guanfacine profile

Guanfacine is an alpha-2 adrenergic receptor agonist used to treat attention deficit hyperactivity disorder (ADHD) and high blood pressure. It is synthesized through a series of chemical reactions starting with a substituted phenylethylamine derivative. Guanfacine works by stimulating alpha-2 receptors in the brain, which leads to decreased norepinephrine release. This action helps to improve focus and attention in individuals with ADHD, and also helps to reduce blood pressure. Guanfacine is an important medication for managing ADHD and high blood pressure, and it is studied extensively to understand its mechanisms of action, efficacy, and potential side effects. It is a valuable tool for treating these conditions and improving the lives of affected individuals.'

Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	3519
CHEMBL ID	862
CHEBI ID	5558
SCHEMBL ID	35094
MeSH ID	M0024935

Synonym
BRD-K32830106-003-03-0
gtpl522
estulic
LOPAC0_000519
cas-29110-48-3
NCGC00015469-01
NCGC00015469-02
lopac-g-1043
NCGC00024950-01
tocris-1030
PRESTWICK2_000339
BSPBIO_000377
BPBIO1_000415
guanfacine
C07037
29110-47-2
DB01018
PRESTWICK3_000339
NCGC00024950-03
guanfacine [inn:ban]
benzeneacetamide, n-(aminoiminomethyl)-2,6-dichloro-
guanfacinum [inn-latin]
einecs 249-442-8
guanfacina [inn-spanish]
PRESTWICK0_000339
SPBIO_002298
PRESTWICK1_000339
NCGC00024950-02
L013430
NCGC00015469-06
CHEMBL862
nsc-759121
chebi:5558 ,
L000286
D08031
guanfacine (inn)
estulic (tn)
FT-0669068
FT-0669067
n-(diaminomethylidene)-2-(2,6-dichlorophenyl)acetamide
NCGC00015469-05
bdbm81984
nsc_3519
cas_29110-47-2
(2,6-dichlorophenylacetyl)-guanidine
CCG-204609
NCGC00015469-03
NCGC00015469-07
NCGC00015469-04
guanfacina
guanfacinum
unii-30omy4g3mk
30omy4g3mk ,
nsc 759121
n-amidino-2-(2,6-dichlorophenyl)acetamide
guanfacine [who-dd]
guanfacine [mi]
guanfacine [vandf]
guanfacine [inn]
HY-17416A
SCHEMBL35094
DTXSID9046944 ,
n-(diaminomethyliden)-2-(2,6-dichlorophenyl)acetamid
guanfacine hydrochloride (salt/mix)
estulic (salt/mix)
tenex (salt/mix)
[(2,6-dichlorophenyl)acetyl]guanidine
lon 798 (salt/mix)
AB01563079_01
n-carbamimidoyl-2-(2,6-dichlorophenyl)acetamide
AKOS030526130
AKOS030255657
J-017394
MRF-0000019
raspberryketoneglucoside
Q5613599
BCP09647
BRD-K32830106-003-11-3
SDCCGSBI-0050502.P002
A918619
[(2,6-dichlorophenyl)acetyl]guanidine hydrochloride;guanfacine hcl
A902647
EN300-243924
guanfacina (inn-spanish)
guanfacinum (inn-latin)
c02ac02
dtxcid7026944

Excerpt	Reference	Relevance
"Guanfacine is a α2A adrenergic receptor agonist approved for treating attention deficit hyperactivity disorder (ADHD). "	( Noradrenergic Add-on Therapy with Extended-Release Guanfacine in Alzheimer's Disease (NorAD): study protocol for a randomised clinical trial and COVID-19 amendments. Fox, C; Golemme, M; Hoang, K; Howard, R; Malhotra, PA; Perry, RJ; Pickett, J; Ritchie, C; Watt, H; Wilson, D, 2022)	2.42
"Guanfacine is a central alpha-2 agonist often prescribed for Attention-deficit hyperactive disorder as well as tic disorder, with a usual dose of 1-4 mg per day. "	( Guanfacine toxic ingestion with subsequent cardiogenic pulmonary edema. Baker, Z; Bridwell, RE; Cibrario, A; Larson, NP; Oliver, JJ; Rosenthal, JB; Wray, J, 2021)	3.51
"Guanfacine is a selective α"	( Systemic administration of guanfacine improves food-motivated impulsive choice behavior primarily via direct stimulation of postsynaptic α Hasegawa, M; Horiguchi, N; Jino, K; Kano, T; Kobayashi, M; Nishitomi, K; Shinohara, S; Yano, K, 2018)	1.5
"1. Guanfacine is a selective α2A-adrenoreceptor agonist primarily excreted as its unchanged form through urine in human. "	( Investigation of the role of organic cation transporter 2 (OCT2) in the renal transport of guanfacine, a selective α2A-adrenoreceptor agonist. Chen, J; Chen, X; Li, J; Li, X; Lu, Y; Sun, X; Wang, C; Zhang, Q; Zhang, Y; Zhao, D, 2015)	1.26
"Guanfacine (Intuniv) is a centrally active alpha-2A adrenergic agonist for the new indication of attention-deficit/hyperactivity disorder. "	( Use of ECG restitution (beat-to-beat QT-TQ interval analysis) to assess arrhythmogenic risk of QTc prolongation with guanfacine. Fossa, AA; Martin, P; Purkayastha, J; Robinson, A; Zhou, M, 2014)	2.05
"Guanfacine is an α2A-adrenoreceptor agonist currently indicated for the treatment of attention deficit hyperactivity disorder (ADHD). "	( Guanfacine for the treatment of attention deficit hyperactivity disorder in children and adolescents. Martino, D; Rizzo, R, 2015)	3.3
"Guanfacine is a selective α2A-adrenergic receptor agonist that has been shown to improve prefrontal cortical cognitive function, including working memory."	( Guanfacine Extended Release: A New Pharmacological Treatment Option in Europe. Chen, W; Huss, M; Ludolph, AG, 2016)	2.6
"Guanfacine is an important medication option in very young children; however, there is a significant pharmacologic "information gap," and further research is needed to help establish appropriate, safe, and effective dosing of guanfacine in this population."	( Clinical and Pharmacologic Considerations for Guanfacine Use in Very Young Children. Black, BT; Jones, BL; Kearns, GL; Soden, SE, 2016)	2.14
"Guanfacine, which is an alpha-2 agonist with a higher affinity for the 2A, compared with 2B or 2C, subtypes, also blocked the ability of PCP to increase dopamine efflux in the prefrontal cortex."	( Clonidine and guanfacine attenuate phencyclidine-induced dopamine overflow in rat prefrontal cortex: mediating influence of the alpha-2A adrenoceptor subtype. Elsworth, JD; Jentsch, JD; Roth, RH; Sanchez, D, 2008)	1.43
"Guanfacine is a noradrenergic agonist that is believed to improve symptoms of attention-deficit/hyperactivity disorder (ADHD) through selective actions at alpha2A-adrenoceptors in the prefrontal cortex. "	( Long-term, open-label extension study of guanfacine extended release in children and adolescents with ADHD. Biederman, J; Donahue, J; Lyne, A; McBurnett, K; Melmed, RD; Patel, A, 2008)	2.05
"Guanfacine is an alpha(2)-adrenoreceptor agonist used for the treatment of attention-deficit hyperactivity disorder and tic disorders. "	( Guanfacine overdose resulting in initial hypertension and subsequent delayed, persistent orthostatic hypotension. Clark, RF; Minns, AB; Schneir, A, 2010)	3.25
"Guanfacine may prove to be a useful tool in the treatment of disorders of attention associated with neurological conditions."	( Attention deficits following ADEM ameliorated by guanfacine. Farmer, SF; Husain, M; Malhotra, P; Singh-Curry, V, 2011)	1.34
"Guanfacine is an alpha2-adrenergic receptor agonist that has been shown to have beneficial effects on working memory and attentional functions in monkeys and in patients with attention deficit hyperactivity disorder."	( Lack of effects of guanfacine on executive and memory functions in healthy male volunteers. Clark, L; Lam, ML; Menon, DK; Moore, RM; Müller, U; Murphy, CL; Richmond, NK; Robbins, TW; Sahakian, BJ; Sandhu, RS; Wilkins, IA, 2005)	2.1
"Guanfacine is an alpha(2)-adrenoreceptor agonist used to treat children and adults with attention-deficit/hyperactivity disorder. "	( A phase I, randomized, open-label, crossover study of the single-dose pharmacokinetic properties of guanfacine extended-release 1-, 2-, and 4-mg tablets in healthy adults. Fiske, K; Lyne, A; Pennick, M; Shojaei, A; Swearingen, D, 2007)	2
"Guanfacine hydrochloride is an alpha(2a)-adrenoreceptor agonist found to be effective in the treatment of attention-deficit/hyperactivity disorder (ADHD). "	( Phase I, double-blind, randomized, placebo-controlled, dose-escalation study of the effects on blood pressure of abrupt cessation versus taper down of guanfacine extended-release tablets in adults aged 19 to 24 years. Fiske, K; Kisicki, JC; Lyne, A, 2007)	1.98
"5. Guanfacine is an effective antihypertensive drug with a spectrum of actions similar to clonidine."	( Guanfacine: effects of long-term treatment and withdrawal. Hamilton, CA; Reid, JL; Zamboulis, C, 1980)	2.22
"Guanfacine is an alpha 2-adrenergic agonist that may have beneficial effects on attention, without the hypotensive or sedative effects of clonidine, which is often used as an alternative to stimulants."	( Guanfacine treatment of comorbid attention-deficit hyperactivity disorder and Tourette's syndrome: preliminary clinical experience. Arnsten, A; Chappell, PB; Cohen, DJ; Leckman, JF; Lynch, KA; Riddle, MA; Scahill, L; Schultz, R, 1995)	2.46
"Guanfacine 1 is a well known centrally acting alpha 2-adrenoceptor agonist with antihypertensive activity. "	( Microsomal catalyzed N-hydroxylation of guanfacine and reduction of N-hydroxyguanfacine. Clement, B; Demesmaeker, M, 1997)	2.01
"Guanfacine hydrochloride is an alpha-2 adrenergic agonist, which has gained recent attention in the field of child and adolescent psychiatry. "	( Guanfacine and secondary mania in children. Barnhill, LJ; Horrigan, JP, 1999)	3.19
"Guanfacine appears to be a safe and effective treatment for children with tic disorders and ADHD."	( A placebo-controlled study of guanfacine in the treatment of children with tic disorders and attention deficit hyperactivity disorder. Arnsten, AF; Chappell, PB; Cohen, DJ; Katsovich, L; Kim, YS; Leckman, JF; Scahill, L; Schultz, RT; Shepherd, E, 2001)	2.04
"Guanfacine is an alpha 2-adrenoceptor agonist with antithermogenic properties. "	( Effects of the alpha 2-adrenoceptor agonist guanfacine on growth and thermogenesis in mice. Lindsay, DB; Matthews, ML; Sillence, MN; Tudor, GD, 1992)	1.99
"Guanfacine is a promising agent in the long-term treatment of stable hypertension, particularly in patients, whom diuretics or beta-blockers are contraindicated."	( [Hypotensive and hemodynamic effects of guanfacine in arterial hypertension]. Beliakova, EV; Charyev, KhZ; Erina, EV; Panfilov, VV, 1989)	1.27
"Guanfacine is a centrally acting alpha-2 adrenergic agonist. "	( The bioavailability and pharmacokinetics of guanfacine after oral and intravenous administration to healthy volunteers. Carchman, SH; Crowe, JT; Wright, GJ, 1987)	1.98

Excerpt	Reference	Relevance
"Guanfacine has a robust antidepressant-like effect and can reverse a depression-like state induced by increased acetylcholine (ACh) signaling. "	( Antidepressant-like effects of guanfacine and sex-specific differences in effects on c-fos immunoreactivity and paired-pulse ratio in male and female mice. Bentham, MP; McKee, SA; Mineur, YS; Picciotto, MR; Plantenga, ME; Zhou, WL, 2015)	2.15
"Guanfacine has a robust antidepressant-like effect and can reverse a depression-like state induced by increased acetylcholine (ACh) signaling. "	( Antidepressant-like effects of guanfacine and sex-specific differences in effects on c-fos immunoreactivity and paired-pulse ratio in male and female mice. Bentham, MP; McKee, SA; Mineur, YS; Picciotto, MR; Plantenga, ME; Zhou, WL, 2015)	2.15
"Guanfacine has been approved by the Food and Drug Administration (FDA) to treat hypertension and conduct disorder, but as it reduces body weight, it is worth examining its effectiveness and safety in models of obesity."	( A Comparison of the Anorectic Effect and Safety of the Alpha2-Adrenoceptor Ligands Guanfacine and Yohimbine in Rats with Diet-Induced Obesity. Bednarski, M; Dudek, M; Głuch-Lutwin, M; Kazek, G; Knutelska, J; Mordyl, B; Nowiński, L; Pytka, K; Sapa, J; Zygmunt, M, 2015)	1.36
"Guanfacine has been shown to reduce hyperactive behaviors in children with attention-deficit/hyperactivity disorder (ADHD) and possibly in children with pervasive developmental disorder (PDD) and hyperactivity. "	( Possible influence of variant of the P-glycoprotein gene (MDR1/ABCB1) on clinical response to guanfacine in children with pervasive developmental disorders and hyperactivity. Aman, MG; Arnold, LE; McCracken, JT; McDougle, CJ; Posey, D; Ritz, L; Scahill, L; Shiraga, S; Tierney, E; Vitiello, B; Whelan, F, 2010)	2.02
"Guanfacine has demonstrated efficacy in reversing working memory deficits in non-human primate."	( Guanfacine treatment of cognitive impairment in schizophrenia. Adler, DN; Davis, KL; Friedman, JI; Harvey, PD; Kemether, E; Parrella, M; Temporini, HD; White, L, 2001)	2.47
"Guanfacine has the advantage over other centrally acting antihypertensives of being less sedative and causing no rebound hypertension after discontinuation of treatment."	( Pharmacology of guanfacine. Fetkovská, N; Scholtysik, G, 1987)	1.34
"Guanfacine has the advantage over other centrally acting antihypertensives of being less sedative and causing no rebound hypertension after discontinuation of treatment."	( Animal pharmacology of guanfacine. Scholtysik, G, 1986)	1.3

Excerpt	Reference	Relevance
"Guanfacine treated women improved their performance on the Stroop task following exposure to all 3 imagery conditions compared with placebo women (p=0.02). "	( Sex differences in guanfacine effects on stress-induced stroop performance in cocaine dependence. Fox, HC; Hermes, G; Jayaram-Lindstrom, N; Milivojevic, V; Sinha, R, 2017)	2.23
"Four guanfacine-treated subjects (13.3%) and four placebo subjects (12.5%) exited the study before week 8."	( Extended-Release Guanfacine for Hyperactivity in Children With Autism Spectrum Disorder. Cowen, J; Deng, Y; Dziura, J; King, BH; Loo, S; McCracken, JT; McDougle, CJ; Minjarez, M; Mullett, J; Page, C; Politte, L; Rockhill, C; Sanders, R; Scahill, L; Shah, B; Ward, D, 2015)	1.21
"Guanfacine treatment significantly increased the expression of BDNF in layer II of the medial PFC during normoxia and HH."	( Guanfacine promotes neuronal survival in medial prefrontal cortex under hypobaric hypoxia. Kauser, H; Panjwani, U; Sahu, S, 2016)	2.6
"Guanfacine treated SHR showed less change in water drinking behavior and ambulation than the clonidine treated SHR."	( Effects of clonidine and guanfacine on drinking and ambulation in spontaneously hypertensive rats. Bando, Y; Koike, Y; Minami, M; Saito, H; Shimamura, K; Togashi, H, 1982)	1.29
"Guanfacine treatment is accompanied by relatively few and slight side-effects."	( [Blood pressure and renin under treatment of hypertension with guanfacine (author's transl)]. Jäger, H; Rosenthal, J, 1980)	1.22
"5. Guanfacine treatment was accompanied by relatively few and mild side-effects."	( Effect of guanfacine on blood pressure and renin activity in hypertensive patients. Rosenthal, J, 1980)	1.18
"Guanfacine treatment significantly improved cognitive performance of the working memory task, and significantly increased rCBF values in the dorsolateral PFC, the brain region most tightly associated with performance of spatial working memory tasks."	( The alpha-2A-adrenoceptor agonist, guanfacine, increases regional cerebral blood flow in dorsolateral prefrontal cortex of monkeys performing a spatial working memory task. Arnsten, AF; Avery, RA; Franowicz, JS; Studholme, C; van Dyck, CH, 2000)	1.31
"Treatment with guanfacine XR at optimized doses was associated with mostly mild or moderate TEAEs."	( Effects of guanfacine extended release on oppositional symptoms in children aged 6-12 years with attention-deficit hyperactivity disorder and oppositional symptoms: a randomized, double-blind, placebo-controlled trial. Connor, DF; Findling, RL; Kollins, SH; López, FA; Lyne, A; Sallee, F; Tremblay, G, 2010)	1.09

