to the behavioral effects of quinpirole. Hernandez-Casner, C; Hussain, S; Poisson, C; Ramos, J; Serafine, KM; Woloshchuk, CJ, 2019) | 0.72 |
| ") using a cumulative dosing procedure." | ( Intermittent dietary supplementation with fish oil prevents high fat diet-induced enhanced sensitivity to dopaminergic drugs. Beltran, NM; Cruz, B; Echeverri Alegre, JI; Galindo, KI; Hernandez-Casner, C; Ramos, J; Serafine, KM, 2021) | 0.62 |
| "Our results showed that intra-VP quinpirole microinjection regulates VTA DAergic neurons according to an inverted U-shaped dose-response curve." | ( The D2-like Dopamine Receptor Agonist Quinpirole Microinjected Into the Ventral Pallidum Dose-Dependently Inhibits the VTA and Induces Place Aversion. Grace, AA; Laszlo, K; Lenard, L; Ollmann, T; Peczely, L, 2022) | 1.27 |
| Role | Description |
|---|---|
| dopamine agonist | A drug that binds to and activates dopamine receptors. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| pyrazoloquinoline | Any organic heterotricyclic compound that consists of a pyrazole ring ortho-fused to a quinoline. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| dopamine D1 receptor | Homo sapiens (human) | Potency | 5.1735 | 0.0052 | 1.3022 | 8.1995 | AID624455 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 2.4840 | 0.1000 | 20.8793 | 79.4328 | AID588453 |
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 10.0000 | 0.0126 | 10.6917 | 88.5700 | AID887 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 6.3096 | 0.0013 | 18.0743 | 39.8107 | AID926 |
| arylsulfatase A | Homo sapiens (human) | Potency | 37.9330 | 1.0691 | 13.9551 | 37.9330 | AID720538 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 24.4485 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 10.0000 | 0.0025 | 5.8400 | 31.6228 | AID899 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 0.0238 | 0.0060 | 26.1688 | 89.1251 | AID488953 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 33.5875 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 2.2387 | 0.0010 | 6.0009 | 35.4813 | AID943 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 5.0119 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 0.0379 | 0.0601 | 10.7453 | 37.9330 | AID485368 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Beta-2 adrenergic receptor | Homo sapiens (human) | Ki | 100.0000 | 0.0000 | 0.6635 | 9.5499 | AID1298705 |
| 5-hydroxytryptamine receptor 2C | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.0002 | 0.6677 | 10.0000 | AID64170 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 1.9809 | 0.0000 | 0.6518 | 10.0000 | AID1153295; AID1153296; AID1225546; AID1225547; AID1297533; AID1297536; AID1298707; AID1298708; AID1443613; AID239106; AID239107; AID239120; AID239121; AID254495; AID254497; AID254520; AID439360; AID439361; AID61302; AID61303; AID61489; AID61490; AID63216; AID63217; AID63227; AID709659; AID756372; AID756373; AID756374 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.0001 | 0.6017 | 10.0000 | AID64170 |
| D | Rattus norvegicus (Norway rat) | IC50 (µMol) | 30.0000 | 0.0003 | 0.5026 | 7.7625 | AID63370 |
| D(3) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 0.0057 | 0.0001 | 0.2567 | 5.8000 | AID65625 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.0001 | 0.7396 | 10.0000 | AID64170 |
| D(2) dopamine receptor | Bos taurus (cattle) | Ki | 1.3798 | 0.0000 | 0.5836 | 6.1000 | AID64170; AID64172; AID64173 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 166.2976 | 0.0001 | 0.8363 | 10.0000 | AID1153294; AID1225544; AID1298706; AID254494; AID63040; AID709661 |
| D(4) dopamine receptor | Homo sapiens (human) | Ki | 0.0180 | 0.0000 | 0.4362 | 10.0000 | AID1153298; AID1225549; AID1298710; AID239128; AID239137; AID254504; AID254506; AID439363; AID63550; AID63670; AID63672; AID756369 |
| Sodium-dependent dopamine transporter | Rattus norvegicus (Norway rat) | Ki | 0.0240 | 0.0003 | 0.3708 | 8.1600 | AID65150 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 25.0000 | 0.0000 | 0.3855 | 10.0000 | AID1225551 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.0003 | 1.2967 | 9.2440 | AID64170 |
| 5-hydroxytryptamine receptor 1D | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.0010 | 1.6747 | 9.2000 | AID64170 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | Ki | 3.0000 | 0.0002 | 1.4940 | 10.0000 | AID254495 |
| 5-hydroxytryptamine receptor 1F | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.0010 | 1.6747 | 9.2000 | AID64170 |
| 5-hydroxytryptamine receptor 2B | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.0002 | 0.5909 | 10.0000 | AID64170 |
| 5-hydroxytryptamine receptor 6 | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.0002 | 0.4254 | 2.1000 | AID64170 |
| 5-hydroxytryptamine receptor 7 | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.0000 | 0.1480 | 3.1800 | AID64170 |
| 5-hydroxytryptamine receptor 5A | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.3010 | 1.3003 | 2.1000 | AID64170 |
| 5-hydroxytryptamine receptor 5B | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.3010 | 1.3003 | 2.1000 | AID64170 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 0.0844 | 0.0000 | 0.6020 | 10.0000 | AID1153297; AID1225548; AID1297534; AID1297537; AID1298709; AID1443614; AID239087; AID239098; AID239943; AID254499; AID254501; AID256758; AID346263; AID439362; AID65150; AID65153; AID65278; AID65454; AID709660; AID756371 |
| 5-hydroxytryptamine receptor 3A | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.0002 | 0.4841 | 10.0000 | AID64170 |
| 5-hydroxytryptamine receptor 2A | Sus scrofa (pig) | Ki | 0.0490 | 0.0300 | 0.4270 | 0.9000 | AID439362 |
| D(1A) dopamine receptor | Sus scrofa (pig) | Ki | 0.0700 | 0.0005 | 1.2223 | 8.8000 | AID756372 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.1000 | 0.0001 | 0.5494 | 8.4000 | AID64282 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 0.0540 | 0.0000 | 0.4375 | 10.0000 | AID65273 |
| 5-hydroxytryptamine receptor 4 | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.0016 | 1.0253 | 5.0119 | AID64170 |
| D | Bos taurus (cattle) | Ki | 20.0000 | 0.0001 | 2.3676 | 10.0000 | AID254428 |
| 5-hydroxytryptamine receptor 3B | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 0.0002 | 0.5023 | 10.0000 | AID64170 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| interferon gamma precursor | Homo sapiens (human) | AC50 | 39.0000 | 0.1280 | 15.1730 | 38.6100 | AID1259420 |
| D | Rattus norvegicus (Norway rat) | K 0.5 | 5.0000 | 0.0004 | 0.0042 | 0.0062 | AID61343 |
| D(3) dopamine receptor | Rattus norvegicus (Norway rat) | Activity | 10.0000 | 0.0140 | 5.0070 | 10.0000 | AID65463 |
| D(3) dopamine receptor | Rattus norvegicus (Norway rat) | K 0.5 | 0.0045 | 0.0004 | 0.0439 | 0.1700 | AID61683 |
| D(4) dopamine receptor | Homo sapiens (human) | Intrinsic activity | 0.1000 | 0.1000 | 0.1000 | 0.1000 | AID272399 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | Intrinsic activity | 0.0950 | 0.0700 | 0.0825 | 0.0950 | AID272397 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | K 0.5 | 1.1394 | 0.0002 | 0.4747 | 2.2500 | AID61330; AID64778 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID240295 | Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles. |
| AID266786 | Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID1769336 | Partial agonist activity at human D3 receptor expressed in HEK293T cell coexpressed GalphaoA using Coelenterazine H as substrate incubated for 10 mins by BRET assay | |||
| AID61489 | In vitro for its ability to displace [3H]- spiperone from cloned human dopamine D2 short receptor expressed in CHO cells; Low binding affinity | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID1297546 | Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry relative to dopamine | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID61683 | Affinity on C6 glioma cells transfected with Dopamine receptor D3 | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5 | Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane. |
| AID1443624 | Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay | |||