Excerpt	Reference	Relevance
" Terminations because of adverse effects were relatively low."	( Comparison of guanfacine versus clonidine for efficacy, safety and occurrence of withdrawal syndrome in step-2 treatment of mild to moderate essential hypertension. Bedsole, G; Fillingim, J; Hall, D; Haring, O; Jagger, P; Lewin, A; McMahon, FG; Roginsky, M; Stepansky, W; Wilson, MF, 1986)	0.63
" Guanfacine, alone and in combination, proved safe and effective."	( Long-term evaluations of therapeutic efficacy and safety of guanfacine. Jerie, P, 1986)	1.42
" A discussion on the pharmacological basis of the side effects of the centrally acting antihypertensives has been limited to those adverse reactions that are somehow related to alpha-adrenergic receptors."	( The hypotensive activity and side effects of methyldopa, clonidine, and guanfacine. Thoolen, MJ; Timmermans, PB; van Zwieten, PA, )	0.36
"Guanfacine exposures reported to the American Association of Poison Control Centers Toxic Exposure Surveillance System from 1993 to 1999 in children and adolescents <19 years of age were analyzed."	( Epidemiology and toxicity of pediatric guanfacine exposures. Klein-Schwartz, W; McGrath, JC, 2002)	2.03
" This review focuses on the tolerability, occurrence of adverse events, precautions required to prevent severe adverse events, and essential pharmacological interaction in the treatment of ADHD symptoms by non-stimulants."	( The safety of non-stimulant agents for the treatment of attention-deficit hyperactivity disorder. Banaschewski, T; Heise, CA; Himpel, S; Rothenberger, A, 2005)	0.33
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."	( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004)	0.32
" This report documents the time course and predictors of symptom efficacy and sedation-related adverse events (AEs) that emerge during GXR treatment throughout 3 randomized, placebo-controlled, double-blind trials of the drug."	( Effects of extended-release guanfacine on ADHD symptoms and sedation-related adverse events in children with ADHD. Faraone, SV; Glatt, SJ, 2010)	0.65
"The majority of adverse events (AEs) were mild to moderate, and few patients discontinued the study because of an AE."	( Long-term safety and efficacy of guanfacine extended release in children and adolescents with attention-deficit/hyperactivity disorder. Lyne, A; McGough, JJ; Sallee, FR; Wigal, T, 2009)	0.63
"Overall, these data support that GXR monotherapy is generally safe and effective for treating ADHD."	( Long-term safety and efficacy of guanfacine extended release in children and adolescents with attention-deficit/hyperactivity disorder. Lyne, A; McGough, JJ; Sallee, FR; Wigal, T, 2009)	0.63
"Safety assessments included adverse events (AEs), vital signs, physical examination, clinical laboratory tests, the Pediatric Daytime Sleepiness Scale, and the Pittsburgh Side Effects Rating Scale."	( Safety and effectiveness of coadministration of guanfacine extended release and psychostimulants in children and adolescents with attention-deficit/hyperactivity disorder. Ginsberg, LD; Greenbaum, M; Murphy, WR; Spencer, TJ, 2009)	0.61
"Coadministration of GXR and MPH or AMP was generally safe and associated with statistically significant and clinically meaningful ADHD symptom improvement in children and adolescents."	( Safety and effectiveness of coadministration of guanfacine extended release and psychostimulants in children and adolescents with attention-deficit/hyperactivity disorder. Ginsberg, LD; Greenbaum, M; Murphy, WR; Spencer, TJ, 2009)	0.61
" While medications for ADHD are generally well-tolerated, there are common, although less severe, as well as rare but severe adverse events AEs during treatment with ADHD drugs."	( Practitioner review: current best practice in the management of adverse events during treatment with ADHD medications in children and adolescents. Banaschewski, T; Buitelaar, J; Coghill, D; Cortese, S; Danckaerts, M; Dittmann, RW; Graham, J; Holtmann, M; Sergeant, J; Taylor, E, 2013)	0.39
" Safety assessments included treatment-emergent adverse events (TEAEs), electrocardiograms and vital signs."	( Efficacy and safety of extended-release guanfacine hydrochloride in children and adolescents with attention-deficit/hyperactivity disorder: a randomized, controlled, phase III trial. Bloomfield, R; Hervas, A; Huss, M; Johnson, M; Lyne, A; McNicholas, F; Robertson, B; Sikirica, V; Sreckovic, S; van Stralen, J, 2014)	0.67
" Partial α2-adrenoceptor agonists might offer the potential for effective and safe treatment of obesity."	( A Comparison of the Anorectic Effect and Safety of the Alpha2-Adrenoceptor Ligands Guanfacine and Yohimbine in Rats with Diet-Induced Obesity. Bednarski, M; Dudek, M; Głuch-Lutwin, M; Kazek, G; Knutelska, J; Mordyl, B; Nowiński, L; Pytka, K; Sapa, J; Zygmunt, M, 2015)	0.64
" A Bayesian network meta-analysis was conducted to compare change in symptoms using the ADHD Rating Scale Version IV (ADHD-RS-IV), Clinical Global Impression-Improvement (CGI-I) response, all-cause discontinuation, and adverse event-related discontinuation."	( Comparative efficacy and safety of attention-deficit/hyperactivity disorder pharmacotherapies, including guanfacine extended release: a mixed treatment comparison. Ayyagari, R; Cai, S; Huss, M; Joseph, A; Sikirica, V; Xie, J; Xie, M, 2017)	0.67
" Clonidine, melatonin, L-theanine, eszopiclone and guanfacine were well tolerated with mild to moderate adverse events; zolpidem was associated with neuropsychiatric adverse effects."	( Safety, Tolerability and Efficacy of Drugs for Treating Behavioural Insomnia in Children with Attention-Deficit/Hyperactivity Disorder: A Systematic Review with Methodological Quality Assessment. Anand, S; Besag, FMC; Chan, EW; Cortese, S; Tong, H; Wong, ICK, 2017)	0.71
" Guanfacine XR was generally well tolerated by both ethnic groups, with most adverse events being mild in both groups."	( Pharmacokinetics, Safety, and Tolerability of Single and Multiple Doses of Guanfacine Extended-Release Formulation in Healthy Japanese and Caucasian Male Adults. Ermer, J; Matsuo, Y; Okita, M; Wajima, T, 2017)	1.6
"7%) experienced a treatment-emergent adverse event (TEAE)."	( Long-term safety and efficacy of guanfacine extended release in children and adolescents with ADHD. Dirks, B; Gu, J; Huss, M; Newcorn, JH; Ramos-Quiroga, JA; Robertson, B, 2018)	0.76
" Other measures were ADHD-RS-IV subscales, Clinical Global Impression-Improvement scale (CGI-I) and Patient Global Impression-Improvement scale (PGI-I) (percentage of patients very much improved/much improved), treatment-emergent adverse event (TEAE) incidences, and TEAEs leading to discontinuation."	( Efficacy and Safety of Guanfacine Extended-Release in the Treatment of Attention-Deficit/Hyperactivity Disorder in Adults: Results of a Randomized, Double-Blind, Placebo-Controlled Study. Fujiwara, M; Ichikawa, H; Iwanami, A; Okutsu, D; Saito, K, 2020)	0.87
" Primary outcome measures were the frequency and nature of treatment-emergent adverse events (TEAEs); secondary outcome measures included the change from week 0 in ADHD Rating Scale IV with Adult Prompts (ADHD-RS-IV; Japanese version) total and subscale scores, Conners' Adult ADHD Rating Scales (CAARS), Clinical Global Impression-Improvement (CGI-I) and Patient Global Impression-Improvement (PGI-I) scales, and quality of life (QoL) and executive functioning measures."	( Safety and efficacy of guanfacine extended-release in adults with attention-deficit/hyperactivity disorder: an open-label, long-term, phase 3 extension study. Fujiwara, M; Ichikawa, H; Iwanami, A; Okutsu, D; Saito, K, 2020)	0.87
" There were no major differences in the incidence/types of treatment-emergent adverse events (TEAEs) across the subgroups."	( Efficacy and safety of guanfacine extended-release in Japanese adults with attention-deficit/hyperactivity disorder: Exploratory post hoc subgroup analyses of a randomized, double-blind, placebo-controlled study. Fujiwara, M; Iwanami, A; Kiguchi, R; Naya, N; Okutsu, D; Sakai, C; Tsuji, T, 2021)	0.93
" Trials of amphetamines, atomoxetine, bupropion, clonidine, guanfacine, methylphenidate, and modafinil with a placebo arm and reporting data on headache as an adverse event, were included."	( Headache in ADHD as comorbidity and a side effect of medications: a systematic review and meta-analysis. Banaschewski, T; Bölte, S; Buitelaar, JK; Coghill, D; Cortese, S; Häge, A; Hohmann, S; Jonsson, U; Nobel Norrman, H; Pan, PY; Şahpazoğlu Çakmak, SS, 2022)	0.96

Excerpt	Reference	Relevance
" Its kinetics were best described by a 2-compartment model, with an elimination half-life of the beta phase of 17 hours."	( Pharmacokinetics of guanfacine in patients with impaired renal function and in some elderly patients. Kiechel, JR, 1986)	0.59
"Estulic [corrected] given orally without food after overnight fast produces a blood concentration curve with a pronounced second peak that does not appear when the drug is taken with food."	( Pharmacokinetics of estulic [corrected] in humans. Cherruault, Y; Sarin, VB, 1986)	0.27
" The principal pharmacokinetic parameters of guanfacine were greatly altered, with extended biotransformation and a decrease in the half-life compared to the values observed in other cases of severe renal insufficiency."	( Pharmacokinetic aspects of guanfacine withdrawal syndrome in a hypertensive patient with chronic renal failure. Comoy, E; Fillastre, JP; Godin, M; Guerret, M; Kiechel, JR; Lavene, D, 1983)	0.82
"59 h-1, corresponding to an elimination half-life of about 12 h, which is similar to the values of patients with normal renal function."	( Pharmacokinetics of guanfacine in patients undergoing haemodialysis. Axthelm, T; Kirch, W; Kohler, H, )	0.45
"The objective of this study was to assess the single-dose pharmacokinetic properties and dose proportionality of guanfacine extended-release (GXR) tablets after oral administration in healthy adults."	( A phase I, randomized, open-label, crossover study of the single-dose pharmacokinetic properties of guanfacine extended-release 1-, 2-, and 4-mg tablets in healthy adults. Fiske, K; Lyne, A; Pennick, M; Shojaei, A; Swearingen, D, 2007)	0.77
" The pharmacokinetic parameters of CmaX, AUC(0-t), and AUC(0-infinity) were determined after each dose of GXR in all subjects."	( A phase I, randomized, open-label, crossover study of the single-dose pharmacokinetic properties of guanfacine extended-release 1-, 2-, and 4-mg tablets in healthy adults. Fiske, K; Lyne, A; Pennick, M; Shojaei, A; Swearingen, D, 2007)	0.56
"In these 49 healthy adult subjects, the single-dose pharmacokinetic properties of GXR 1-, 2-, and 4-mg tablets appeared to be statistically linear; that is, increases in mean C(max), AUC(0-t), and AUC(0-infinity) of guanfacine were proportional to dose, with the exception of the increase in mean C(max) between GXR 1 and 2 mg."	( A phase I, randomized, open-label, crossover study of the single-dose pharmacokinetic properties of guanfacine extended-release 1-, 2-, and 4-mg tablets in healthy adults. Fiske, K; Lyne, A; Pennick, M; Shojaei, A; Swearingen, D, 2007)	0.74
" After a single 2-mg dose, half-life was 14."	( Pharmacokinetics of a guanfacine extended-release formulation in children and adolescents with attention-deficit-hyperactivity disorder. Boellner, SW; Fiske, K; Lyne, A; Pennick, M; Shojaei, A, 2007)	0.65
" Plasma concentrations and concentration-related pharmacokinetic parameters were higher in children than in adolescents."	( Pharmacokinetics of a guanfacine extended-release formulation in children and adolescents with attention-deficit-hyperactivity disorder. Boellner, SW; Fiske, K; Lyne, A; Pennick, M; Shojaei, A, 2007)	0.65
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."	( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Lombardo, F; Obach, RS; Waters, NJ, 2008)	0.35
" However, data on the pharmacokinetic profiles and safety of combination treatments in ADHD are needed."	( Pharmacokinetics of coadministration of guanfacine extended release and methylphenidate extended release. Corcoran, M; Ermer, J; Haffey, M; Martin, P; Purkayastha, J; Roesch, B; Stevenson, A; Wang, P, 2013)	0.66
"The primary objective of this study was to evaluate the pharmacokinetic profiles of guanfacine extended release (GXR) and methylphenidate hydrochloride (MPH) extended release, alone and in combination."	( Pharmacokinetics of coadministration of guanfacine extended release and methylphenidate extended release. Corcoran, M; Ermer, J; Haffey, M; Martin, P; Purkayastha, J; Roesch, B; Stevenson, A; Wang, P, 2013)	0.88
" Overall, combining GXR and MPH did not alter the pharmacokinetic parameters of either medication."	( Pharmacokinetics of coadministration of guanfacine extended release and methylphenidate extended release. Corcoran, M; Ermer, J; Haffey, M; Martin, P; Purkayastha, J; Roesch, B; Stevenson, A; Wang, P, 2013)	0.66
"In this short-term, open-label study of healthy adults, coadministration of GXR and MPH did not result in significant pharmacokinetic drug-drug interactions."	( Pharmacokinetics of coadministration of guanfacine extended release and methylphenidate extended release. Corcoran, M; Ermer, J; Haffey, M; Martin, P; Purkayastha, J; Roesch, B; Stevenson, A; Wang, P, 2013)	0.66
" However, the potential for pharmacokinetic drug-drug interactions (DDIs) between GXR and lisdexamfetamine dimesylate (LDX, Vyvanse®; Shire US LLC, Wayne, PA, USA) has not been thoroughly evaluated."	( Pharmacokinetics of coadministered guanfacine extended release and lisdexamfetamine dimesylate. Corcoran, ME; Ermer, J; Fetterolf, J; Haffey, M; Martin, P; Preston, P; Purkayastha, J; Roesch, B; Wang, P, 2013)	0.67
" Following administration of LDX alone or in combination with GXR, the statistical comparisons of the AUC0-∞ and Cmax of d-amphetamine fell entirely within the reference interval."	( Pharmacokinetics of coadministered guanfacine extended release and lisdexamfetamine dimesylate. Corcoran, ME; Ermer, J; Fetterolf, J; Haffey, M; Martin, P; Preston, P; Purkayastha, J; Roesch, B; Wang, P, 2013)	0.67
"In healthy adults, coadministration of GXR and LDX did not result in a clinically meaningful pharmacokinetic DDI compared with either treatment alone."	( Pharmacokinetics of coadministered guanfacine extended release and lisdexamfetamine dimesylate. Corcoran, ME; Ermer, J; Fetterolf, J; Haffey, M; Martin, P; Preston, P; Purkayastha, J; Roesch, B; Wang, P, 2013)	0.67
" The established method was successfully applied to an in vivo pharmacokinetic study in beagle dogs after a single oral dose of 4 mg guanfacine extended-release tablets."	( Development and validation of a simple, sensitive and accurate LC-MS/MS method for the determination of guanfacine, a selective α2A -adrenergicreceptor agonist, in plasma and its application to a pharmacokinetic study. Chen, X; Dai, Y; Li, N; Li, X; Sun, X; Wang, C; Wang, S; Xu, J; Yang, W; Zhang, W, 2013)	0.81
"Using a previously developed population pharmacokinetic model, an exposure-response (ER) model was successfully developed to describe guanfacine plasma concentrations and changes in heart rate (HR) and the QT interval."	( Population pharmacokinetic/pharmacodynamic modeling of guanfacine effects on QTc and heart rate in pediatric patients. Ermer, J; Gastonguay, MR; Knebel, W; Martin, P; Purkayastha, J, 2014)	0.85
"Typical population pharmacokinetic parameters (95 % confidence interval), given the reference covariates (Caucasian, male, age 12 years, weight 50 kg), were 33."	( Population Pharmacokinetic Modeling of Guanfacine in Pediatric Patients. Corcoran, M; Ermer, J; Gastonguay, MR; Knebel, W, 2015)	0.69
" Single- and multiple-dose pharmacokinetic parameters were estimated based on plasma concentration-time data and urine concentration data of guanfacine by non-compartmental analysis."	( Pharmacokinetics, Safety, and Tolerability of Single and Multiple Doses of Guanfacine Extended-Release Formulation in Healthy Japanese and Caucasian Male Adults. Ermer, J; Matsuo, Y; Okita, M; Wajima, T, 2017)	0.89
" The results of clinical pharmacokinetic (PK) studies indicate that guanfacine is sensitive to drug-drug interactions (DDIs) perpetrated by strong inhibitors and inducers of CYP3A4."	( Development of Guanfacine Extended-Release Dosing Strategies in Children and Adolescents with ADHD Using a Physiologically Based Pharmacokinetic Model to Predict Drug-Drug Interactions with Moderate CYP3A4 Inhibitors or Inducers. Li, A; Rong, H; Welty, D; Yeo, K, 2018)	1.07
"We demonstrated similar pharmacokinetic profiles between 3 mg/d of IR guanfacine and 4 mg/d of ER guanfacine, as hypothesized."	( Pharmacokinetics and Pharmacodynamics of Immediate-Release Versus Extended-Release Guanfacine in Adult Daily Smokers. McKee, SA; Moore, KE; Oberleitner, LM; Peltier, MR; Roberts, W; Verplaetse, TL, )	0.59
" The aims of this study were to develop a population pharmacokinetic model of guanfacine after administration of GXR and to evaluate factors influencing the pharmacokinetics of guanfacine in pediatric ADHD patients."	( Population pharmacokinetic and exposure-response analyses of guanfacine in Japanese pediatric ADHD patients. Matsumoto, S; Matsuo, Y; Tsuda, Y; Wajima, T, 2019)	0.98
" However, its pharmacokinetic properties and tolerability make viloxazine ER a useful addition to the collection of FDA approved ADHD treatments."	( Evaluating the pharmacokinetics of extended release viloxazine in the treatment of children with attention-deficit/hyperactivity disorder. Burton, S; Childress, A, 2022)	0.72

Excerpt	Reference	Relevance
" The mechanism of this proposed interaction may involve drug-drug competition at the level of hepatic glucuronidation (conjugation), although shifts in protein binding cannot be ruled out."	( Increased plasma valproate concentrations when coadministered with guanfacine. Ambrosini, PJ; Sheikh, RM, 1998)	0.54
" The results of clinical pharmacokinetic (PK) studies indicate that guanfacine is sensitive to drug-drug interactions (DDIs) perpetrated by strong inhibitors and inducers of CYP3A4."	( Development of Guanfacine Extended-Release Dosing Strategies in Children and Adolescents with ADHD Using a Physiologically Based Pharmacokinetic Model to Predict Drug-Drug Interactions with Moderate CYP3A4 Inhibitors or Inducers. Li, A; Rong, H; Welty, D; Yeo, K, 2018)	1.07

Excerpt	Reference	Relevance
" The absolute bioavailability of guanfacine after a single oral dose was 81."	( The bioavailability and pharmacokinetics of guanfacine after oral and intravenous administration to healthy volunteers. Carchman, SH; Crowe, JT; Wright, GJ, 1987)	0.82
" In normal subjects, guanfacine was found to be rapidly and completely absorbed, with an absolute bioavailability close to 100% and therefore no evidence of a noticeable first-pass effect."	( Pharmacokinetics of guanfacine in patients with impaired renal function and in some elderly patients. Kiechel, JR, 1986)	0.91
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."	( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010)	0.36
" Addition of clonidine to the formulations decreased the systemic absorption rate of the anesthetics from the patch application site without impacting the coating performance or the rapid onset of anesthesia."	( Adjuvants to prolong the local anesthetic effects of coated microneedle products. Brown, K; Dohmeier, D; Hansen, K; Siebenaler, K; Zhang, Y, 2012)	0.38

Excerpt	Relevance	Reference
" The principal disadvantages of this class of medications are an overlap between the therapeutic dosage and that producing sedation and dry mouth and the potential to cause the discontinuation syndrome and sexual dysfunction."	( Use of centrally acting sympatholytic agents in the management of hypertension. Epstein, M; Oster, JR, 1991)	0.28
" With guanfacine the maximal fall of blood pressure was comparable to that obtained with the 5-HT1A receptor ligands; however, in contrast to the latter, the dose-response curve was U-shaped, the highest dose eliciting a pressor effect with reversal of the vasodilatation."	( 8-OH-DPAT, flesinoxan and guanfacine: systemic and regional haemodynamic effects of centrally acting antihypertensive agents in anaesthetized rabbits. Fozard, JR; Hof, RP, 1989)	1.06
" Human pharmacokinetic studies in patients with renal failure indicate that due to an increase in metabolic clearance and increase in non-renal elimination of the drug guanfacine may be administered to elderly patients and patients with renal impairment without dosage adjustment."	( Pharmacology of guanfacine. Fetkovská, N; Scholtysik, G, 1987)	0.81
" The net blood pressure response during multiple dosing is the sum of these effects and is dependent on drug kinetics, receptor affinity, and receptor occupancy."	( Concentration-dependent blood pressure effects of guanfacine. Frisk-Holmberg, M; Wibell, L, 1986)	0.52
"In the present study, the antinociceptive effects of intrathecal injections of the alpha 2-adrenoceptor agonists clonidine and guanfacine in rats was determined to establish their dose-response curves."	( Antinociceptive effects and spinal cord tissue concentrations after intrathecal injection of guanfacine or clonidine into rats. Archer, T; Freedman, J; Gordh, T; Minor, BG; Post, C, 1987)	0.7
" B-HT920 was found to produce a dose-response profile qualitatively similar to, but weaker than, clonidine: low doses impaired memory and began to lower blood pressure and produce sedation, while high doses improved memory."	( The alpha-2 adrenergic agonist guanfacine improves memory in aged monkeys without sedative or hypotensive side effects: evidence for alpha-2 receptor subtypes. Arnsten, AF; Cai, JX; Goldman-Rakic, PS, 1988)	0.56
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage of guanfacine hydrochloride are reviewed."	( Guanfacine hydrochloride: a centrally acting antihypertensive agent. Cornish, LA, 1988)	1.94
" Blood samples were obtained before dosing and up to 72 hours after dosing for determination of drug levels in plasma."	( The bioavailability and pharmacokinetics of guanfacine after oral and intravenous administration to healthy volunteers. Carchman, SH; Crowe, JT; Wright, GJ, 1987)	0.53
" Based on pharmacokinetic studies in these target groups and on the dual renal and nonrenal clearance of guanfacine, the drug may, most probably, be administered to elderly patients and patients with renal insufficiency without dosage adjustment."	( Pharmacokinetics of guanfacine in patients with impaired renal function and in some elderly patients. Kiechel, JR, 1986)	0.81
" When this preparation was incubated with morphine for 1 h tolerance developed to the inhibitory effect, since dose-response curves were shifted to the right."	( Yohimbine reduces morphine tolerance in guinea-pig ileum. Alamo, C; Alguacil, LF; Cuenca, E; Santos, C, 1987)	0.27
"A series of N-(aminoiminomethyl)-1H-pyrrole-1-acetamides, related to guanfacine, were prepared and tested for antidiarrheal activity in castor oil dosed rats."	( Synthesis and antidiarrheal activity of N-(aminoiminomethyl)-1H-pyrrole-1-acetamides related to guanfacine. Beattie, DE; Dover, GM; Ward, TJ, 1985)	0.72
" The dose-response curve to guanfacine for increase in blood pressure was shifted in a parallel fashion to the right by 1 mg/kg of yohimbine, an alpha 2-antagonist and by 1 mg/kg of phentolamine, a nonselective alpha 1- and alpha 2-antagonist."	( [Effects of guanfacine on pre- and postsynaptic alpha-adrenoceptors studied in comparison with those of clonidine]. Chin, W; Imai, S; Nakagawa, Y, 1982)	0.94
" In contrast, the dose-response curves to tiamenidine and clonidine were flatter and bell-shaped with maxima of 30 and 60 min, respectively."	( Sleeping times evoked by alpha adrenoceptor agonists in two-day-old chicks: an experimental model to evaluate full and partial agonists at central alpha-2 adrenoceptors. Cavero, I; Doxey, JC; Roach, AG; Strachan, DA, 1983)	0.27
" Advice about the dosage regimen in such cases is given."	( Pharmacokinetic aspects of guanfacine withdrawal syndrome in a hypertensive patient with chronic renal failure. Comoy, E; Fillastre, JP; Godin, M; Guerret, M; Kiechel, JR; Lavene, D, 1983)	0.56
" Guanfacine in once-daily dosage reduced BP during rest (supine BP: control, 175 +/- 6/103 +/- 4 mm Hg; 1 yr guanfacine, 161 +/- 5/91 +/- 3 mm Hg)."	( Guanfacine in essential hypertension: effects during rest and isometric exercise. Hedner, T; Mellstrand, T; Nyberg, G, 1984)	2.62
" The results on efficacy and dosage after 5-7 years were identical with those obtained for the entire group after 1 year (n = 580) and 2 years (n = 162)."	( Long-term efficacy and tolerance of the antihypertensive agent guanfacine. Jerie, P; Lasance, A, 1984)	0.51
" We administered both drugs to rats using a dosage schedule which we had shown to produce hypertension and tachycardia when clonidine, but not guanfacine, was stopped after 3 weeks treatment."	( Studies on clonidine and guanfacine withdrawal after short term treatment in the rat. Barber, ND; Reid, JL, 1982)	0.77
" Thus guanfacine may be dosed independently of haemodialysis treatment periods."	( Pharmacokinetics of guanfacine in patients undergoing haemodialysis. Axthelm, T; Kirch, W; Kohler, H, )	0.94
" The vasodepressor effect of guanfacine was clearly dose-dependent, and was more marked when the initial level of the blood pressure was high, while that of clonidine was dose-dependent, only within a limited dosage range."	( [Antihypertensive effect of guanfacine in rats]. Hamamura, M; Hashimoto, T; Imai, S; Kumada, M; Mitomi, A; Nakagawa, Y; Sakurai, H; Takeda, K, 1981)	0.85
" For a 2 mg dosage the biological half-life was 22."	( [Clinical pharmacology of the antihypertensive action of guanfacine]. Georges, D; Safar, M; Weiss, Y, 1980)	0.51
" This could be overcome by either increasing dosage or adding a diuretic."	( Evaluation of long-term treatment of essential hypertension with guanfacine. Higuchi, M; Overlack, A; Stumpe, KO, 1980)	0.5
" A dose-response relationship could only be observed in vigilosomnograms, in the tests of self-estimation related to well-being and mood and in the decrease in plasma noradrenaline in the clonidine group."	( Differences in psychic performance with guanfacine and clonidine in normotensive subjects. Brecht, HM; Krauskopf, R; Kugler, J; Raschig, A; Seus, R, 1980)	0.53
" During the following time blood pressure and dosage remained almost unchanged."	( [A new antihypertensive agent used in a clinical setting]. Kaiser, HJ; Raschig, A; Wetzels, E, 1980)	0.26
" The other two patients required twice-daily dosing for optimal control of blood pressure."	( Effects of single and multiple doses of guanfacine in essential hypertension. Reid, JL; Zamboulis, C, 1980)	0.53
" The daily dosage of guanfacine did not have to be changed during the 3 years of treatment."	( Blood pressure and prolactin: effects of guanfacine. Three-year follow-up study. Gerber, S; Hauger-Klevene, JH; Pinkas, MB, )	0.72
"The results of one year's treatment of 243 hypertensive patients with guanfacine, given alone in a variety of doses and dosage schedules, were analyzed in terms of antihypertensive efficacy and incidence of side effects."	( Guanfacine in the treatment of hypertension: two years' experience with low dose monotherapy. Jerie, P; Lasance, A, 1981)	1.94
"5 mg/kg dosing for one aggressive episode, and resolved in the three milder episodes without dose or frequency being increased."	( Use of guanfacine to control self-injurious behavior in two rhesus macaques (Macaca mulatta) and one baboon (Papio anubis). Arnsten, AF; Beattie, TA; Macy, JD; Morgenstern, SE, 2000)	0.76
" Methylphenidate and amphetamine-based stimulants are now available in longer-acting, once-daily and shorter-acting divided dosing schedules."	( Pharmacological management of attention-deficit hyperactivity disorder. Reeves, G; Schweitzer, J, 2004)	0.32
" All mean vital-sign measurements and mean ECG parameters remained within normal limits after dosing and no marked changes from baseline measurements were noted."	( A phase I, randomized, open-label, crossover study of the single-dose pharmacokinetic properties of guanfacine extended-release 1-, 2-, and 4-mg tablets in healthy adults. Fiske, K; Lyne, A; Pennick, M; Shojaei, A; Swearingen, D, 2007)	0.56
"Blood samples, vital signs, and electrocardiograms (ECGs) were obtained before dosing on day 1 and at intervals over 24 hours, with repeat measurements on days 14 and 28."	( Pharmacokinetics of a guanfacine extended-release formulation in children and adolescents with attention-deficit-hyperactivity disorder. Boellner, SW; Fiske, K; Lyne, A; Pennick, M; Shojaei, A, 2007)	0.65
" Because the available immediate-release formulation requires multiple daily dosing and has been associated with rebound hypertension on abrupt cessation, an extended-release (ER) formulation has been developed for study of efficacy and tolerability parameters in patients with ADHD."	( Phase I, double-blind, randomized, placebo-controlled, dose-escalation study of the effects on blood pressure of abrupt cessation versus taper down of guanfacine extended-release tablets in adults aged 19 to 24 years. Fiske, K; Kisicki, JC; Lyne, A, 2007)	0.54
" Side effects of stimulants are generally mild, short lived, and responsive to adjustments in dosage or timing."	( Changes and challenges: managing ADHD in a fast-paced world. Bukstein, OG; Crismon, ML; Manos, MJ; Tom-Revzon, C, 2007)	0.34
" Somnolence, sedation, and fatigue adverse events emerged within the first 2 weeks of dosing and generally resolved by study end."	( Guanfacine extended release in children and adolescents with attention-deficit/hyperactivity disorder: a placebo-controlled trial. Biederman, J; Donahue, J; Lyne, A; McGough, J; Sallee, FR; Wigal, T, 2009)	1.8
" Improvements in ADHD symptoms were sustained over 24 months in two noncomparative, open-label extension trials in children and adolescents who received guanfacine ER at an optimized dosage of 1-4 mg/day."	( Guanfacine extended-release: in attention deficit hyperactivity disorder. Muir, VJ; Perry, CM, 2010)	2
" change in the ADHD rating scale, fourth edition [ADHD-RS-IV] total score from baseline) was compared between each GXR dosing group and the ATX group."	( Cost effectiveness of guanfacine extended-release versus atomoxetine for the treatment of attention-deficit/hyperactivity disorder: application of a matching-adjusted indirect comparison. Chen, KS; Erder, MH; Hodgkins, P; Lu, M; Signorovitch, JE; Sikirica, V; Wu, EQ; Xie, J, 2012)	0.69
" The levels of response and tolerability observed with GXR were similar regardless of time of dosing (morning versus evening), indicating that once-daily GXR monotherapy is effective whether administered in the morning or evening."	( Randomized, double-blind trial of guanfacine extended release in children with attention-deficit/hyperactivity disorder: morning or evening administration. Childress, AC; Enright, G; Newcorn, JH; Rubin, J; Stein, MA; White, C; Youcha, S, 2013)	0.67
" Similar results were observed in MAIC sensitivity analyses evaluating other dosage ranges and using more heterogeneous trial populations (e."	( Comparative efficacy of guanfacine extended release versus atomoxetine for the treatment of attention-deficit/hyperactivity disorder in children and adolescents: applying matching-adjusted indirect comparison methodology. Dammerman, R; Erder, MH; Findling, RL; Hodgkins, P; Lu, M; Signorovitch, J; Sikirica, V; Wu, EQ; Xie, J, 2013)	0.7
" Results were consistent in a variety of dosage range comparisons and within increasingly heterogeneous trial populations."	( Comparative efficacy of guanfacine extended release versus atomoxetine for the treatment of attention-deficit/hyperactivity disorder in children and adolescents: applying matching-adjusted indirect comparison methodology. Dammerman, R; Erder, MH; Findling, RL; Hodgkins, P; Lu, M; Signorovitch, J; Sikirica, V; Wu, EQ; Xie, J, 2013)	0.7
"The objective of this article was to review the efficacy, safety profile, mechanism of action, pharmacokinetics, and appropriate dosing of GXR in children and adolescents with ADHD."	( Guanfacine extended release: a novel treatment for attention-deficit/hyperactivity disorder in children and adolescents. Faraone, SV; López, FA; McBurnett, K; Sallee, FR; Steeber, J, 2013)	1.83
" Clinical trials analyzed according to weight-adjusted doses suggest a dose-response relationship for efficacy."	( Guanfacine extended release: a novel treatment for attention-deficit/hyperactivity disorder in children and adolescents. Faraone, SV; López, FA; McBurnett, K; Sallee, FR; Steeber, J, 2013)	1.83
"Guanfacine is an important medication option in very young children; however, there is a significant pharmacologic "information gap," and further research is needed to help establish appropriate, safe, and effective dosing of guanfacine in this population."	( Clinical and Pharmacologic Considerations for Guanfacine Use in Very Young Children. Black, BT; Jones, BL; Kearns, GL; Soden, SE, 2016)	2.14
" For many adolescents, such dosing would exceed 4 mg/day, the highest approved dose."	( Pharmacokinetics and pharmacodynamics of guanfacine extended release in adolescents aged 13-17 years with attention-deficit/hyperactivity disorder. Corcoran, M; Ermer, J; Martin, P; Padilla, AF; Satin, L; Stevenson, A; Vince, BD; White, C, 2014)	0.67
" The IR forms, while themselves not FDA approved for ADHD, may, with dosage adjustment, be reasonable alternatives (with considerable cost savings)."	( Treating ADHD in Prison: Focus on Alpha-2 Agonists (Clonidine and Guanfacine). Mattes, JA, 2016)	0.67
"Two hundred seven participants aged 7-14 years enrolled in an 8-week double-blind randomized trial of GUAN-IR (1-3 milligrams (mg)/day), DMPH (5-20 mg/day), or COMB with fixed-flexible dosing and titrated to optimal behavioral response."	( Acute and Long-Term Cardiovascular Effects of Stimulant, Guanfacine, and Combination Therapy for Attention-Deficit/Hyperactivity Disorder. Castelo, E; Cowen, J; Levitt, J; McCracken, JT; McGough, JJ; Sayer, GR; Sturm, A, 2016)	0.68
"Youth aged 6-17 years with a primary diagnosis of GAD, SAD, and/or social anxiety disorder were treated with flexibly dosed GXR (1-6 mg daily, n = 62) or placebo (n = 21) for 12 weeks."	( Extended Release Guanfacine in Pediatric Anxiety Disorders: A Pilot, Randomized, Placebo-Controlled Trial. Albano, AM; Compton, SN; Hamdani, M; Robertson, B; Rynn, MA; Strawn, JR, 2017)	0.79
" In one study, tics limited further dosage increases of methylphenidate."	( Pharmacological treatment for attention deficit hyperactivity disorder (ADHD) in children with comorbid tic disorders. Osland, ST; Pringsheim, T; Steeves, TD, 2018)	0.48
" Medication was titrated to stable dosing after each laboratory day (3 mg/d IR, then 4 mg/d ER, then 6 mg/d ER)."	( Pharmacokinetics and Pharmacodynamics of Immediate-Release Versus Extended-Release Guanfacine in Adult Daily Smokers. McKee, SA; Moore, KE; Oberleitner, LM; Peltier, MR; Roberts, W; Verplaetse, TL, )	0.36
" Our results showed that overall, nicotine induced significant place preference acquisition and swim stress-induced reinstatement in both male and female mice, but with different nicotine dose-response patterns."	( Variability in nicotine conditioned place preference and stress-induced reinstatement in mice: Effects of sex, initial chamber preference, and guanfacine. Calarco, CA; Lee, AM; McKee, SA; Mineur, YS; Picciotto, MR, 2020)	0.76
" The dosage administered as milligram per body weight to balance the potential benefits and risks of treatment."	( Determination of Guanfacine in Oral Fluid and Serum of Children and Adolescents with Attention-Deficit/Hyperactivity Disorder: A Short Communication. Fekete, S; Gerlach, M; Högger, P; Romanos, M; Scherf-Clavel, O; Wohkittel, C, 2022)	1.06
" Human mesenchymal stem cells (hMSCs) were incubated with a therapeutic plasma dosage of modafinil, atomoxetine and guanfacine."	( Psychostimulants Modafinil, Atomoxetine and Guanfacine Impair Bone Cell Differentiation and MSC Migration. Böker, KO; Di Fazio, P; Jäckle, K; Lehmann, W; Schilling, AF; Wagener, N; Weiser, L, 2022)	1.19