| AID239106 | Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D2L expressed in CHO cells | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID239121 | High inhibition constant against [3H]spiperone binding to human Dopamine receptor D2S expressed in CHO cells | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID265142 | Displacement of [3H]WAY-100635 from 5HT1A receptor in porcine striatal membrane | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11 | Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. |
| AID244408 | Intrinsic activity to sitmulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assay | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID439359 | Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | 1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands. |
| AID61806 | Intrinsic activity as rate of incorporation of [3H]thymidine in human D4.2 receptor established in mitogenesis assay relative to quinpirole | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. |
| AID196868 | Ability to induce contralateral rotational behavior in unilateral 6-hydroxydopamine nigrostriatal-lesioned rats and no. of turns was determined after 15 minutes of start at intraperitoneal dosage of 1.0 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID1546915 | Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to control | |||
| AID1153297 | Displacement of [3H]Spiperone from human dopamine D3 receptor expressed in CHO cells by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1297541 | Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID610685 | Agonist activity at human recombinant D2L receptor expressed in HEK cells assessed as inhibition of forskolin-induced [3H]cAMP production at 1 uM after 20 mins by spectrophotometry | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Synthesis and characterization of selective dopamine D₂ receptor ligands using aripiprazole as the lead compound. |
| AID1298706 | Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID1232231 | Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- at 3 uM incubated for 60 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay relative to basal level | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14 | Fluoro-substituted phenylazocarboxamides: Dopaminergic behavior and N-arylating properties for irreversible binding. |
| AID254494 | Binding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18 | Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. |
| AID64282 | Displacement of [3H]- -spiperone from Dopamine receptor D2 in rat striatum | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | trans-10,11-dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine: a highly potent selective dopamine D1 full agonist. |
| AID63646 | Degradation rate constant for dopamine transporter by Dopamine receptor D2 in striatum was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID196435 | Inhibition constant on radiolabeled [125 I] FIDA1 binding to rat striatal membranes | 1993 | Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2 | Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT. |
| AID254428 | Binding affinity (low) towards bovine dopamine receptor 1 by using [3H]-SCH- 23390 (0.3 nM) as radioligand | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18 | Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. |
| AID610687 | Agonist activity at human recombinant D3 receptor expressed in HEK cells assessed as inhibition of forskolin-induced [3H]cAMP production at 100 nM after 20 mins by spectrophotometry | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Synthesis and characterization of selective dopamine D₂ receptor ligands using aripiprazole as the lead compound. |
| AID65461 | Antagonist activity by measuring the inhibition of quinpirole stimulated [3H]- thymidine uptake against Dopamine receptor D3; NA means Not Active | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907). |
| AID272392 | Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist. |
| AID226202 | Intrinsic activity which is established by measuring the stimulation of mitogenesis | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213). |
| AID63370 | Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | trans-10,11-dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine: a highly potent selective dopamine D1 full agonist. |
| AID272397 | Intrinsic activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production relative to dopamine | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist. |
| AID244410 | Intrinsic activity to stimulate human Dopamine receptor D3 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID388682 | Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies. |
| AID239943 | Inhibition constant against [3H]-spiperone binding to human Dopamine receptor D3 expressed in CHO cells | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID63859 | Effective concentration of compound required against human Dopamine D4.2 receptor | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID1225545 | Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID64919 | In vitro affinity at mutant D2 receptor (S197A) in C6 (glioma) cell membranes. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors. |
| AID1297540 | Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay relative to dopamine | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID1782430 | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID63647 | Degradation rate constant for dopamine transporter by Dopamine receptor D2 in nucleus accumbens was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID64170 | Tested for binding affinity against Dopamine receptor D2 like from bovine striatum membranes by using [3H]YM-09151-2 radioligand | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and receptor binding studies. |
| AID63670 | In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID1598357 | Agonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay | |||
| AID64172 | Inhibition of [3H]YM-09151-2 binding to bovine retina membrane Dopamine receptor D2, high affinity site | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and receptor binding studies. |
| AID1225546 | Displacement of [3H]spiperone from human dopamine D2L receptor transfected in CHO cells after 1 hr by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID756373 | Displacement of [3H]7-OH-DPAT from human dopamine D2L receptor expressed in CHO cells | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. |
| AID1782434 | Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 min | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1153305 | Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1633737 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay relative to dopamine | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists. |
| AID64173 | Inhibition of [3H]YM-09151-2 binding to bovine retina membrane Dopamine receptor D2, low affinity site | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and receptor binding studies. |
| AID240225 | Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles. |
| AID1633735 | Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay relative to dopamine | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists. |
| AID1595593 | Partial agonist activity at human D2L receptor expressed in HEK293T cells co-expressing N-terminal venus-tagged beta-arrestin2 assessed as beta-arrestin2 recruitment after 15 mins in presence of coelenterazine H by BRET assay relative to control | |||
| AID709659 | Displacement of [3H]YM-09151-2 from human dopamine D2 receptor expressed in CHOp cells | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID254506 | High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18 | Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. |
| AID243233 | Agonist activity in [3H]thymidine uptake assay in CHO dhfr- mutant cells expressing human D3 receptor | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles. |
| AID63648 | Half life of recovery for dopamine transporter by Dopamine receptor D2 in nucleus accumbens was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID1895221 | Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay | |||
| AID61490 | In vitro for its ability to displace [3H]- spiperone from cloned human dopamine D2 short receptor expressed in CHO cells; high binding affinity | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID439363 | Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | 1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands. |