Class	Description
acetamides	Compounds with the general formula RNHC(=O)CH3.
[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)
Chain A, HADH2 protein	Homo sapiens (human)	Potency	7.9433	0.0251	20.2376	39.8107	AID886
Chain B, HADH2 protein	Homo sapiens (human)	Potency	7.9433	0.0251	20.2376	39.8107	AID886
thioredoxin reductase	Rattus norvegicus (Norway rat)	Potency	1.0000	0.1000	20.8793	79.4328	AID588453
TDP1 protein	Homo sapiens (human)	Potency	30.0534	0.0008	11.3822	44.6684	AID686978; AID686979
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)	Homo sapiens (human)	Potency	10.0000	0.0013	7.7625	44.6684	AID914; AID915
euchromatic histone-lysine N-methyltransferase 2	Homo sapiens (human)	Potency	12.5893	0.0355	20.9770	89.1251	AID504332
cytochrome P450 2D6 isoform 1	Homo sapiens (human)	Potency	0.1259	0.0020	7.5337	39.8107	AID891
cytochrome P450 2C19 precursor	Homo sapiens (human)	Potency	0.2512	0.0025	5.8400	31.6228	AID899
cytochrome P450 2C9 precursor	Homo sapiens (human)	Potency	25.1382	0.0063	6.9043	39.8107	AID883
D(1A) dopamine receptor	Homo sapiens (human)	Potency	10.0000	0.0224	5.9449	22.3872	AID488983
mitogen-activated protein kinase 1	Homo sapiens (human)	Potency	0.0040	0.0398	16.7842	39.8107	AID995
geminin	Homo sapiens (human)	Potency	21.5957	0.0046	11.3741	33.4983	AID624296; AID624297
cytochrome P450 3A4 isoform 1	Homo sapiens (human)	Potency	12.5893	0.0316	10.2792	39.8107	AID884; AID885
muscarinic acetylcholine receptor M1	Rattus norvegicus (Norway rat)	Potency	0.0126	0.0010	6.0009	35.4813	AID943
lethal factor (plasmid)	Bacillus anthracis str. A2012	Potency	12.5893	0.0200	10.7869	31.6228	AID912
lamin isoform A-delta10	Homo sapiens (human)	Potency	0.3548	0.8913	12.0676	28.1838	AID1487
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Histamine H2 receptor	Cavia porcellus (domestic guinea pig)	Potency	25.1382	0.0063	8.2350	39.8107	AID883
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
GABA theta subunit	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
[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)
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50 (µMol)	133.0000	0.6315	4.4531	9.3000	AID1473740
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50 (µMol)	133.0000	0.2000	5.6774	10.0000	AID1473741
5-hydroxytryptamine receptor 4	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	1.4530	0.0001	1.0076	8.7800	AID625218
5-hydroxytryptamine receptor 4	Cavia porcellus (domestic guinea pig)	Ki	0.7610	0.0000	0.8871	10.0000	AID625218
Bile salt export pump	Homo sapiens (human)	IC50 (µMol)	134.0000	0.1100	7.1903	10.0000	AID1443980; AID1473738
Alpha-2A adrenergic receptor	Homo sapiens (human)	IC50 (µMol)	0.1340	0.0000	1.4421	7.3470	AID625201
Alpha-2A adrenergic receptor	Homo sapiens (human)	Ki	0.0500	0.0001	0.8074	10.0000	AID625201
Alpha-2B adrenergic receptor	Homo sapiens (human)	IC50 (µMol)	0.2490	0.0000	1.2380	8.1590	AID625202
Alpha-2B adrenergic receptor	Homo sapiens (human)	Ki	0.1140	0.0002	0.7257	10.0000	AID625202
Alpha-2C adrenergic receptor	Homo sapiens (human)	IC50 (µMol)	6.4470	0.0000	1.4725	7.8980	AID625203
Alpha-2C adrenergic receptor	Homo sapiens (human)	Ki	0.9370	0.0003	0.4834	10.0000	AID625203
5-hydroxytryptamine receptor 2A	Homo sapiens (human)	IC50 (µMol)	3.0140	0.0001	0.8801	8.8500	AID625192
5-hydroxytryptamine receptor 2A	Homo sapiens (human)	Ki	0.8610	0.0000	0.3855	10.0000	AID625192
5-hydroxytryptamine receptor 2C	Homo sapiens (human)	IC50 (µMol)	1.4530	0.0001	1.0302	9.0000	AID625218
5-hydroxytryptamine receptor 2C	Homo sapiens (human)	Ki	0.7610	0.0001	0.9549	10.0000	AID625218
5-hydroxytryptamine receptor 2B	Homo sapiens (human)	IC50 (µMol)	2.0980	0.0001	1.1873	8.9125	AID625217
5-hydroxytryptamine receptor 2B	Homo sapiens (human)	Ki	1.3350	0.0003	0.7693	10.0000	AID625217
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50 (µMol)	133.0000	2.4100	6.3433	10.0000	AID1473739
Nischarin	Homo sapiens (human)	Ki	0.0190	0.0042	0.2192	3.8019	AID342861
[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)
POU domain, class 2, transcription factor 1	Homo sapiens (human)	Km	8.6000	2.1000	5.3900	8.6000	AID1769498
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
xenobiotic metabolic process	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
bile acid and bile salt transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
leukotriene transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
monoatomic anion transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transport across blood-brain barrier	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
prostaglandin secretion	Multidrug resistance-associated protein 4	Homo sapiens (human)
cilium assembly	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet degranulation	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic metabolic process	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
bile acid and bile salt transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
cAMP transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
leukotriene transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
monoatomic anion transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
export across plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
transport across blood-brain barrier	Multidrug resistance-associated protein 4	Homo sapiens (human)
guanine nucleotide transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
fatty acid metabolic process	Bile salt export pump	Homo sapiens (human)
bile acid biosynthetic process	Bile salt export pump	Homo sapiens (human)
xenobiotic metabolic process	Bile salt export pump	Homo sapiens (human)
xenobiotic transmembrane transport	Bile salt export pump	Homo sapiens (human)
response to oxidative stress	Bile salt export pump	Homo sapiens (human)
bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
response to organic cyclic compound	Bile salt export pump	Homo sapiens (human)
bile acid and bile salt transport	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transport	Bile salt export pump	Homo sapiens (human)
protein ubiquitination	Bile salt export pump	Homo sapiens (human)
regulation of fatty acid beta-oxidation	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transport	Bile salt export pump	Homo sapiens (human)
bile acid signaling pathway	Bile salt export pump	Homo sapiens (human)
cholesterol homeostasis	Bile salt export pump	Homo sapiens (human)
response to estrogen	Bile salt export pump	Homo sapiens (human)
response to ethanol	Bile salt export pump	Homo sapiens (human)
xenobiotic export from cell	Bile salt export pump	Homo sapiens (human)
lipid homeostasis	Bile salt export pump	Homo sapiens (human)
phospholipid homeostasis	Bile salt export pump	Homo sapiens (human)
positive regulation of bile acid secretion	Bile salt export pump	Homo sapiens (human)
regulation of bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
transmembrane transport	Bile salt export pump	Homo sapiens (human)
positive regulation of cytokine production	Alpha-2A adrenergic receptor	Homo sapiens (human)
DNA replication	Alpha-2A adrenergic receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Alpha-2A adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Alpha-2A adrenergic receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Alpha-2A adrenergic receptor	Homo sapiens (human)
Ras protein signal transduction	Alpha-2A adrenergic receptor	Homo sapiens (human)
Rho protein signal transduction	Alpha-2A adrenergic receptor	Homo sapiens (human)
female pregnancy	Alpha-2A adrenergic receptor	Homo sapiens (human)
positive regulation of cell population proliferation	Alpha-2A adrenergic receptor	Homo sapiens (human)
negative regulation of norepinephrine secretion	Alpha-2A adrenergic receptor	Homo sapiens (human)
regulation of vasoconstriction	Alpha-2A adrenergic receptor	Homo sapiens (human)
actin cytoskeleton organization	Alpha-2A adrenergic receptor	Homo sapiens (human)
platelet activation	Alpha-2A adrenergic receptor	Homo sapiens (human)
positive regulation of cell migration	Alpha-2A adrenergic receptor	Homo sapiens (human)
activation of protein kinase activity	Alpha-2A adrenergic receptor	Homo sapiens (human)
activation of protein kinase B activity	Alpha-2A adrenergic receptor	Homo sapiens (human)
negative regulation of epinephrine secretion	Alpha-2A adrenergic receptor	Homo sapiens (human)
cellular response to hormone stimulus	Alpha-2A adrenergic receptor	Homo sapiens (human)
receptor transactivation	Alpha-2A adrenergic receptor	Homo sapiens (human)
vasodilation	Alpha-2A adrenergic receptor	Homo sapiens (human)
glucose homeostasis	Alpha-2A adrenergic receptor	Homo sapiens (human)
fear response	Alpha-2A adrenergic receptor	Homo sapiens (human)
positive regulation of potassium ion transport	Alpha-2A adrenergic receptor	Homo sapiens (human)
positive regulation of MAP kinase activity	Alpha-2A adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Alpha-2A adrenergic receptor	Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathway	Alpha-2A adrenergic receptor	Homo sapiens (human)
negative regulation of calcium ion-dependent exocytosis	Alpha-2A adrenergic receptor	Homo sapiens (human)
negative regulation of insulin secretion	Alpha-2A adrenergic receptor	Homo sapiens (human)
intestinal absorption	Alpha-2A adrenergic receptor	Homo sapiens (human)
thermoception	Alpha-2A adrenergic receptor	Homo sapiens (human)
negative regulation of lipid catabolic process	Alpha-2A adrenergic receptor	Homo sapiens (human)
positive regulation of membrane protein ectodomain proteolysis	Alpha-2A adrenergic receptor	Homo sapiens (human)
negative regulation of calcium ion transport	Alpha-2A adrenergic receptor	Homo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulus	Alpha-2A adrenergic receptor	Homo sapiens (human)
negative regulation of uterine smooth muscle contraction	Alpha-2A adrenergic receptor	Homo sapiens (human)
adrenergic receptor signaling pathway	Alpha-2A adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Alpha-2A adrenergic receptor	Homo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathway	Alpha-2A adrenergic receptor	Homo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathway	Alpha-2A adrenergic receptor	Homo sapiens (human)
positive regulation of wound healing	Alpha-2A adrenergic receptor	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	Alpha-2A adrenergic receptor	Homo sapiens (human)
negative regulation of calcium ion transmembrane transporter activity	Alpha-2A adrenergic receptor	Homo sapiens (human)
negative regulation of DNA-templated transcription	POU domain, class 2, transcription factor 1	Homo sapiens (human)
negative regulation of DNA-templated transcription	POU domain, class 2, transcription factor 1	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	POU domain, class 2, transcription factor 1	Homo sapiens (human)
positive regulation of miRNA transcription	POU domain, class 2, transcription factor 1	Homo sapiens (human)
regulation of transcription by RNA polymerase II	POU domain, class 2, transcription factor 1	Homo sapiens (human)
MAPK cascade	Alpha-2B adrenergic receptor	Homo sapiens (human)
angiogenesis	Alpha-2B adrenergic receptor	Homo sapiens (human)
regulation of vascular associated smooth muscle contraction	Alpha-2B adrenergic receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Alpha-2B adrenergic receptor	Homo sapiens (human)
cell-cell signaling	Alpha-2B adrenergic receptor	Homo sapiens (human)
female pregnancy	Alpha-2B adrenergic receptor	Homo sapiens (human)
negative regulation of norepinephrine secretion	Alpha-2B adrenergic receptor	Homo sapiens (human)
platelet activation	Alpha-2B adrenergic receptor	Homo sapiens (human)
activation of protein kinase B activity	Alpha-2B adrenergic receptor	Homo sapiens (human)
negative regulation of epinephrine secretion	Alpha-2B adrenergic receptor	Homo sapiens (human)
receptor transactivation	Alpha-2B adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Alpha-2B adrenergic receptor	Homo sapiens (human)
positive regulation of neuron differentiation	Alpha-2B adrenergic receptor	Homo sapiens (human)
positive regulation of blood pressure	Alpha-2B adrenergic receptor	Homo sapiens (human)
positive regulation of uterine smooth muscle contraction	Alpha-2B adrenergic receptor	Homo sapiens (human)
adrenergic receptor signaling pathway	Alpha-2B adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Alpha-2B adrenergic receptor	Homo sapiens (human)
regulation of smooth muscle contraction	Alpha-2C adrenergic receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Alpha-2C adrenergic receptor	Homo sapiens (human)
cell-cell signaling	Alpha-2C adrenergic receptor	Homo sapiens (human)
negative regulation of norepinephrine secretion	Alpha-2C adrenergic receptor	Homo sapiens (human)
regulation of vasoconstriction	Alpha-2C adrenergic receptor	Homo sapiens (human)
platelet activation	Alpha-2C adrenergic receptor	Homo sapiens (human)
activation of protein kinase B activity	Alpha-2C adrenergic receptor	Homo sapiens (human)
negative regulation of epinephrine secretion	Alpha-2C adrenergic receptor	Homo sapiens (human)
receptor transactivation	Alpha-2C adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Alpha-2C adrenergic receptor	Homo sapiens (human)
positive regulation of neuron differentiation	Alpha-2C adrenergic receptor	Homo sapiens (human)
adrenergic receptor signaling pathway	Alpha-2C adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Alpha-2C adrenergic receptor	Homo sapiens (human)
negative regulation of insulin secretion	Alpha-2C adrenergic receptor	Homo sapiens (human)
temperature homeostasis	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of cytokine production involved in immune response	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
glycolytic process	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
intracellular calcium ion homeostasis	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
activation of phospholipase C activity	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
memory	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of cell population proliferation	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
response to xenobiotic stimulus	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
regulation of dopamine secretion	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
artery smooth muscle contraction	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
urinary bladder smooth muscle contraction	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of heat generation	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
negative regulation of potassium ion transport	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of neuron apoptotic process	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
protein localization to cytoskeleton	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of fat cell differentiation	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of glycolytic process	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of vasoconstriction	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
symbiont entry into host cell	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
sensitization	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
behavioral response to cocaine	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of inflammatory response	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
release of sequestered calcium ion into cytosol	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergic	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of execution phase of apoptosis	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of platelet aggregation	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
positive regulation of DNA biosynthetic process	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
behavioral fear response	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
intracellular calcium ion homeostasis	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
locomotory behavior	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
feeding behavior	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
cGMP-mediated signaling	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
regulation of nervous system process	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
regulation of appetite	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
regulation of corticotropin-releasing hormone secretion	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
positive regulation of fat cell differentiation	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
positive regulation of calcium-mediated signaling	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
release of sequestered calcium ion into cytosol	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
neural crest cell migration	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of cytokine production	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of endothelial cell proliferation	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled receptor internalization	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
heart morphogenesis	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cardiac muscle hypertrophy	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
intracellular calcium ion homeostasis	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
activation of phospholipase C activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of cell population proliferation	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
response to xenobiotic stimulus	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
neural crest cell differentiation	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
intestine smooth muscle contraction	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
phosphorylation	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
calcium-mediated signaling	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cGMP-mediated signaling	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
vasoconstriction	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
negative regulation of apoptotic process	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of MAP kinase activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
embryonic morphogenesis	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
regulation of behavior	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of nitric-oxide synthase activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
release of sequestered calcium ion into cytosol	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of cell division	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
ERK1 and ERK2 cascade	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
protein kinase C signaling	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cellular response to temperature stimulus	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
xenobiotic metabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
negative regulation of gene expression	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bile acid and bile salt transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
heme catabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic export from cell	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transepithelial transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
leukotriene transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
monoatomic anion transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apoptotic process	Nischarin	Homo sapiens (human)
Rac protein signal transduction	Nischarin	Homo sapiens (human)
actin cytoskeleton organization	Nischarin	Homo sapiens (human)
negative regulation of cell migration	Nischarin	Homo sapiens (human)