| AID272395 | Intrinsic activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production relative to dopamine | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist. |
| AID193330 | Ability to lower the serum prolactin levels in comparison with that of pergolide expressed as percent inhibition change at ip dose of 5.0 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID1633732 | Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists. |
| AID1595595 | Partial agonist activity at human D2L receptor expressed in HEK293T cells co-expressing Galpahi1/Gbeta1/GFP2-Ggamma2 assessed as Galphai1 dissociation after 15 mins in presence of coelenterazine 400a by luciferase reporter gene assay relative to control | |||
| AID64638 | Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from rat | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907). |
| AID1526899 | Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay | |||
| AID1769333 | Antagonist activity at human D2L receptor expressed in HEK293T cell coexpressed GalphaoA using Coelenterazine H as substrate incubated for 10 mins by BRET assay | |||
| AID1526902 | Ratio of EC50 for agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay to EC50 for agonist activity | |||
| AID629489 | Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22 | Development of a bivalent dopamine D₂ receptor agonist. |
| AID346263 | Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II. |
| AID63854 | Effective dose was measured by the stimulation of mitogenesis at Dopamine receptor D4.2 | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments. |
| AID188335 | Ability to lower the serum prolactin levels in comparison with that of pergolide was determined for the control rats at ip dose of 0.05 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID64804 | Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists. |
| AID1297539 | Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID1756665 | Agonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H |
| AID1225553 | Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID1606882 | Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9 | Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands. |
| AID1464186 | Agonist activity at human D2SR expressed in HEK293 cell membranes co-expressing PTX insensitive variant of Galphao1 incubated for 30 mins by [35S]GTP-gammaS binding assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation. |
| AID1297537 | Displacement of [3H]7-OH-DPAT from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID266795 | Intrinsic activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID239481 | Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like in porcine striatal membranes; NT= not tested | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | Preparation and pharmacological characterization of trans-2-amino-5(6)-fluoro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes as D2-like dopamine receptor agonists. |
| AID1168799 | Agonist activity at D2 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles. |
| AID254504 | Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18 | Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. |
| AID1413596 | Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay | 2018 | MedChemComm, Sep-01, Volume: 9, Issue:9 | Design, synthesis, and evaluation of bitopic arylpiperazine-phthalimides as selective dopamine D |
| AID1332845 | Agonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1153301 | Displacement of [3Hprazosin from adrenergic alpha1 receptor in pig cerebral cortex homogenates by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1225544 | Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID1782432 | Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID265133 | Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11 | Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. |
| AID1633734 | Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists. |
| AID61303 | In vitro for its ability to displace [3H]- spiperone from cloned human dopamine D2 long receptor expressed in CHO cells; high binding affinity | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID388685 | Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release relative to quinpirole | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies. |
| AID1245100 | Activity at pro-link-tagged D2S-ARMS2PK2 (unknown origin) expressed in HEK293 cells by beta-arrestin-2 recruitment assay | 2015 | Bioorganic & medicinal chemistry, Sep-15, Volume: 23, Issue:18 | 1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation. |
| AID239098 | High inhibition constant against [3H]spiperone binding to human Dopamine receptor D3 expressed in CHO cells | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID1442570 | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure. |
| AID1782431 | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay relative to control | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID594018 | Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Aromatic ring functionalization of benzolactam derivatives: new potent dopamine D3 receptor ligands. |
| AID1298715 | Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID193327 | Ability to lower the serum prolactin levels in comparison with that of pergolide expressed as percent inhibition change at ip dose of 0.05 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID1782423 | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 min | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID188337 | Ability to lower the serum prolactin levels in comparison with that of pergolide was determined for the control rats at ip dose of 0.5 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID272399 | Intrinsic activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production relative to dopamine | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist. |
| AID265137 | Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11 | Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. |
| AID196867 | Ability to induce contralateral rotational behavior in unilateral 6-hydroxydopamine nigrostriatal-lesioned rats and no. of turns was determined after 15 minutes of start at intraperitoneal dosage of 0.1 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID709654 | Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay relative to quinpirole | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID1782433 | Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay relative to control | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1153298 | Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID301650 | Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes. |
| AID1298710 | Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID1232227 | Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14 | Fluoro-substituted phenylazocarboxamides: Dopaminergic behavior and N-arylating properties for irreversible binding. |
| AID1595592 | Partial agonist activity at human D2L receptor expressed in HEK293T cells co-expressing N-terminal venus-tagged beta-arrestin2 assessed as beta-arrestin2 recruitment after 15 mins in presence of coelenterazine H by BRET assay | |||
| AID265135 | Intrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assay | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11 | Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. |
| AID756369 | Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. |
| AID254501 | High binding affinity towards human dopamine receptor 3 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18 | Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. |
| AID756372 | Displacement of [3H]spiperone from human dopamine D2S receptor expressed in CHO cells | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. |
| AID1895220 | Agonist activity at human D2 long receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD2longR-ElucC assessed as maximum efficacy at 10 uM by beta-arrestin2 recruitment assay relative to control | |||
| AID1332839 | Agonist activity at D3 receptor (unknown origin) expressed in cell membranes at 10 uM after 40 mins by [35S]GTPgammaS binding assay relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID319915 | Agonist activity at rat dopamine D4.2 receptor expressed in CHO10001A cells assessed as incorporation of [3H]thymidine | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET. |
| AID1443613 | Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D2 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis | |||
| AID1298705 | Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID63040 | Affinity towards Dopamine receptor D1 | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | CoMFA-based prediction of agonist affinities at recombinant D1 vs D2 dopamine receptors. |
| AID1464187 | Agonist activity at human D2SR expressed in HEK293 cell membranes co-expressing PTX insensitive variant of Galphao1 incubated for 30 mins by [35S]GTP-gammaS binding assay relative to quinpirole | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation. |
| AID63227 | Affinity towards Dopamine receptor D2 | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | CoMFA-based prediction of agonist affinities at recombinant D1 vs D2 dopamine receptors. |
| AID64959 | Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D3 in CHO cells; 24/420 | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID1298716 | Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol relative to isoprenaline | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID1595588 | Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assay | |||
| AID1298718 | Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol relative to quinpirole | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID240284 | Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID1298717 | Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID1153303 | Displacement of [3H]-ketanserin from pig 5HT2 receptor by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID492188 | Intrinsic efficacy at human dopamine D2 long receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase activity at 10 nM after 20 mins by spectrophotometric analysis | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626. |
| AID65273 | Compound was evaluated for its ability to displace [3H]raclopride from dopamine receptor D2 in rat striatal homogenates | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Dopaminergic and serotonergic activities of imidazoquinolinones and related compounds. |
| AID1442574 | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure. |
| AID756371 | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. |
| AID265131 | Intrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assay | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11 | Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. |
| AID1782436 | Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID629490 | Agonist activity at FLAG-tagged DRD2 Long receptor expressed in human HEK293 cells assessed as induction of receptor internalization at 10 uM after 30 mins by confocal microscopy | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22 | Development of a bivalent dopamine D₂ receptor agonist. |
| AID1633736 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists. |
| AID1895218 | Agonist activity at human D2 long receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD2longR-ElucC by beta-arrestin2 recruitment assay | |||
| AID196130 | Ability to induce contralateral rotational behavior in unilateral 6-hydroxydopamine nigrostriatal-lesioned rats and percent of rats turning was determined at intraperitoneal dosage of 0.1 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID679976 | TP_TRANSPORTER: Luciferase assay in H35 hepatoma cells | 1997 | The Journal of biological chemistry, Apr-25, Volume: 272, Issue:17 | Bromocriptine transcriptionally activates the multidrug resistance gene (pgp2/mdr1b) by a novel pathway. |
| AID1769334 | Partial agonist activity at human D2L receptor expressed in HEK293T cell coexpressed GalphaoA using Coelenterazine H as substrate incubated for 10 mins by BRET assay | |||
| AID256759 | Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assay | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25 | First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure. |
| AID1225559 | Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID65467 | Basal binding towards Dopamine receptor D3 was evaluated using [35S]- GTP-gamma S radioligand | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors. |
| AID1232229 | Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14 | Fluoro-substituted phenylazocarboxamides: Dopaminergic behavior and N-arylating properties for irreversible binding. |
| AID1298707 | Displacement of [3H]spiperone from human D2L receptor expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID1225549 | Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID709657 | Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay relative to quinpirole | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID1633726 | Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists. |
| AID1297538 | Selectivity index, ratio Ki for human D3 receptor to Ki for human D2 receptor using [3H]7-OH-DPAT displacement assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID756370 | Displacement of [3H]WAY100635 from 5-HT1A receptor in porcine cerebral cortex | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. |
| AID61857 | Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina; not determined | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand. |
| AID1442584 | Agonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure. |
| AID1153307 | Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID196131 | Ability to induce contralateral rotational behavior in unilateral 6-hydroxydopamine nigrostriatal-lesioned rats and percent of rats turning was determined at intraperitoneal dosage of 1.0 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID1297534 | Displacement of [3H]N-methylspiperone from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID1756667 | Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H |
| AID256758 | Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 in CHO cell membrane | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25 | First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure. |
| AID1464189 | Bias factor, ratio of agonist activity at human D2SR expressed in HEK293 cell membranes co-expressing PTX insensitive variant by [35S]GTP-gammaS binding assay to human D2SR expressed in HEK293 cells by by beta-Arrestin 2 recruitment assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation. |
| AID1232233 | Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- at 3 uM incubated for 60 mins followed by 10 uM haloperidol addition and further incubated for additional 180 mins by scintillation counting based myo- | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14 | Fluoro-substituted phenylazocarboxamides: Dopaminergic behavior and N-arylating properties for irreversible binding. |
| AID718718 | Partial agonist activity at human dopamine D4.2 receptor expressed in CHO10001 cells assessed as stimulation of mitogenesis measuring [3H]thymidine incorporation after 20 hrs by scintillation counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Novel azulene derivatives for the treatment of erectile dysfunction. |
| AID240277 | Effective concentration to stimulate rat Dopamine receptor D2S mediated [3H]thymidine incorporation into growing cells using mitogenesis assay | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID65596 | Intrinsic activity (IA) by the mitogenesis assay against Dopamine receptor D3 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907). |
| AID1606890 | Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay relative to 5-HT | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9 | Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands. |
| AID1606885 | Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9 | Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands. |
| AID1400251 | Agonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Synthesis toward Bivalent Ligands for the Dopamine D |
| AID388683 | Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay relative to quinpirole | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies. |
| AID1243920 | Agonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293 cells assessed as induction of ERK1/2 phosphorylation at 10 uM after 5 mins by Western blotting | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Bifunctional compounds targeting both D2 and non-α7 nACh receptors: design, synthesis and pharmacological characterization. |