outer dynein arm assembly	Nischarin	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
ATP binding	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type xenobiotic transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type bile acid transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATP hydrolysis activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
icosanoid transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
guanine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
protein binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
purine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type bile acid transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
efflux transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP hydrolysis activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
protein binding	Bile salt export pump	Homo sapiens (human)
ATP binding	Bile salt export pump	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Bile salt export pump	Homo sapiens (human)
bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
ABC-type bile acid transporter activity	Bile salt export pump	Homo sapiens (human)
ATP hydrolysis activity	Bile salt export pump	Homo sapiens (human)
alpha2-adrenergic receptor activity	Alpha-2A adrenergic receptor	Homo sapiens (human)
protein binding	Alpha-2A adrenergic receptor	Homo sapiens (human)
protein kinase binding	Alpha-2A adrenergic receptor	Homo sapiens (human)
alpha-1B adrenergic receptor binding	Alpha-2A adrenergic receptor	Homo sapiens (human)
alpha-2C adrenergic receptor binding	Alpha-2A adrenergic receptor	Homo sapiens (human)
thioesterase binding	Alpha-2A adrenergic receptor	Homo sapiens (human)
heterotrimeric G-protein binding	Alpha-2A adrenergic receptor	Homo sapiens (human)
protein homodimerization activity	Alpha-2A adrenergic receptor	Homo sapiens (human)
protein heterodimerization activity	Alpha-2A adrenergic receptor	Homo sapiens (human)
epinephrine binding	Alpha-2A adrenergic receptor	Homo sapiens (human)
norepinephrine binding	Alpha-2A adrenergic receptor	Homo sapiens (human)
guanyl-nucleotide exchange factor activity	Alpha-2A adrenergic receptor	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	POU domain, class 2, transcription factor 1	Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA binding	POU domain, class 2, transcription factor 1	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	POU domain, class 2, transcription factor 1	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	POU domain, class 2, transcription factor 1	Homo sapiens (human)
DNA binding	POU domain, class 2, transcription factor 1	Homo sapiens (human)
protein binding	POU domain, class 2, transcription factor 1	Homo sapiens (human)
sequence-specific DNA binding	POU domain, class 2, transcription factor 1	Homo sapiens (human)
alpha2-adrenergic receptor activity	Alpha-2B adrenergic receptor	Homo sapiens (human)
protein binding	Alpha-2B adrenergic receptor	Homo sapiens (human)
epinephrine binding	Alpha-2B adrenergic receptor	Homo sapiens (human)
alpha2-adrenergic receptor activity	Alpha-2C adrenergic receptor	Homo sapiens (human)
protein binding	Alpha-2C adrenergic receptor	Homo sapiens (human)
alpha-2A adrenergic receptor binding	Alpha-2C adrenergic receptor	Homo sapiens (human)
protein homodimerization activity	Alpha-2C adrenergic receptor	Homo sapiens (human)
protein heterodimerization activity	Alpha-2C adrenergic receptor	Homo sapiens (human)
epinephrine binding	Alpha-2C adrenergic receptor	Homo sapiens (human)
guanyl-nucleotide exchange factor activity	Alpha-2C adrenergic receptor	Homo sapiens (human)
Gq/11-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
virus receptor activity	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
protein tyrosine kinase activator activity	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
identical protein binding	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
protein-containing complex binding	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
serotonin binding	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
Gq/11-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
identical protein binding	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
serotonin binding	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
Gq/11-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G-protein alpha-subunit binding	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
GTPase activator activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
serotonin binding	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
protein binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
organic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP hydrolysis activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
integrin binding	Nischarin	Homo sapiens (human)
protein binding	Nischarin	Homo sapiens (human)
phosphatidylinositol binding	Nischarin	Homo sapiens (human)
identical protein binding	Nischarin	Homo sapiens (human)
dynein heavy chain binding	Nischarin	Homo sapiens (human)
alpha-tubulin binding	Nischarin	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basal plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basolateral plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
nucleolus	Multidrug resistance-associated protein 4	Homo sapiens (human)
Golgi apparatus	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
basolateral plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet dense granule membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
external side of apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
basolateral plasma membrane	Bile salt export pump	Homo sapiens (human)
Golgi membrane	Bile salt export pump	Homo sapiens (human)
endosome	Bile salt export pump	Homo sapiens (human)
plasma membrane	Bile salt export pump	Homo sapiens (human)
cell surface	Bile salt export pump	Homo sapiens (human)
apical plasma membrane	Bile salt export pump	Homo sapiens (human)
intercellular canaliculus	Bile salt export pump	Homo sapiens (human)
intracellular canaliculus	Bile salt export pump	Homo sapiens (human)
recycling endosome	Bile salt export pump	Homo sapiens (human)
recycling endosome membrane	Bile salt export pump	Homo sapiens (human)
extracellular exosome	Bile salt export pump	Homo sapiens (human)
membrane	Bile salt export pump	Homo sapiens (human)
cytoplasm	Alpha-2A adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-2A adrenergic receptor	Homo sapiens (human)
basolateral plasma membrane	Alpha-2A adrenergic receptor	Homo sapiens (human)
neuronal cell body	Alpha-2A adrenergic receptor	Homo sapiens (human)
axon terminus	Alpha-2A adrenergic receptor	Homo sapiens (human)
presynaptic active zone membrane	Alpha-2A adrenergic receptor	Homo sapiens (human)
dopaminergic synapse	Alpha-2A adrenergic receptor	Homo sapiens (human)
postsynaptic density membrane	Alpha-2A adrenergic receptor	Homo sapiens (human)
glutamatergic synapse	Alpha-2A adrenergic receptor	Homo sapiens (human)
GABA-ergic synapse	Alpha-2A adrenergic receptor	Homo sapiens (human)
receptor complex	Alpha-2A adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-2A adrenergic receptor	Homo sapiens (human)
nucleus	POU domain, class 2, transcription factor 1	Homo sapiens (human)
nucleoplasm	POU domain, class 2, transcription factor 1	Homo sapiens (human)
endoplasmic reticulum	POU domain, class 2, transcription factor 1	Homo sapiens (human)
intracellular membrane-bounded organelle	POU domain, class 2, transcription factor 1	Homo sapiens (human)
chromatin	POU domain, class 2, transcription factor 1	Homo sapiens (human)
RNA polymerase II transcription regulator complex	POU domain, class 2, transcription factor 1	Homo sapiens (human)
cytosol	Alpha-2B adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-2B adrenergic receptor	Homo sapiens (human)
cell surface	Alpha-2B adrenergic receptor	Homo sapiens (human)
intracellular membrane-bounded organelle	Alpha-2B adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-2B adrenergic receptor	Homo sapiens (human)
plasma membrane	Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)
cytoplasm	Alpha-2C adrenergic receptor	Homo sapiens (human)
endosome	Alpha-2C adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-2C adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-2C adrenergic receptor	Homo sapiens (human)
neurofilament	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
caveola	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
axon	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
cytoplasmic vesicle	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
presynaptic membrane	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
neuronal cell body	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
dendritic shaft	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
postsynaptic membrane	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
cell body fiber	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
glutamatergic synapse	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
G protein-coupled serotonin receptor complex	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 2A	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
G protein-coupled serotonin receptor complex	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
nucleoplasm	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cytoplasm	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled serotonin receptor complex	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
plasma membrane	Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)
plasma membrane	Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)
plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
cell surface	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
intercellular canaliculus	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
nucleoplasm	Nischarin	Homo sapiens (human)
early endosome	Nischarin	Homo sapiens (human)
cytosol	Nischarin	Homo sapiens (human)
plasma membrane	Nischarin	Homo sapiens (human)
microtubule cytoskeleton	Nischarin	Homo sapiens (human)
membrane	Nischarin	Homo sapiens (human)
intracellular membrane-bounded organelle	Nischarin	Homo sapiens (human)
intercellular bridge	Nischarin	Homo sapiens (human)
recycling endosome	Nischarin	Homo sapiens (human)
cytoplasm	Nischarin	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
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.
AID540212	Mean residence time in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540213	Half life in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID588216	FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588217	FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID540210	Clearance in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625286	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625288	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444053	Renal clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1473740	Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1473739	Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID588219	FDA HLAED, gamma-glutamyl transferase (GGT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588218	FDA HLAED, lactate dehydrogenase (LDH) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588214	FDA HLAED, liver enzyme composite activity	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID342861	Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR	2008	Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15	QSAR study of imidazoline antihypertensive drugs.
AID444051	Total clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444052	Hepatic clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625280	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588215	FDA HLAED, alkaline phosphatase increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID444058	Volume of distribution at steady state in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1474166	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID425653	Renal clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID444055	Fraction absorbed in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625287	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625292	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID540209	Volume of distribution at steady state in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444056	Fraction escaping gut-wall elimination in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625279	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID625285	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625284	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444057	Fraction escaping hepatic elimination in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID425652	Total body clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID444054	Oral bioavailability in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625282	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444050	Fraction unbound in human plasma	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625289	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1473741	Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1443980	Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch	2010	Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2	Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID625290	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625291	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID540211	Fraction unbound in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1473738	Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1769501	Ratio of drug uptake in human OCT1 expressing HEK293 cells at 2.5 uM to drug uptake in empty vector transfected human HEK293 cells at 2.5 uM	2021	Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5	Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation.
AID1769498	Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring Km incubated for 2 mins by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5	Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation.
AID1769500	Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring intrinsic clearance incubated for 2 mins by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5	Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation.
AID1769499	Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring Vmax incubated for 2 mins by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5	Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation.
AID227718	Binding energy by using the equation deltaG obsd = -RT ln KD	1984	Journal of medicinal chemistry, Dec, Volume: 27, Issue:12	Functional group contributions to drug-receptor interactions.
AID625283	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
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.
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.
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.
AID588349	qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
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.
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.
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.
AID588378	qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1346049	Human alpha2A-adrenoceptor (Adrenoceptors)	1998	Biochemical pharmacology, Apr-01, Volume: 55, Issue:7	Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
AID1346049	Human alpha2A-adrenoceptor (Adrenoceptors)	1997	British journal of pharmacology, Aug, Volume: 121, Issue:8	Characterization of alpha 2-adrenoceptors mediating contraction of dog saphenous vein: identity with the human alpha 2A subtype.
AID1346159	Human alpha2C-adrenoceptor (Adrenoceptors)	1998	Biochemical pharmacology, Apr-01, Volume: 55, Issue:7	Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
AID1346058	Human alpha2B-adrenoceptor (Adrenoceptors)	1998	Biochemical pharmacology, Apr-01, Volume: 55, Issue:7	Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
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.
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	244 (33.06)	18.7374
1990's	95 (12.87)	18.2507
2000's	108 (14.63)	29.6817
2010's	221 (29.95)	24.3611
2020's	70 (9.49)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	180 (22.96%)	5.53%
Reviews	103 (13.14%)	6.00%
Case Studies	53 (6.76%)	4.05%
Observational	3 (0.38%)	0.25%
Other	445 (56.76%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (75)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Language-based Learning Skills and ADHD: Impact of Treatment With Sustained-release Guanfacine [NCT01146002]	Phase 4	30 participants (Actual)	Interventional	2010-06-30	Completed
A Double-Blind, Randomized, Multi-Center, Flexible Dose Study Evaluating the Efficacy and Safety of SPD503 (Guanfacine Hydrochloride) in Children Aged 6-12 With Symptoms of Oppositionality and a Diagnosis of Attention Deficit/Hyperactivity Disorder [NCT00367835]	Phase 3	217 participants (Actual)	Interventional	2006-12-04	Completed
Guanfacine for PONV and Pain After Sinus Surgery [NCT02882854]		84 participants (Actual)	Interventional	2016-11-30	Completed
Guanfacine Extended-release Randomised Controlled Trial for Adolescents With Cannabis usE (GRACE) [NCT05957848]	Phase 2	100 participants (Anticipated)	Interventional	2023-07-27	Recruiting
Guanfacine Enhancement of Working Memory: Prospects for Augmenting Cognitive Remediation in the Schizophrenia Spectrum [NCT02524899]	Phase 2	45 participants (Actual)	Interventional	2014-01-31	Completed
The Use of Guanfacine (GUA) (3mg/Day) to Reduce Drug Craving, Improve Cognitive Flexibility and Result in Associated Lower Drug Use in Women With Substance Use Disorder (SUD). [NCT03980184]	Phase 2	74 participants (Actual)	Interventional	2019-11-01	Active, not recruiting
Phase 4 Study of the Effect of Extended Release Guanfacine on Working Memory in Children With ADHD [NCT01177306]	Phase 4	18 participants (Actual)	Interventional	2010-07-31	Completed
Guanfacine Extended Release and Mindfulness in Traumatically Stressed Children and Adolescents Study [NCT03258476]	Phase 4	0 participants (Actual)	Interventional	2019-03-01	Withdrawn(stopped due to Contract terminated)
Electrophysiological Effects of Guanfacine Extended-Release (GXR) on Inhibitory Control in Children With Attention Deficit/Hyperactivity Disorder (ADHD) [NCT01069523]	Phase 4	42 participants (Actual)	Interventional	2010-03-31	Completed
Phase 3,Double Blind,Placebo-controlled,Multicentre,Randomised-withdrawal,Long-term Maintenance of Efficacy&Safety Study of Extended-release Guanfacine Hydrochloride in Children/Adolescents Aged 6-17 With ADHD [NCT03662763]	Phase 3	12 participants (Actual)	Interventional	2011-09-30	Completed
A Phase III, Randomized, Double-Blind, Multi-Center, Parallel-Group, Placebo-Controlled Safety and Efficacy Study of SPD503 in Children and Adolescents Aged 6-17 With Attention Deficit Hyperactivity Disorder (ADHD) [NCT00150618]	Phase 3	324 participants (Actual)	Interventional	2004-03-30	Completed
A Phase III, Double-Blind, Randomized, Placebo-Controlled, Multi-Center, Dose Optimization Study Evaluating the Efficacy and Safety of SPD503 in Combination With Psychostimulants in Children and Adolescents Aged 6-17 Years With a Diagnosis of Attention-De [NCT00734578]	Phase 3	461 participants (Actual)	Interventional	2008-09-02	Completed
A Phase II, Open-Label Co-Administration Study of SPD503 and Psychostimulants in Children and Adolescents Aged 6-17 With Attention-Deficit/Hyperactivity Disorder (ADHD) [NCT00151996]	Phase 2	75 participants (Actual)	Interventional	2004-08-16	Completed