| AID1298708 | Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID1823685 | Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay | |||
| AID1298709 | Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID65625 | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand. |
| AID193329 | Ability to lower the serum prolactin levels in comparison with that of pergolide expressed as percent inhibition change at ip dose of 0.5 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID64779 | Affinity towards Dopamine receptor D2 was evaluated in rat striatal membrane using [3H]spiperone as radioligand | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | Conformational analysis of D1 dopamine receptor agonists: pharmacophore assessment and receptor mapping. |
| AID255229 | Ligand efficacy towards dopamine D3 receptor | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18 | Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. |
| AID1298721 | Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID188338 | Ability to lower the serum prolactin levels in comparison with that of pergolide was determined for the control rats at ip dose of 5.0 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID5447 | Ability to displace [3H]ketanserin radioligand from porcine 5-hydroxytryptamine 2A receptor; ND denotes not determined | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID1443614 | Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D3 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis | |||
| AID1782421 | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins b | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1225551 | Displacement of [3H]ketanserin from human 5-HT2A receptor transfected in HEK293 cells by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID699936 | Agonist activity at human D2S receptor expressed in HEK293T cells coexpressing GalphaoA-91-Rluc8 and mVenus-Gbeta1gamma2 after 2 mins by bioluminescence resonance energy transfer assay relative to dopamine | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Molecular determinants of selectivity and efficacy at the dopamine D3 receptor. |
| AID61803 | Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. |
| AID61345 | Affinity towards Dopamine receptor D1 was evaluated in rat striatal membrane using [3H]SCH-23,390 as radioligand | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | Conformational analysis of D1 dopamine receptor agonists: pharmacophore assessment and receptor mapping. |
| AID1464185 | Agonist activity at human D2SR expressed in HEK293 cells incubated for 5 hrs by beta-Arrestin 2 recruitment assay relative to quinpirole | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation. |
| AID266244 | Agonist activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation relative to quinpirole by mitogenesis assay | 2006 | Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12 | Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists. |
| AID3968 | Ability to displace [3H]8-OH-DPAT radioligand from porcine 5-hydroxytryptamine 1A receptor; ND denotes not determined | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID1769335 | Antagonist activity at human D3 receptor expressed in HEK293T cell coexpressed GalphaoA using Coelenterazine H as substrate incubated for 10 mins by BRET assay | |||
| AID1232232 | Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- at 3 uM incubated for 240 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay relative to basal level | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14 | Fluoro-substituted phenylazocarboxamides: Dopaminergic behavior and N-arylating properties for irreversible binding. |
| AID1225555 | Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID1443628 | Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay | |||
| AID63855 | Agonist effect was measured by the stimulation of mitogenesis at Dopamine receptor D4.2 | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments. |
| AID1595585 | Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence ass | |||
| AID61854 | Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand; ND = Not determined | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and receptor binding studies. |
| AID272398 | Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist. |
| AID709661 | Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID62902 | Ability to displace [3H]SCH-23390 radioligand from cloned human Dopamine receptor D2 in CHO cells; 64/3100 | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID254520 | High binding affinity towards human dopamine receptor 2 (short) expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18 | Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. |
| AID709655 | Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID63217 | In vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D2 short in CHO cells | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. |
| AID254497 | Binding affinity (low) towards human dopamine receptor 2 (long) against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18 | Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. |
| AID266245 | Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay | 2006 | Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12 | Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists. |
| AID226638 | Hill coefficient value. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand. |
| AID1442576 | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure. |
| AID301652 | Intrinsic activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as rate of incorporation of [3H]thymidine relative to quinpirole | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes. |
| AID265143 | Displacement of [3H]WAY100635 from 5HT2 receptor in porcine striatal membrane | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11 | Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. |
| AID1823686 | Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay relative to control | |||
| AID65153 | In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D3 expressed in CHO cells; high binding affinity | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID64636 | Antagonist activity by measuring the inhibition of quinpirole stimulated [3H]- thymidine uptake against Dopamine receptor D2L; NA means Not Active | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907). |
| AID1245098 | Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay | 2015 | Bioorganic & medicinal chemistry, Sep-15, Volume: 23, Issue:18 | 1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation. |
| AID64925 | In vitro affinity at wild type Dopamine receptor D2 on C6 (glioma) cell membranes. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors. |
| AID592072 | Induction of FLAG-tagged human D2long receptor internalization expressed in HEK293 cells assessed as translocation of receptor from plasma membrane to cytosol at 10 uM after 30 mins by immunocytochemistry | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Highly potent 5-aminotetrahydropyrazolopyridines: enantioselective dopamine D3 receptor binding, functional selectivity, and analysis of receptor-ligand interactions. |
| AID756367 | Displacement of [3H]prazosin from alpha-1 adrenergic receptor in porcine cerebral cortex | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. |
| AID65150 | In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D3 in CHO cells | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. |
| AID1297542 | Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay relative to dopamine | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID756375 | Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. |
| AID64790 | In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors. |
| AID1153294 | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1298704 | Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cells | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID1442571 | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure. |
| AID65278 | In vitro for its ability to displace [3H]- spiperoneI from cloned human Dopamine receptor D3 expressed in CHO cells; Low binding affinity | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID240271 | Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2 | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles. |