A Phase I, Randomized, Gender Stratified, Double-Blind, Placebo- and Positive-Controlled, Three Period Crossover Trial to Assess the Effect of Guanfacine Hydrochloride on QT/QTc Interval in Healthy Men and Women [NCT00672984]	Phase 1	83 participants (Actual)	Interventional	2008-04-18	Completed
Maximizing trEatment of Neurological Dysfunction Using INtravenous Guanfacine Study [NCT04742673]	Phase 2	50 participants (Anticipated)	Interventional	2021-05-04	Recruiting
Interdisciplinary Medication Development for Multiple Risk Factors in Relapse. [NCT00613015]	Phase 2	109 participants (Actual)	Interventional	2008-05-31	Completed
A Phase 3 Randomized, Double-Blind, Placebo- and Active-Controlled, Multi-center, Parallel Group Study to Evaluate the Safety and Efficacy of Darusentan in Subjects With Resistant Hypertension Receiving Combination Therapy With Three or More Antihypertens [NCT00389779]	Phase 3	849 participants (Actual)	Interventional	2006-09-30	Completed
Double-Blind, Randomized, Placebo-Controlled, Single- Center, Dose Optimization Study Evaluating Efficacy and Safety of Guanfacine Hydrochloride in Combination With Psychostimulants in Adults Aged 18-65 Years With a Diagnosis of ADHD [NCT02141113]	Phase 4	26 participants (Actual)	Interventional	2012-11-30	Completed
Mechanistic Evaluation of Guanfacine on Drinking Behavior in Women and Men With Alcohol Use Disorders [NCT03764098]	Phase 2	160 participants (Anticipated)	Interventional	2020-08-10	Recruiting
Association Between Angiotensin Converting Enzyme Inhibitor or Angiotensin Receptor Blocker Use and COVID-19 Severity and Mortality Among US Veterans [NCT04467931]		22,213 participants (Actual)	Observational	2020-01-19	Completed
A Phase 3, Double-blind, Placebo-controlled, Multicentre, Randomised Withdrawal, Long-term Maintenance of Efficacy and Safety Study of Extended-release Guanfacine Hydrochloride in Children and Adolescents Aged 6-17 With Attention Deficit/Hyperactivity Dis [NCT01081145]	Phase 3	528 participants (Actual)	Interventional	2010-05-11	Completed
Randomised Clinical Trial of Noradrenergic Add-on Therapy With Extended-Release Guanfacine in Alzheimer's Disease [NCT03116126]	Phase 3	160 participants (Anticipated)	Interventional	2019-01-04	Recruiting
Pharmacokinetics, Pharmacodynamics, and Safety Profile of Understudied Drugs [NCT04278404]		5,000 participants (Anticipated)	Observational	2020-03-05	Recruiting
Combining Varenicline and Guanfacine for Smoking Cessation [NCT04198116]	Phase 2	140 participants (Anticipated)	Interventional	2020-11-01	Recruiting
An Eight-Week, Randomized, Double-Blind Comparison of Guanfacine, Focalin XR, and the Combination, With a Twelve Month Open-Label Extension for the Treatment of ADHD in Pediatric Subjects Aged 7 to 14 Years [NCT00429273]	Phase 4	212 participants (Actual)	Interventional	2007-01-31	Completed
A Randomized, Double-Blind, 2-Way Crossover Trial to Assess the Efficacy of Guanfacine and Lidocaine Combination Versus Lidocaine Alone in Trigeminal Nerve Block for Pain Management in Painful Trigeminal Neuropathy Patients [NCT03865940]	Phase 2	36 participants (Actual)	Interventional	2019-11-04	Active, not recruiting
Non-interventional Trial to Investigate the Change of Psychopathological Markers of Affective Dysregulation (AD) in Children With Attention Deficit Hyperactivity Disorder (ADHD) Treated by Guanfacin, a Pilot Trial [NCT04016207]		40 participants (Anticipated)	Observational	2020-04-01	Not yet recruiting
Attention Deficit/Hyperactivity Disorder (ADHD) Medications in Japan: A Retrospective Cohort Study of Label Compliance [NCT04113551]		17,418 participants (Actual)	Observational	2019-10-01	Completed
A Double Blind, Placebo Controlled, Fixed-Flexible Dose Clinical Trial of Guanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome [NCT05657860]	Phase 4	33 participants (Anticipated)	Interventional	2020-12-17	Recruiting
Dose Clinical Trial of Guanfacine Extended Release for the Reduction of Aggression and Self-injuries Behavior Associated With Prader-Willi Syndrome [NCT04066088]	Phase 4	0 participants (Actual)	Interventional	2019-12-01	Withdrawn(stopped due to PI departure from institution)
Effect of Guanfacine on the Reversal of Opioid-induced Hyperalgesia (OIH) [NCT02192398]		120 participants (Anticipated)	Interventional	2014-09-30	Active, not recruiting
Effect of Guanfacine on Opioid-induced Hyperalgesia (OIH) and Tolerance [NCT01681264]	Phase 4	200 participants (Anticipated)	Interventional	2013-11-30	Active, not recruiting
A Phase II Study to Assess the Safety, Tolerability and Efficacy of SPD503 Administered to Children and Adolescents Aged 6-17 With Attention-Deficit/Hyperactivity Disorder (ADHD) [NCT00150592]	Phase 2	182 participants (Actual)	Interventional	2005-05-12	Completed
A Phase 3, Double-blind, Randomized, Multi-center, Placebo Controlled, Dose-optimization Study Evaluating the Safety, Efficacy, and Tolerability of Once Daily Dosing With Extended-release Guanfacine Hydrochloride in Adolescents Aged 13-17 Years Diagnosed [NCT01081132]	Phase 3	314 participants (Actual)	Interventional	2011-09-19	Completed
Open-Label Pilot Study of Guanfacine-Extended Release for the Treatment of Cannabis Dependence [NCT01467999]	Phase 1	22 participants (Actual)	Interventional	2012-02-29	Completed
A Phase 3, Double-blind, Randomized, Multicenter, Placebo-controlled, Dose Optimization Study Evaluating the Tolerability and Efficacy of AM and PM Once Daily Dosing With Extended-release Guanfacine Hydrochloride in Children Aged 6-12 With a Diagnosis of [NCT00997984]	Phase 3	340 participants (Actual)	Interventional	2009-11-17	Completed
Effect of Guanfacine Extended-Release on Attention Deficit Hyperactivity Disorder (ADHD)-Associated Insomnia [NCT01156051]	Phase 4	29 participants (Actual)	Interventional	2010-06-30	Terminated(stopped due to extended beyond completion date; chose to close out rather than renew IRB review)
A Phase 1, Open-label, Randomized, Three-period Crossover Drug Interaction Study Evaluating the Pharmacokinetic Profiles of SPD503 and VYVANSE, Administered Alone and in Combination in Healthy Adult Volunteers [NCT00919867]	Phase 1	42 participants (Actual)	Interventional	2009-06-24	Completed
Pharmacology of Cognition in Schizotypal Personality Disorder: Guanfacine for Cognitive Symptoms in Schizotypal Personality Disorder [NCT00353379]	Phase 4	29 participants (Actual)	Interventional	1995-09-30	Terminated(stopped due to low enrollment)
Guanfacine Treatment for Prefrontal Cognitive Dysfunction in Elderly Subjects [NCT00935493]		154 participants (Actual)	Interventional	2009-06-30	Completed
The Relative Efficacy of Aerobic Exercise in the Treatment of Adults With Attention Deficit Hyperactivity Disorder (ADHD) Versus Medication Only and the Combination of the Two: A Pilot Study [NCT02788851]		70 participants (Anticipated)	Interventional	2016-04-30	Active, not recruiting
Guanfacine to Reduce Stress-Induced Cocaine/Alcohol Craving and Relapse [NCT00585754]	Phase 1	75 participants (Actual)	Interventional	2006-04-30	Completed
A Double Blind Placebo Controlled Study of Guanfacine Adjunctive Treatment to Atypical Antipsychotics for Cognitive Dysfunction in Schizophrenia [NCT00469664]	Phase 4	50 participants (Anticipated)	Interventional	2000-02-29	Active, not recruiting
Naturalistic Study of ADHD Medication and Predictors of Treatment Outcome [NCT02136147]		632 participants (Actual)	Observational [Patient Registry]	2015-06-30	Completed
Guanfacine for the Treatment of Hyperactivity in Pervasive Developmental Disorder [NCT01238575]	Phase 4	62 participants (Actual)	Interventional	2011-12-31	Completed
Precision Mental Health: Evaluating Biotype-guided Interventions for Depression [NCT04181736]	Phase 4	64 participants (Anticipated)	Interventional	2022-07-01	Recruiting
[NCT00004376]	Phase 3	35 participants	Interventional	1994-09-30	Completed
Reading ICARD: Interventions for Children With Attention and Reading Disorders [NCT01133847]	Phase 4	222 participants (Actual)	Interventional	2010-11-30	Completed
A Phase 3, Randomised, Double-blind, Multicentre, Parallel-group, Placebo- and Active-reference, Dose-optimisation Efficacy and Safety Study of Extended-release Guanfacine Hydrochloride in Children and Adolescents Aged 6-17 Years With Attention-Deficit/Hy [NCT01244490]	Phase 3	338 participants (Actual)	Interventional	2011-01-17	Completed
The Effect of Guanfacine on Delirium in Critically Ill Patients [NCT04578886]	Phase 3	101 participants (Actual)	Interventional	2020-11-23	Completed
Guanfacine in the Treatment of Borderline Personality Disorder [NCT00358969]		0 participants	Interventional	2006-07-31	Recruiting
Guanfacine for the Treatment of PTSD [NCT00018603]	Phase 1	0 participants	Interventional	1999-11-30	Completed
Methylphenidate for Hyperactivity and Impulsiveness in Children and Adolescents With Pervasive Developmental Disorders [NCT00025779]		60 participants	Interventional	2001-10-31	Completed
The Effects of Ketamine and Guanfacine on Working Memory in Healthy Subjects [NCT01600885]		16 participants (Actual)	Interventional	2008-08-31	Completed
The Pathophysiology and Treatment of Supine Hypertension in Patients With Autonomic Failure [NCT00223717]	Phase 1	152 participants (Actual)	Interventional	2001-01-31	Completed
Experimental fMRI Study on the Comparison of the Brain Function Effects of a Single Dose of Guanfacine and Lisdexamfetamine Relative to Placebo in Children and Adolescents With ADHD. [NCT03333668]		20 participants (Anticipated)	Interventional	2018-10-01	Active, not recruiting
Pharmacokinetic/Dynamic (PK/PD) Comparison of Guanfacine Extended Release (ER) and Immediate Release (IR) in Smokers [NCT01904526]	Phase 2	5 participants (Actual)	Interventional	2013-07-31	Completed
Does Guanfacine Attenuate Stress-Induced Drinking? [NCT02164422]	Phase 2	70 participants (Actual)	Interventional	2014-06-30	Completed
Neurobiological Basis of Response to Guanfacine Extended Release in Children and Adolescents With Attention-deficit/Hyperactivity Disorder (ADHD): an Functional Magnetic Resonance Imaging(fMRI) Study of Brain Activation Pre and Post Treatment [NCT01709695]	Phase 4	27 participants (Actual)	Interventional	2011-03-31	Completed
A Double-Blind, Active-Controlled, Long-Term Safety Extension Study of Optimized Doses of Darusentan in Subjects With Resistant Hypertension Despite Receiving Combination Therapy With Three or More Antihypertensive Drugs, Including a Diuretic, as Compared [NCT00389675]	Phase 3	661 participants (Actual)	Interventional	2007-05-31	Terminated(stopped due to Study DAR-312 did not meet its primary co-endpoints.)
Guanfacine in Children With Tic Disorders: A Multi-site Study [NCT01547000]	Phase 4	34 participants (Actual)	Interventional	2012-04-30	Completed
A Phase 3, Open-label, Multicentre Study to Provide Access to Guanfacine Hydrochloride Extended-release for European Subjects With Attention-deficit/Hyperactivity Disorder (ADHD) Who Participated in Study SPD503-315 or SPD503-316 [NCT01500694]	Phase 3	215 participants (Actual)	Interventional	2012-03-20	Completed
Imaging Stimulant vs. Non-Stimulant Treatment of Attention Deficit Hyperactivity Disorder (ADHD) [NCT02259517]		38 participants (Actual)	Interventional	2014-09-30	Terminated(stopped due to Recruitment/enrollment ended early due to the COVID-19 pandemic)
A Trial of Guanfacine, an Alpha 2 Adrenergic Agonist, for Spatial Neglect and Impaired Vigilance Following Stroke and Focal Brain Damage [NCT00955253]	Phase 2	13 participants (Actual)	Interventional	2010-04-30	Completed
Modeling Stress-precipitated Smoking Behavior for Medication Development [NCT00773357]	Phase 2	100 participants (Actual)	Interventional	2008-10-31	Completed
Intuniv vs Placebo in the Treatment of Childhood Intermittent Explosive Disorder [NCT02048241]	Phase 4	11 participants (Actual)	Interventional	2011-07-31	Completed
A Single-Center, Randomized, Double Blind, Placebo-Controlled, Crossover Evaluation of the Effect of GXR as Adjunctive Treatment With Stimulant on Executive Function and Quality of Life at Home and School in Children With ADHD [NCT01985581]	Phase 4	50 participants (Actual)	Interventional	2013-10-31	Completed
A Randomized Controlled Trial of Guanfacine-er for Cannabis Use Disorder [NCT05273567]	Phase 2	90 participants (Anticipated)	Interventional	2022-06-01	Active, not recruiting
A Phase 2, Randomized, Double-blind, Placebo-controlled, Multicenter Study to Assess the Safety and Tolerability of SPD503 in Subjects Aged 6-17 Years With Generalized Anxiety Disorder (GAD), Separation Anxiety Disorder (SAD), or Social Phobia (SoP). [NCT01470469]	Phase 2	83 participants (Actual)	Interventional	2012-01-04	Completed
A Placebo Controlled Double Blinded Crossover Study of the Antihypertensive Efficacy of Guanfacine vs Hydrochlorothiazide in Obstructive Sleep Apnea (OSA) Associated Hypertension [NCT02699125]	Phase 4	41 participants (Actual)	Interventional	2015-01-31	Completed
Guanfacine to Reduce Relapse Risk in Women With Alcohol Use Disorder (AUD) [NCT03137082]	Phase 1/Phase 2	60 participants (Anticipated)	Interventional	2017-01-31	Recruiting
A Phase 4, Multicenter, 2-part Study Composed of a 1-Year Randomized, Double-blind, Parallel-group, Placebo-controlled, Active-comparator, Dose-optimization Evaluation Followed by a 1-Year Open-label Evaluation to Assess the Safety and Efficacy of Guanfac [NCT04085172]	Phase 4	288 participants (Anticipated)	Interventional	2019-09-18	Recruiting
Guanfacine for Hyperactivity in Children With Down Syndrome (HYPEbeGONE_DS) [NCT06042257]	Phase 2	60 participants (Anticipated)	Interventional	2023-12-31	Not yet recruiting
A Phase III, Randomized, Multi-Center, Double-Blind, Parallel-Group, Placebo-Controlled Safety and Efficacy Study of SPD503 in Children and Adolescents Aged 6-17 With Attention-Deficit/Hyperactivity Disorder (ADHD) [NCT00152009]	Phase 3	345 participants (Actual)	Interventional	2003-01-29	Completed
Phase-II Clinical Trial Evaluating Guanfacine for Smoking Cessation [NCT02051309]	Phase 2	121 participants (Actual)	Interventional	2014-03-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00150592 (8) [back to overview]	Change From Baseline in Choice Reaction Time (CRT) at 6 Weeks
NCT00150592 (8) [back to overview]	Change From Baseline in Digital Symbol Substitution Task/Coding Test (DSST/Coding) Scores at 6 Weeks in Age Category 8-17 Years
NCT00150592 (8) [back to overview]	Change From Baseline in DSST/Coding Scores at 6 Weeks in Age Category 6-7 Years
NCT00150592 (8) [back to overview]	Change From Baseline in Pediatric Daytime Sleepiness Scale (PDSS) Scores at 6 Weeks
NCT00150592 (8) [back to overview]	Change From Baseline in Pictorial Sleepiness Scale (PSS) Scores at 6 Weeks
NCT00150592 (8) [back to overview]	Number of Participants With Improvement in Clinical Global Impression-Improvement (CGI-I) at 6 Weeks
NCT00150592 (8) [back to overview]	Change From Baseline in Spatial Working Memory (SWM) Scores at 6 Weeks
NCT00150592 (8) [back to overview]	Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale (ADHD-RS-IV) Total Score at 6 Weeks
NCT00150618 (5) [back to overview]	Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale (ADHD-RS-IV) Score at 6 Weeks
NCT00150618 (5) [back to overview]	Change From Baseline in Conner's Parent Rating Scale-revised Short Version (CPRS-R) Score at 6 Weeks
NCT00150618 (5) [back to overview]	Number of Participants With Improvement in Clinical Global Impression-Improvement (CGI-I)
NCT00150618 (5) [back to overview]	Number of Participants With Improvement in Parent Global Assessment (PGA)
NCT00150618 (5) [back to overview]	Change From Baseline in Child Health Questionnaire-Parent Form (CHQ-PF50) Score at 6 Weeks
NCT00151996 (5) [back to overview]	Number of Participants With Improvement on Clinical Global Impression-Improvement (CGI-I) Scores
NCT00151996 (5) [back to overview]	Number of Participants With Improvement on Parent Global Assessment (PGA) Scores
NCT00151996 (5) [back to overview]	Change From Baseline in Child Health Questionnaire-Parent Form (CHQ-PF50) Scores at 6 Weeks
NCT00151996 (5) [back to overview]	Change From Baseline in Conner's Parent Rating Scale-revised Short Version (CPRS-R) Total Score at 6 Weeks
NCT00151996 (5) [back to overview]	Change From Baseline in the Attention Deficit Hyperactivity Disorder Rating Scale (ADHD-RS-IV) Total Score at 6 Weeks
NCT00152009 (6) [back to overview]	Number of Participants With Improvement in Parent Global Assessment (PGA)
NCT00152009 (6) [back to overview]	Change From Baseline in Child Health Questionnaire-Parent Form (CHQ-PF50) Score at 5 Weeks
NCT00152009 (6) [back to overview]	Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale (ADHD-RS-IV) Score at Up to 5 Weeks
NCT00152009 (6) [back to overview]	Change From Baseline in Conner's Parent Rating Scale-revised Short Version (CPRS-R) Score at Up to 5 Weeks
NCT00152009 (6) [back to overview]	Change From Baseline in Conner's Teacher Rating Scale-revised Short Version (CTRS-R) Score at Up to 5 Weeks
NCT00152009 (6) [back to overview]	Number of Participants With Improvement in Clinical Global Impression-Improvement (CGI-I)
NCT00367835 (11) [back to overview]	Change From Baseline in Diastolic Blood Pressure at Up to 8 Weeks
NCT00367835 (11) [back to overview]	Change From Baseline in Electrocardiogram Results (QTcF Interval) at Up to 8 Weeks
NCT00367835 (11) [back to overview]	Change From Baseline in Pulse Rate at Up to 8 Weeks
NCT00367835 (11) [back to overview]	Change From Baseline in Systolic Blood Pressure at Up to 8 Weeks
NCT00367835 (11) [back to overview]	Change From Baseline in the 40-Item Conduct Problem Scale of the New York Parent's Rating Scale-School-aged (NYPRS-S) Score at Up to 8 Weeks
NCT00367835 (11) [back to overview]	Change From Baseline in the Oppositional Subscale of the Conners' Parent Rating Scale-Revised Long Form (CPRS-R:L) Score at Up to 8 Weeks
NCT00367835 (11) [back to overview]	Change From Baseline in the Parent Stress Index-Short Form (PSI/SF) Score at Up to 8 Weeks
NCT00367835 (11) [back to overview]	Number of Participants With Improvement on Clinical Global Impression-Improvement (CGI-I)
NCT00367835 (11) [back to overview]	Assessment of Clinical Global Impression-Severity of Illness (CGI-S)
NCT00367835 (11) [back to overview]	Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale (ADHD-RS-IV) Total Score at Up to 8 Weeks
NCT00367835 (11) [back to overview]	Number of Participants With Overall Satisfaction on the Medication Satisfaction Survey (MSS)
NCT00429273 (1) [back to overview]	ADHD IV Rating Scale (Attention Deficit Hyperactivity Disorder Rating Scale)
NCT00613015 (2) [back to overview]	Cocaine Craving
NCT00613015 (2) [back to overview]	Cortisol- 2:30 pm, Immediately Following Trier Social Stress Task + Cocaine Cue Exposure
NCT00672984 (14) [back to overview]	Change From Baseline in Electrocardiogram Results (QTcF) at Tmax on Day 6
NCT00672984 (14) [back to overview]	Change From Baseline in Heart Rate (HR) at Tmax on Day 6
NCT00672984 (14) [back to overview]	Area Under the Steady-state Plasma Concentration-time Curve (AUC) for Guanfacine and Moxifloxacin on Day 6
NCT00672984 (14) [back to overview]	Change From Baseline in Electrocardiogram Results (QT) Interval at Tmax on Day 1
NCT00672984 (14) [back to overview]	Change From Baseline in Electrocardiogram Results (QT) Interval at Tmax on Day 6
NCT00672984 (14) [back to overview]	Change From Baseline in Electrocardiogram Results (QTcF) at Tmax on Day 1
NCT00672984 (14) [back to overview]	Change From Baseline in Electrocardiogram Results (QTcNi) at Time of Maximum Plasma Concentration (Tmax) on Day 1
NCT00672984 (14) [back to overview]	Change From Baseline in Electrocardiogram Results (QTcNi) at Tmax on Day 6
NCT00672984 (14) [back to overview]	Change From Baseline in Heart Rate (HR) at Tmax on Day 1
NCT00672984 (14) [back to overview]	Maximum Plasma Concentration (Cmax) of Guanfacine and Moxifloxacin on Day 1
NCT00672984 (14) [back to overview]	Maximum Plasma Concentration (Cmax) of Guanfacine and Moxifloxacin on Day 6
NCT00672984 (14) [back to overview]	Time of Maximum Plasma Concentration (Tmax) of Guanfacine and Moxifloxacin on Day 1
NCT00672984 (14) [back to overview]	Time of Maximum Plasma Concentration (Tmax) of Guanfacine and Moxifloxacin on Day 6
NCT00672984 (14) [back to overview]	Area Under the Steady-state Plasma Concentration-time Curve (AUC) for Guanfacine and Moxifloxacin on Day 1
NCT00734578 (9) [back to overview]	Assessment of Clinical Global Impression-Severity of Illness (CGI-S) at Week 8 - LOCF
NCT00734578 (9) [back to overview]	Percentage of Participants With Improvement on Parent Global Assessment (PGA) at Week 8 - LOCF
NCT00734578 (9) [back to overview]	Percentage of Participants With Improvement on Clinical Global Impression-Improvement (CGI-I) at Week 8 - LOCF
NCT00734578 (9) [back to overview]	Change From Baseline in Before School Functioning Questionnaire (BSFQ) at Week 8 - LOCF
NCT00734578 (9) [back to overview]	Change From Baseline in Conners' Global Index - Parent (CGI-P) Total Score at Week 8 - LOCF: Morning Assessment (Before School)
NCT00734578 (9) [back to overview]	Change From Baseline in Conners' Global Index - Parent (CGI-P) Total Score at Week 8 - LOCF: Evening Assessment (Before Bedtime)
NCT00734578 (9) [back to overview]	Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale-fourth Edition (ADHD-RS-IV) Total Score at Week 8 - Last Observation Carried Forward (LOCF)
NCT00734578 (9) [back to overview]	Change From Baseline in the Oppositional Subscale of the Conners' Parent Rating Scale-Revised Long Form (CPRS-R:L) Score at Week 8 - LOCF
NCT00734578 (9) [back to overview]	Post Sleep Questionnaire (PSQ) Quality of Sleep at Week 8 - LOCF
NCT00773357 (1) [back to overview]	Latency to Initiate Ad-lib Smoking Session
NCT00919867 (8) [back to overview]	Time of Maximum Plasma Concentration (Tmax) of Guanfacine
NCT00919867 (8) [back to overview]	T 1/2 of d-Amphetamine
NCT00919867 (8) [back to overview]	Maximum Plasma Concentration (Cmax) of Guanfacine
NCT00919867 (8) [back to overview]	Cmax of d-Amphetamine
NCT00919867 (8) [back to overview]	AUC of d-Amphetamine
NCT00919867 (8) [back to overview]	Tmax of d-Amphetamine
NCT00919867 (8) [back to overview]	Time of Plasma Half-Life(T 1/2) of Guanfacine
NCT00919867 (8) [back to overview]	Area Under the Steady-state Plasma Concentration-time Curve (AUC) of Guanfacine
NCT00935493 (3) [back to overview]	Quality of Life (SF-36 MCS)
NCT00935493 (3) [back to overview]	Alzheimer's Disease Cooperative Study-Clinical Global Impression of Change (ADCS-CGIC)
NCT00935493 (3) [back to overview]	Mean in the Prefrontal Executive Function Z-score (PEF6_6)
NCT00955253 (1) [back to overview]	Performance on Tests of Hemispatial Neglect and Sustained Attention
NCT00997984 (15) [back to overview]	Change From Baseline in Weight at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Improvement on Clinical Global Impression-Improvement (CGI-I) Scale at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Assessment of Clinical Global Impression-Severity of Illness (CGI-S) at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Change From Baseline in Diastolic Blood Pressure at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Change From Baseline in Pulse Rate at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Change From Baseline in Systolic Blood Pressure at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Post Sleep Questionnaire (PSQ) Quality of Sleep at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Change From Baseline in Pediatric Daytime Sleepiness Scale (PDSS) Total Score at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Change From Baseline in Attention-Deficit/Hyperactivity Disorder-Rating Scale-IV (ADHD-RS-IV) Total Score at Week 8 - Last Observation Carried Forward (LOCF)
NCT00997984 (15) [back to overview]	Change From Baseline in Conner's Parent Rating Scale - Revised Short Version (CPRS-R:S) Score at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Change From Baseline in Health Utilities Index-2/3 (HUI 2/3) Scores at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Change From Baseline in Height at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Change From Baseline in Mean Weiss Functional Impairment Rating Scale - Parent Report (WFIRS-P) Global Score at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Change From Baseline in Oral Temperature at Week 8 - LOCF
NCT00997984 (15) [back to overview]	Change From Baseline in the Bedtime Resistance Subscale of Child's Sleep Habits Questionnaire (CSHQ) at Week 8 - LOCF
NCT01069523 (2) [back to overview]	Clinical Global Impression- Improvement
NCT01069523 (2) [back to overview]	Dupaul ADHD Rating Scale
NCT01081132 (17) [back to overview]	Percent of Subjects With Improvement on Clinical Global Impression-Improvement (CGI-I) Scores at the Last On-Treatment Assessment
NCT01081132 (17) [back to overview]	Changes From Baseline in Behavior Rating Inventory of Executive Function (BRIEF) Scores at Week 13
NCT01081132 (17) [back to overview]	Columbia-Suicide Severity Rating Scale (C-SSRS)
NCT01081132 (17) [back to overview]	Structure Side-Effect Questionnaire (SSEQ)
NCT01081132 (17) [back to overview]	Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale-fourth Edition (ADHD-RS-IV) Total Score at Week 13
NCT01081132 (17) [back to overview]	Change From Baseline in Pediatric Daytime Sleepiness Scale (PDSS) Total Score at Week 13
NCT01081132 (17) [back to overview]	Change From Baseline in Brief Psychiatric Rating Scale for Children (BPRS-C) Total Score at Last On-Treatment Assessment
NCT01081132 (17) [back to overview]	Change From Baseline in the Weiss Functional Impairment Rating Scale - Parent Report (WFIRS-P) Learning and School Domain Scores at Week 13
NCT01081132 (17) [back to overview]	Change From Baseline in the WFIRS-P Academic Performance Domain Score at Week 13
NCT01081132 (17) [back to overview]	Change From Baseline in the WFIRS-P Behavior in School Domain Score at Week 13
NCT01081132 (17) [back to overview]	Change From Baseline in the WFIRS-P Child Self-Concept Domain Score at Week 13
NCT01081132 (17) [back to overview]	Change From Baseline in the WFIRS-P Global Domain Score at Week 13
NCT01081132 (17) [back to overview]	Change From Baseline in the WFIRS-P Family Domain Score at Week 13
NCT01081132 (17) [back to overview]	Change From Baseline in the WFIRS-P Life Skills Domain Score at Week 13
NCT01081132 (17) [back to overview]	Change From Baseline in the WFIRS-P Risk Domain Score at Week 13
NCT01081132 (17) [back to overview]	Change From Baseline in the WFIRS-P Social Domain Score at Week 13
NCT01081132 (17) [back to overview]	Percent of Subjects With an Assessment of Normal/Borderline Mentally Ill on Clinical Global Impression-Severity of Illness (CGI-S) Scale at the Last On-Treatment Assessment
NCT01081145 (14) [back to overview]	Health Utilities Index-2/3 (HUI 2/3) Scores During the Double-Blind Randomized-Withdrawal Phase - LOCF
NCT01081145 (14) [back to overview]	Change From Double-Blind Randomized-Withdrawal Baseline in the Weiss Functional Impairment Rating Scale - Parent Report (WFIRS-P) Global Score at Week 26 of the Double-Blind Randomized-Withdrawal Phase - LOCF
NCT01081145 (14) [back to overview]	Change From Double-Blind Randomized-Withdrawal Baseline in Attention Deficit Hyperactivity Disorder Rating Scale-fourth Edition (ADHD-RS-IV) Total Score at Week 26 of the Double-Blind Randomized-Withdrawal Phase - Last Observation Carried Forward (LOCF)
NCT01081145 (14) [back to overview]	Columbia-Suicide Severity Rating Scale During Double-Blind Randomized-Withdrawal Phase
NCT01081145 (14) [back to overview]	Change From Open-Label Baseline in WFIRS-P Global Score at Week 13 of the Open-Label Phase - LOCF
NCT01081145 (14) [back to overview]	Time to Treatment Failure During the Double-Blind Randomized-Withdrawal Phase
NCT01081145 (14) [back to overview]	Percentage of Responders in the Open-Label Phase - LOCF
NCT01081145 (14) [back to overview]	Percentage of Participants With Treatment Failures During the Double-Blind Randomized-Withdrawal Phase
NCT01081145 (14) [back to overview]	Columbia-Suicide Severity Rating Scale During Open-Label Phase
NCT01081145 (14) [back to overview]	Percent of Subjects With Improvement on Clinical Global Impression-Improvement (CGI-I) Scores During Open-Label Phase - LOCF
NCT01081145 (14) [back to overview]	Percent of Subjects With an Assessment of Normal/Borderline Mentally Ill on Clinical Global Impression-Severity of Illness (CGI-S) Scale During the Double-Blind Randomized-Withdrawal Phase - LOCF
NCT01081145 (14) [back to overview]	Change From Open-Label Baseline in ADHD-RS-IV Total Score at Week 13 of the Open-Label Phase - LOCF
NCT01081145 (14) [back to overview]	Percent of Subjects With an Assessment of Normal/Borderline Mentally Ill on CGI-S Scale During the Open-Label Phase - LOCF
NCT01081145 (14) [back to overview]	HUI 2/3 Scores During the Open-Label Phase - LOCF
NCT01133847 (11) [back to overview]	Wechsler Individual Achievement Test-III (WIAT-III) Reading Comprehension Subtest
NCT01133847 (11) [back to overview]	Wechsler Individual Achievement Test-III (WIAT-III) Pseudoword Decoding Subtest
NCT01133847 (11) [back to overview]	Wechsler Individual Achievement Test-III (WIAT-III) Word Reading Subtest
NCT01133847 (11) [back to overview]	Test of Silent Reading Fluency and Comprehension (TOSREC)
NCT01133847 (11) [back to overview]	Swanson, Nolan, and Pelham Checklist for DSM-IV (SNAP)- Parent Rating of Hyperactivity-impulsivity
NCT01133847 (11) [back to overview]	Test of Word Reading Efficiency (TOWRE) - Sight Word Efficiency
NCT01133847 (11) [back to overview]	Swanson, Nolan, and Pelham Checklist for DSM-IV (SNAP)- Parent Rating of Inattention
NCT01133847 (11) [back to overview]	Swanson, Nolan, and Pelham Checklist for DSM-IV (SNAP)- Teacher Rating of Hyperactivity-impulsivity
NCT01133847 (11) [back to overview]	Swanson, Nolan, and Pelham Checklist for DSM-IV (SNAP)- Teacher Rating of Inattention
NCT01133847 (11) [back to overview]	Test of Word Reading Efficiency (TOWRE) - Phonemic Decoding Efficiency
NCT01133847 (11) [back to overview]	Dynamic Indicators of Basic Early Literacy Skills Oral Reading Fluency Subtest (DIBELS ORF)
NCT01156051 (4) [back to overview]	Change in Baseline to Treatment ADHD-Rating Scale IV Total Score
NCT01156051 (4) [back to overview]	Change in Baseline to Treatment Latency to Persistent Sleep (LPS)
NCT01156051 (4) [back to overview]	Change in Baseline to Treatment Minutes of Wake Time After Sleep Onset (WASO)
NCT01156051 (4) [back to overview]	Change in Polysomnographic Total Sleep Time (TST)
NCT01238575 (16) [back to overview]	ADHD Rating Scale - Inattention Subscale
NCT01238575 (16) [back to overview]	ADHD Rating Scale - Total
NCT01238575 (16) [back to overview]	ADHD Rating Scale - Total
NCT01238575 (16) [back to overview]	Aberrant Behavior Checklist Sterotypy Subscale
NCT01238575 (16) [back to overview]	Aberrant Behavior Checklist Sterotypy Subscale
NCT01238575 (16) [back to overview]	Aberrant Behavior Checklist Social Withdrawal Subscale
NCT01238575 (16) [back to overview]	Aberrant Behavior Checklist Social Withdrawal Subscale
NCT01238575 (16) [back to overview]	Aberrant Behavior Checklist Irritability Subscale
NCT01238575 (16) [back to overview]	ADHD Rating Scale - Inattention Subscale
NCT01238575 (16) [back to overview]	Aberrant Behavior Checklist Hyperactivity Subscale
NCT01238575 (16) [back to overview]	Aberrant Behavior Checklist Hyperactivity Subscale
NCT01238575 (16) [back to overview]	Aberrant Behavior Checklist Inappropriate Speech Subscale
NCT01238575 (16) [back to overview]	Aberrant Behavior Checklist Inappropriate Speech Subscale
NCT01238575 (16) [back to overview]	Aberrant Behavior Checklist Irritability Subscale
NCT01238575 (16) [back to overview]	ADHD Rating Scale - Hyperactivity Subscale
NCT01238575 (16) [back to overview]	ADHD Rating Scale - Hyperactivity Subscale
NCT01244490 (16) [back to overview]	Change From Baseline in the Weiss Functional Impairment Rating Scale - Parent Report (WFIRS-P) Learning and School Domain Scores at Week 10/13 - LOCF
NCT01244490 (16) [back to overview]	Change From Baseline in the WFIRS-P Academic Performance Domain Score at Week 10/13 - LOCF
NCT01244490 (16) [back to overview]	Change From Baseline in the WFIRS-P Behavior in School Domain Score at Week 10/13 - LOCF
NCT01244490 (16) [back to overview]	Change From Baseline in the WFIRS-P Child Self-Concept Domain Score at Week 10/13 - LOCF
NCT01244490 (16) [back to overview]	Change From Baseline in the WFIRS-P Family Domain Score at Week 10/13 - LOCF
NCT01244490 (16) [back to overview]	Change From Baseline in the WFIRS-P Global Score at Week 10/13 - LOCF
NCT01244490 (16) [back to overview]	Change From Baseline in the WFIRS-P Life Skills Domain Score at Week 10/13 - LOCF
NCT01244490 (16) [back to overview]	Change From Baseline in the WFIRS-P Risk Domain Score at Week 10/13 - LOCF
NCT01244490 (16) [back to overview]	Change From Baseline in the WFIRS-P Social Domain Score at Week 10/13 - LOCF
NCT01244490 (16) [back to overview]	Health Utilities Index-2/3 (HUI 2/3) Scores - LOCF
NCT01244490 (16) [back to overview]	Percentage of Participants With Improvement on Clinical Global Impression-Improvement (CGI-I) Scores
NCT01244490 (16) [back to overview]	Clinical Global Impression-Severity of Illness (CGI-S) - LOCF
NCT01244490 (16) [back to overview]	Columbia-Suicide Severity Rating Scale (C-SSRS)
NCT01244490 (16) [back to overview]	Structure Side-Effect Questionnaire
NCT01244490 (16) [back to overview]	Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale-fourth Edition (ADHD-RS-IV) Total Score at Week 10/13 - Last Observation Carried Forward (LOCF)
NCT01244490 (16) [back to overview]	Change From Baseline in Brief Psychiatric Rating Scale for Children (BPRS-C) Total Score at Weeks 10/13 - LOCF
NCT01467999 (1) [back to overview]	Reduction in Mean Number of Days of Cannabis Use Per Week
NCT01470469 (7) [back to overview]	Change From Baseline in ECG QTcF Interval at up to 12 Weeks
NCT01470469 (7) [back to overview]	Change From Baseline in Electrocardiogram (ECG) QRS Interval at up to 12 Weeks
NCT01470469 (7) [back to overview]	Change From Baseline in Height at up to 12 Weeks
NCT01470469 (7) [back to overview]	Change From Baseline in Pulse Rate at Up to 12 Weeks
NCT01470469 (7) [back to overview]	Change From Baseline in Weight at up to 12 Weeks
NCT01470469 (7) [back to overview]	Change From Baseline in Systolic Blood Pressure at Up to 12 Weeks
NCT01470469 (7) [back to overview]	Change From Baseline in Diastolic Blood Pressure at Up to 12 Weeks
NCT01500694 (10) [back to overview]	Change From Baseline in Mean Height at Final Assessment
NCT01500694 (10) [back to overview]	Change From Baseline in Mean Weight at Final Assessment
NCT01500694 (10) [back to overview]	Change From Baseline in Mean Systolic Blood Pressure at Final Assessment
NCT01500694 (10) [back to overview]	Change From Baseline in Mean Supine Pulse at Final Assessment
NCT01500694 (10) [back to overview]	Change From Baseline in Mean Diastolic Blood Pressure at Final Assessment
NCT01500694 (10) [back to overview]	Change From Baseline in Electrocardiogram Result (QT Interval) at Final Assessment
NCT01500694 (10) [back to overview]	Number of Participants Assessed With Clinical Global Impression Severity of Illness (CGI-S) Scale
NCT01500694 (10) [back to overview]	Change From Baseline in Attention-deficit and Hyperactivity Disorder Rating Scale-IV (ADHD-RS-IV) - Total Score at Final Assessment
NCT01500694 (10) [back to overview]	"Number of Participants With Suicidal Behavior and / or Ideation (Yes Response) on the Columbia Suicide Severity Rating Scale (C-SSRS)"
NCT01500694 (10) [back to overview]	Change From Baseline in Electrocardiogram Result (QRS Interval) at Final Assessment
NCT01547000 (1) [back to overview]	Yale Global Tic Severity Scale (YGTSS)
NCT01600885 (3) [back to overview]	Percent Change in Amelioration of Ketamine-related Task Activation as Measured by Functional Magnetic Resonance Imaging in Superior Frontal Gyrus
NCT01600885 (3) [back to overview]	Percent Change in Amelioration of Ketamine-related Task Activation as Measured by Functional Magnetic Resonance Imaging in Inferior Parietal Lobule
NCT01600885 (3) [back to overview]	Percent Change in Amelioration of Ketamine-related Task Activation as Measured by Functional Magnetic Resonance Imaging in Middle Frontal Gyrus
NCT01709695 (9) [back to overview]	Go/No-go Task Performance Correct Inhibitions
NCT01709695 (9) [back to overview]	Go/No-go Task Performance Correct Responses
NCT01709695 (9) [back to overview]	Go/No-go Task Reaction Time
NCT01709695 (9) [back to overview]	Digit Span
NCT01709695 (9) [back to overview]	Attention Deficit Hyperactivity Disorder Rating Scale IV (ADHDRS IV)
NCT01709695 (9) [back to overview]	Percentage Change in Atomoxetine Stimulant Side Effects Rating Scale (ASSERS)
NCT01709695 (9) [back to overview]	Continuous Performance Test - Commissions
NCT01709695 (9) [back to overview]	Clinical Global Impressions (CGI-I)
NCT01709695 (9) [back to overview]	Finger Windows
NCT01904526 (3) [back to overview]	Plasma Trough Levels of Guanfacine
NCT01904526 (3) [back to overview]	Heart Rate
NCT01904526 (3) [back to overview]	Systolic Blood Pressure
NCT01985581 (7) [back to overview]	Effect of Adjunct Therapy on ADHD Symptom Control as Assessed by the Change in the ADHD Rating Scale (ADHD-RS-IV)
NCT01985581 (7) [back to overview]	Effect of Adjunct Therapy on ADHD Symptom Control as Assessed by the Change on the Clinical Global Impression of Severity (CGI-S) Scale
NCT01985581 (7) [back to overview]	Effect of Adjunctive INTUNIV Extended Release Treatment on Executive Function as Assessed by Change From Baseline on the BRIEF-parent Questionnaires
NCT01985581 (7) [back to overview]	Evaluate the Effect of Adjunct Therapy on ADHD Symptom Control as Assessed by the Change in Clinical Global Impression of Improvement (CGI-I) Scale
NCT01985581 (7) [back to overview]	Evaluate the Effect of Adjunctive INTUNIV Extended Release Treatment on Change in Quality of Life as Assessed by the KINDL®-Parent Questionnaire.
NCT01985581 (7) [back to overview]	Subjects Experiencing Suicidal Ideation, Suicidal Behaviour and Self-injurious Behaviour Without Suicidal Intent and Incident of Serious Adverse Events in Each Treatment Arm
NCT01985581 (7) [back to overview]	Effect of Adjunctive INTUNIV Extended Release Treatment on Change in Quality of Life as Assessed by the KINDL®-Child Questionnaire.
NCT02048241 (1) [back to overview]	Number of Participants That Were Responders
NCT02051309 (1) [back to overview]	Rates of Prolonged Smoking Abstinence
NCT02164422 (1) [back to overview]	mL Per 15 Minutes
NCT02259517 (1) [back to overview]	Changes in Brain Segmentation Volume Produced by Stimulant or Non-stimulant Medications in Patients With ADHD
NCT02699125 (2) [back to overview]	Brachial Artery Flow Mediated Dilation
NCT02699125 (2) [back to overview]	24-h, Wake and Sleep Period Systolic and Diastolic Blood Pressure
NCT02882854 (5) [back to overview]	Postoperative Nausea Assessment Using 11-point Nausea Scale (nVRS)
NCT02882854 (5) [back to overview]	Postoperative Pain Assessment Using 11-point Visual/Verbal Analog (VAS)
NCT02882854 (5) [back to overview]	Total Narcotic Requirement in PACU
NCT02882854 (5) [back to overview]	Maximum Postoperative Pain Assessment Using 11-point Visual/Verbal Analog (VAS)
NCT02882854 (5) [back to overview]	PACU Length of Stay in Minutes