| AID62756 | In vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptor | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Studies of the active conformation of a novel series of benzamide dopamine D2 agonists. |
| AID1730258 | Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Discovery of a true bivalent dopamine D |
| AID1297543 | Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID1298720 | Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay relative to isoprenaline | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID436913 | Agonist activity at dopamine D2 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | 'Click' D(1) receptor agonists with a 5-HT(1A) receptor pharmacophore producing D(2) receptor activity. |
| AID1782422 | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 min | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID64302 | Binding affinity for dopamine D2-D3 like receptor labelled with [3H]YM-09151-2 in striatum | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand. |
| AID63672 | In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinity | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID196436 | Inhibition constant on radiolabeled [125 I] FIDA2 binding to rat striatal membranes | 1993 | Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2 | Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT. |
| AID239344 | Inhibitory constant for [3H]YM-09151-2 binding to Dopamine receptor D2-like in porcine striatal membranes | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | Preparation and pharmacological characterization of trans-2-amino-5(6)-fluoro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes as D2-like dopamine receptor agonists. |
| AID65454 | Tested for the ability to displace [125I]iodosulpiride from human cloned Dopamine receptor D3, expressed in CHO cells | 1999 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18 | Heterocyclic analogues of 2-aminotetralins with high affinity and selectivity for the dopamine D3 receptor. |
| AID243236 | Maximum [35S]GTP-gamma-S, binding in CHO K1 cells expressing human D4.4 receptor; relative to quinpirole | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles. |
| AID272394 | Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist. |
| AID64644 | Intrinsic activity (IA) by the mitogenesis assay against Dopamine receptor D2L | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907). |
| AID266796 | Intrinsic activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID1297536 | Displacement of [3H]7-OH-DPAT from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID1225557 | Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID1606889 | Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9 | Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands. |
| AID64017 | In vitro functional assay measuring the [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor was performed | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. |
| AID63216 | In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D2 long in CHO cells | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. |
| AID239128 | Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID239120 | High inhibition constant against [3H]spiperone binding to human Dopamine receptor D2L expressed in CHO cells | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID756368 | Displacement of [3H]ketanserin from 5-HT2 receptor in porcine cerebral cortex | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. |
| AID61330 | Affinity on C6 glioma cells transfected with Dopamine receptor D2L | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5 | Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane. |
| AID188345 | Ability to lower the serum prolactin levels in comparison with that of pergolide was determined for the drug-treated rats at ip dose of 5.0 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID1442582 | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of renilla luciferase 2-tagged beta-arrestin-2 recruitment after 15 mins by BRET assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure. |
| AID1782420 | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins b | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1225547 | Displacement of [3H]spiperone from human dopamine D2S receptor transfected in CHO cells after 1 hr by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID1443615 | Selectivity ratio of Ki for human dopamine D3 receptor expressed in HEK293 cell membranes to Ki for human dopamine D2 receptor expressed in HEK293 cell membranes | |||
| AID1297544 | Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry relative to dopamine | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID272393 | Displacement of [3H]spiperone from dopamine D2-like receptor in porcine striata homogenate | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist. |
| AID1225561 | Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID1298719 | Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID388684 | Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies. |
| AID64806 | Rate of [3H]thymidine uptake compared to quinpirole (100%) in Dopamine receptor D3 expressing CHO cells | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists. |
| AID254499 | Low binding affinity towards human dopamine receptor 3 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18 | Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. |
| AID1153315 | Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1153295 | Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1225550 | Displacement of [3H]WAY100635 from poricne cerebral cortex 5-HT1A receptor by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID61807 | Agonist effect for Dopamine D4.2 receptor determined as rate of incorporation of [3H]- thymidine relative to quinpirole | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID439361 | Displacement of [3H]spiperone from human cloned dopamine D2short receptor expressed in CHO cells | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | 1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands. |
| AID586712 | Intrinsic activity at human D3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-dependent accumulation of [3H]-cyclic AMP at 100 nM by spectrophotometric analysis | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Synthesis and pharmacological evaluation of fluorine-containing D₃ dopamine receptor ligands. |
| AID265129 | Intrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11 | Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. |
| AID439360 | Displacement of [3H]spiperone from human cloned dopamine D2long receptor expressed in CHO cells | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | 1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands. |
| AID301651 | Agonist activity at human dopamine D4.2 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 2 hrs | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes. |
| AID1633727 | Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay relative to dopamine | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists. |
| AID239137 | High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID1782437 | Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay relative to contro | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID239087 | Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D3 expressed in CHO cells | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID1526897 | Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay | |||
| AID254617 | Effective concentration against dopamine D3 receptor | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18 | Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. |
| AID1153299 | Displacement of [3H]WAY-100635 from 5-HT1A receptor in pig cerebral cortex homogenates by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID239107 | Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D2S expressed in CHO cells | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID1448008 | Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 | Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for β-Arrestin-Biased D |
| AID1895222 | Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC assessed as maximum efficacy by beta-arrestin2 recruitment assay relative to control | |||
| AID61343 | Inhibition of [3H]SCH-23390 binding to rat striatal membrane Dopamine receptor D1 | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5 | Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane. |
| AID1225552 | Displacement of [3H]prazosin from poricne cerebral cortex alpha1 adrenergic receptor by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID63192 | In vitro ability to displace dopamine receptor D1 of bovine striatal membrane preparations using [3H]-SCH- 23390; nd =not determined | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. |
| AID65466 | Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from rat | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907). |
| AID1606886 | Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay relative to control | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9 | Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands. |
| AID64818 | Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay (intrinsic activity) | 2000 | Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19 | Thiazoloindans and thiazolobenzopyrans: a novel class of orally active central dopamine (partial) agonists. |
| AID65947 | Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells; 1.6/49 | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID1400252 | Agonist activity at human dopamine D2 receptor /mGluR5a (unknown origin) expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Synthesis toward Bivalent Ligands for the Dopamine D |
| AID63649 | Half life of recovery for dopamine transporter by Dopamine receptor D2 in striatum was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID65463 | Maximal stimulation reached was evaluated by using [35S]- GTP-gamma S radioligand | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors. |
| AID1297545 | Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID61800 | Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID1298711 | Selectivity index, ratio of Ki for human beta2 receptor to Ki for human D2S receptor | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID1448003 | Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 | Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for β-Arrestin-Biased D |
| AID63550 | In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. |
| AID1598359 | Agonist activity at recombinant human D2 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay | |||
| AID63048 | Ability to displace [3H]SCH-23390 radioligand from bovine Dopamine receptor D1; not determined | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID64917 | In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors. |
| AID266788 | Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID188344 | Ability to lower the serum prolactin levels in comparison with that of pergolide was determined for the drug-treated rats at ip dose of 0.5 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID63196 | In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells; Not determined | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID188342 | Ability to lower the serum prolactin levels in comparison with that of pergolide was determined for the drug-treated rats at ip dose of 0.05 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists. |
| AID709658 | Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID64778 | Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D2 | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5 | Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane. |
| AID63853 | Binding affinity for dopamine D4-like receptor labelled with [3H]YM-09151-2 in retina | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand. |
| AID240291 | Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID61302 | In vitro for its ability to displace [3H]- spiperone from cloned human dopamine D2 long receptor expressed in CHO cells; Low binding affinity | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID64321 | Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity) | 2000 | Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19 | Thiazoloindans and thiazolobenzopyrans: a novel class of orally active central dopamine (partial) agonists. |
| AID63856 | Intrinsic activity at human Dopamine D4.2 receptor as stimulation of mitogenesis | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID1298722 | Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay relative to quinpirole | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists. |
| AID1442580 | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of renilla luciferase 2-tagged beta-arrestin-1 recruitment after 15 mins by BRET assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure. |
| AID254495 | Binding affinity (low) towards human dopamine receptor 2 short against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18 | Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. |
| AID226201 | Rate of incorporation of [3H]thymidine as evidence of mitogenetic activity | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213). |
| AID232373 | Ratio of D2-D3 like receptor to D4 like receptor | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand. |
| AID240276 | Effective concentration to stimulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assay | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID238979 | Inhibition constant against [3H]SCH-23390 binding to Dopamine receptor D1 in bovine striatal membranes | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID62904 | Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D2 in CHO cells; 52/4000 | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID1204361 | Agonist activity at dopamine D2 receptor (unknown origin) transfected in CHO cells assessed as increase in ERK1/2 phosphorylation at 1 uM after 5 mins by Western blot analysis | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | A solid-phase combinatorial approach for indoloquinolizidine-peptides with high affinity at D(1) and D(2) dopamine receptors. |
| AID1606888 | Antagonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 15 mins followed by 5-HT addition and measured at 1 sec interval for 60 secs by Fluo | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9 | Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands. |
| AID243237 | Agonist activity in [3H]-thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2 receptor; relative to quinpirole | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles. |
| AID301653 | Intrinsic activity at human dopamine D4.2 receptor expressed in CHO10001 mutant cells assessed as rate of incorporation of [3H]thymidine relative to quinpirole | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes. |
| AID718719 | Partial agonist activity at human dopamine D4.2 receptor expressed in CHO10001 cells assessed as stimulation of mitogenesis measuring [3H]thymidine incorporation at 0.01 to 10000 nM after 20 hrs by scintillation counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Novel azulene derivatives for the treatment of erectile dysfunction. |
| AID63645 | Degradation rate constant for dopamine transporter by Dopamine receptor D2 in nucleus accumbens was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID1443620 | Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay | |||
| AID1297533 | Displacement of [3H]N-methylspiperone from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID265141 | Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11 | Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. |
| AID1443616 | Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay | |||
| AID265139 | Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11 | Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. |
| AID1464184 | Agonist activity at human D2SR expressed in HEK293 cells incubated for 5 hrs by beta-Arrestin 2 recruitment assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation. |
| AID244409 | Intrinsic activity to stimulate rat Dopamine receptor D2S mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID64016 | Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. |
| AID1225548 | Displacement of [3H]spiperone from human dopamine D3 receptor transfected in CHO cells after 1 hr by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Molecular determinants of biased agonism at the dopamine D₂ receptor. |
| AID439362 | Displacement of [3H]spiperone from human cloned dopamine D3 receptor expressed in CHO cells | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | 1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands. |
| AID586714 | Intrinsic activity at human D2 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-dependent accumulation of [3H]-cyclic AMP at 1 uM by spectrophotometric analysis | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Synthesis and pharmacological evaluation of fluorine-containing D₃ dopamine receptor ligands. |
| AID1442578 | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure. |
| AID1448005 | Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 | Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for β-Arrestin-Biased D |
| AID1297535 | Selectivity index, ratio Ki for human D3 receptor to Ki for human D2 receptor using [3H]N-methylspiperone displacement assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. |
| AID1595594 | Partial agonist activity at human D2L receptor expressed in HEK293T cells co-expressing Galpahi1/Gbeta1/GFP2-Ggamma2 assessed as Galphai1 dissociation after 15 mins in presence of coelenterazine 400a by luciferase reporter gene assay | |||
| AID1782435 | Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 min | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID756374 | Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cells | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. |
| AID709660 | Displacement of [3H]YM-09151-2 from human dopamine D3 receptor expressed in CHOp cells | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID1606883 | Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay relative to d | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9 | Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands. |
| AID1153296 | Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID25013 | Tested in vitro for intrinsic activity relative to quinpirole | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Studies of the active conformation of a novel series of benzamide dopamine D2 agonists. |
| AID244411 | Intrinsic activity to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID272396 | Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist. |
| AID1633733 | Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay relative to dopamine | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists. |
| AID699935 | Agonist activity at human D3 receptor expressed in HEK293T cells coexpressing GalphaoA-91-Rluc8 and mVenus-Gbeta1gamma2 after 2 mins by bioluminescence resonance energy transfer assay relative to dopamine | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Molecular determinants of selectivity and efficacy at the dopamine D3 receptor. |
| AID629488 | Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay relative to quinpirole | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22 | Development of a bivalent dopamine D₂ receptor agonist. |
| AID1245096 | Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay | 2015 | Bioorganic & medicinal chemistry, Sep-15, Volume: 23, Issue:18 | 1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID1345783 | Rat D2 receptor (Dopamine receptors) | 1990 | Nature, Sep-13, Volume: 347, Issue:6289 | Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 1992 | European journal of pharmacology, Apr-10, Volume: 225, Issue:4 | Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor. |
| AID1346893 | Human 5-HT2C receptor (5-Hydroxytryptamine receptors) | 2002 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2 | Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. |
| AID1345814 | Human D4 receptor (Dopamine receptors) | 1996 | Molecular pharmacology, Dec, Volume: 50, Issue:6 | Identification and pharmacological characterization of [125I]L-750,667, a novel radioligand for the dopamine D4 receptor. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1999 | Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 359, Issue:6 | Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 1995 | Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Jul, Volume: 12, Issue:4 | Lack of discrimination by agonists for D2 and D3 dopamine receptors. |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 1991 | Nature, Apr-18, Volume: 350, Issue:6319 | Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 1995 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 275, Issue:2 | Functional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: 1. Activation of postsynaptic D3 receptors mediates hypothermia, whereas blockade of D2 receptors elicits prolactin |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 1995 | Neuroreport, Jan-26, Volume: 6, Issue:2 | A functional test identifies dopamine agonists selective for D3 versus D2 receptors. |
| AID1345898 | Rat D3 receptor (Dopamine receptors) | 1995 | Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Jul, Volume: 12, Issue:4 | Lack of discrimination by agonists for D2 and D3 dopamine receptors. |
| AID1259419 | Human 5-HT2A receptor (5-Hydroxytryptamine receptors) | 2002 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2 | Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. |
| AID1345898 | Rat D3 receptor (Dopamine receptors) | 1990 | Nature, Sep-13, Volume: 347, Issue:6289 | Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 1990 | Nature, Sep-13, Volume: 347, Issue:6289 | Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. |
| AID1259419 | Human 5-HT2A receptor (5-Hydroxytryptamine receptors) | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 1995 | European journal of pharmacology, Jun-23, Volume: 290, Issue:1 | Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors. |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1999 | Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 359, Issue:6 | Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors. |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 1995 | European journal of pharmacology, Jun-23, Volume: 290, Issue:1 | Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors. |
| AID1345814 | Human D4 receptor (Dopamine receptors) | 2002 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2 | Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. |
| AID1345814 | Human D4 receptor (Dopamine receptors) | 1991 | Nature, Apr-18, Volume: 350, Issue:6319 | Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 1991 | Nature, Apr-18, Volume: 350, Issue:6319 | Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 1992 | European journal of pharmacology, Apr-10, Volume: 225, Issue:4 | Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor. |
| AID1346893 | Human 5-HT2C receptor (5-Hydroxytryptamine receptors) | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 1990 | Nature, Sep-13, Volume: 347, Issue:6289 | Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. |
| AID1346867 | Human 5-HT2B receptor (5-Hydroxytryptamine receptors) | 2002 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2 | Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 1996 | Molecular pharmacology, Dec, Volume: 50, Issue:6 | Identification and pharmacological characterization of [125I]L-750,667, a novel radioligand for the dopamine D4 receptor. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 1996 | Molecular pharmacology, Dec, Volume: 50, Issue:6 | Identification and pharmacological characterization of [125I]L-750,667, a novel radioligand for the dopamine D4 receptor. |
| AID1346867 | Human 5-HT2B receptor (5-Hydroxytryptamine receptors) | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 1995 | Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Jul, Volume: 12, Issue:4 | Lack of discrimination by agonists for D2 and D3 dopamine receptors. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 302 (14.01) | 18.7374 |
| 1990's | 906 (42.02) | 18.2507 |
| 2000's | 537 (24.91) | 29.6817 |
| 2010's | 339 (15.72) | 24.3611 |
| 2020's | 72 (3.34) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.
| This Compound (35.28) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 23 (1.04%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 2,190 (98.96%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||