Change From Baseline in Choice Reaction Time (CRT) at 6 Weeks

Choice reaction time (CRT) is a computerized assessment that trains the subject in holding down a press-pad and releasing the press-pad in response to stimuli presented on the screen. The task requires the subject to react as soon as a yellow dot appears in one of five locations, and the subject must respond by lifting their hand from the press-pad. This is the reaction time (RT) and ranges from 100 to 5000 msec. Lower scores indicate better performance. (NCT00150592)
Timeframe: Baseline and 6 weeks

Intervention	msec (Mean)
SPD503	20.7
Placebo	21.9

Intervention	Units on a scale (Mean)
	Between errors	Within errors	Double errors	Strategy
Placebo	-3.2	-0.1	0.1	-0.1
SPD503	-4.4	0.0	-0.0	-0.9

Intervention	Units on a Scale (Least Squares Mean)
SPD503 (1 mg)	-19.44
SPD503 (2 mg)	-18.09
SPD503 (3 mg)	-20.00
SPD503 (4 mg)	-20.57
Placebo	-12.69

Intervention	Units on a Scale (Least Squares Mean)
SPD503 (1 mg)	-19.50
SPD503 (2 mg)	-14.96
SPD503 (3 mg)	-17.94
SPD503 (4 mg)	-15.93
Placebo	-8.41

Intervention	units on a scale (Least Squares Mean)
	Physical	Psychosocial
Placebo	-0.01	6.34
SPD503 (1 mg)	0.32	10.61
SPD503 (2 mg)	0.35	7.47
SPD503 (3 mg)	-0.91	9.07
SPD503 (4 mg)	-2.44	9.43

Intervention	Units on a scale (Mean)
	Physical Summary Score	Psychosocial Summary Score
Amphetamine + SPD503	0.22	11.56
Methylphenidate + SPD503	-0.38	8.98

Intervention	Units on a Scale (Least Squares Mean)
SPD503 2mg	-15.93
SPD503 3mg	-16.03
SPD503 4mg	-18.51
Placebo	-8.51

Intervention	Units on a Scale (Least Squares Mean)
SPD503 2mg	-15.59
SPD503 3mg	-15.43
SPD503 4mg	-21.49
Placebo	-8.66

Intervention	Units on a Scale (Least Squares Mean)
SPD503 2mg	-13.02
SPD503 3mg	-14.88
SPD503 4mg	-15.26
Placebo	-2.17

Intervention	Participants (Number)
	1 (Normal, not at all ill)	2 (Borderline mentally ill)	3 (Mildly ill)	4 (Moderately ill)	5 (Markedly ill)	6 (Severely ill)	7 (Among the most extremely ill)
Placebo	3	6	15	24	22	5	0
SPD503	25	33	29	26	13	4	0

Intervention	units on a scale (Least Squares Mean)
	Total ADHD-RS Score	Inattentive Subscale	Hyperactive Impulsive Subscale
Estimated Difference Between DMPH and Placebo	-7.99	-4.10	-4.0
Estimated Difference Between Guan and Placebo	-7.77	-4.14	-3.73
Estimated Difference Between Placebo and Combo	-10.66	-5.89	-5.10

Intervention	units on a scale (Mean)
Modafinil/Stress	3.08
Modafinil/No Stress	4.36
Guanfacine/Stress	1.54
Guanfacine/No Stress	3.13
Placebo/Stress	1.8
Placebo/No Stress	2.11

Intervention	mcg/dl (Mean)
Modafinil/Stress	12.55
Modafinil/No Stress	11.69
Guanfacine/Stress	13.19
Guanfacine/No Stress	9.06
Placebo/Stress	12.42
Placebo/No Stress	8.94

Intervention	msec (Least Squares Mean)
Guanfacine 8 mg	-2.67
Moxifloxacin	6.44
Placebo (Guanfacine)	-4.31
Placebo (Moxifloxacin)	-4.35

Intervention	bpm (Least Squares Mean)
Guanfacine 8 mg	-19.74
Moxifloxacin	4.66
Placebo (Guanfacine)	0.11
Placebo (Moxifloxacin)	1.22

Intervention	msec (Least Squares Mean)
Guanfacine 4 mg	15.88
Moxifloxacin	-1.27
Placebo (Guanfacine)	0.56
Placebo (Moxifloxacin)	-2.20

Intervention	msec (Least Squares Mean)
Guanfacine 8 mg	46.21
Moxifloxacin	-3.09
Placebo (Guanfacine)	-3.63
Placebo (Moxifloxacin)	-6.71

Intervention	msec (Least Squares Mean)
Guanfacine 4 mg	0.15
Moxifloxacin	9.96
Placebo (Guanfacine)	-0.83
Placebo (Moxifloxacin)	-1.14

Intervention	msec (Least Squares Mean)
Guanfacine 4 mg	-3.37
Moxifloxacin	12.96
Placebo (Guanfacine)	-0.94
Placebo (Moxifloxacin)	-0.91

Intervention	msec (Least Squares Mean)
Guanfacine 8 mg	-12.45
Moxifloxacin	8.99
Placebo (Guanfacine)	-4.37
Placebo (Moxifloxacin)	-4.13

Intervention	bpm (Least Squares Mean)
Guanfacine 4 mg	-7.18
Moxifloxacin	5.46
Placebo (Guanfacine)	-0.42
Placebo (Moxifloxacin)	0.73

guanfacine

Description

Cross-References

Synonyms (87)

Research Excerpts

Overview

Effects

Treatment

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (46)

Potency Measurements

Inhibition Measurements

Other Measurements

Biological Processes (166)

Molecular Functions (57)

Ceullar Components (47)

Bioassays (75)

Research

Studies (738)

Market Indicators

Research Demand Index: 117.80

Study Types

Clinical Trials (75)

Trial Overview

Trial Outcomes

Change From Baseline in Choice Reaction Time (CRT) at 6 Weeks

Change From Baseline in Digital Symbol Substitution Task/Coding Test (DSST/Coding) Scores at 6 Weeks in Age Category 8-17 Years

Change From Baseline in DSST/Coding Scores at 6 Weeks in Age Category 6-7 Years

Change From Baseline in Pediatric Daytime Sleepiness Scale (PDSS) Scores at 6 Weeks

Change From Baseline in Pictorial Sleepiness Scale (PSS) Scores at 6 Weeks

Number of Participants With Improvement in Clinical Global Impression-Improvement (CGI-I) at 6 Weeks

Change From Baseline in Spatial Working Memory (SWM) Scores at 6 Weeks

Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale (ADHD-RS-IV) Total Score at 6 Weeks

Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale (ADHD-RS-IV) Score at 6 Weeks

Change From Baseline in Conner's Parent Rating Scale-revised Short Version (CPRS-R) Score at 6 Weeks

Number of Participants With Improvement in Clinical Global Impression-Improvement (CGI-I)

Number of Participants With Improvement in Parent Global Assessment (PGA)

Change From Baseline in Child Health Questionnaire-Parent Form (CHQ-PF50) Score at 6 Weeks

Number of Participants With Improvement on Clinical Global Impression-Improvement (CGI-I) Scores

Number of Participants With Improvement on Parent Global Assessment (PGA) Scores

Change From Baseline in Child Health Questionnaire-Parent Form (CHQ-PF50) Scores at 6 Weeks

Change From Baseline in Conner's Parent Rating Scale-revised Short Version (CPRS-R) Total Score at 6 Weeks

Change From Baseline in the Attention Deficit Hyperactivity Disorder Rating Scale (ADHD-RS-IV) Total Score at 6 Weeks

Number of Participants With Improvement in Parent Global Assessment (PGA)

Change From Baseline in Child Health Questionnaire-Parent Form (CHQ-PF50) Score at 5 Weeks

Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale (ADHD-RS-IV) Score at Up to 5 Weeks

Change From Baseline in Conner's Parent Rating Scale-revised Short Version (CPRS-R) Score at Up to 5 Weeks

Change From Baseline in Conner's Teacher Rating Scale-revised Short Version (CTRS-R) Score at Up to 5 Weeks

Number of Participants With Improvement in Clinical Global Impression-Improvement (CGI-I)

Change From Baseline in Diastolic Blood Pressure at Up to 8 Weeks

Change From Baseline in Electrocardiogram Results (QTcF Interval) at Up to 8 Weeks

Change From Baseline in Pulse Rate at Up to 8 Weeks

Change From Baseline in Systolic Blood Pressure at Up to 8 Weeks

Change From Baseline in the 40-Item Conduct Problem Scale of the New York Parent's Rating Scale-School-aged (NYPRS-S) Score at Up to 8 Weeks

Change From Baseline in the Oppositional Subscale of the Conners' Parent Rating Scale-Revised Long Form (CPRS-R:L) Score at Up to 8 Weeks

Change From Baseline in the Parent Stress Index-Short Form (PSI/SF) Score at Up to 8 Weeks

Number of Participants With Improvement on Clinical Global Impression-Improvement (CGI-I)

Assessment of Clinical Global Impression-Severity of Illness (CGI-S)

Change From Baseline in Attention Deficit Hyperactivity Disorder Rating Scale (ADHD-RS-IV) Total Score at Up to 8 Weeks

Number of Participants With Overall Satisfaction on the Medication Satisfaction Survey (MSS)

ADHD IV Rating Scale (Attention Deficit Hyperactivity Disorder Rating Scale)

Cocaine Craving

Cortisol- 2:30 pm, Immediately Following Trier Social Stress Task + Cocaine Cue Exposure

Change From Baseline in Electrocardiogram Results (QTcF) at Tmax on Day 6

Change From Baseline in Heart Rate (HR) at Tmax on Day 6

Area Under the Steady-state Plasma Concentration-time Curve (AUC) for Guanfacine and Moxifloxacin on Day 6

Change From Baseline in Electrocardiogram Results (QT) Interval at Tmax on Day 1

Change From Baseline in Electrocardiogram Results (QT) Interval at Tmax on Day 6

Change From Baseline in Electrocardiogram Results (QTcF) at Tmax on Day 1

Change From Baseline in Electrocardiogram Results (QTcNi) at Time of Maximum Plasma Concentration (Tmax) on Day 1

Change From Baseline in Electrocardiogram Results (QTcNi) at Tmax on Day 6

Change From Baseline in Heart Rate (HR) at Tmax on Day 1

Maximum Plasma Concentration (Cmax) of Guanfacine and Moxifloxacin on Day 1

Maximum Plasma Concentration (Cmax) of Guanfacine and Moxifloxacin on Day 6

Time of Maximum Plasma Concentration (Tmax) of Guanfacine and Moxifloxacin on Day 1

Intervention	Percent of participants (Number)
	Normal, not at all ill	Borderline mentally ill	Mildly ill	Moderately ill	Markedly ill	Severely ill	Most extremely ill
Placebo + Psychostimulant	15.1	17.8	28.9	27.0	9.2	2.0	0.0
SPD503-AM + Psychostimulant	22.8	19.5	34.2	16.1	6.0	1.3	0.0
SPD503-PM + Psychostimulant	25.0	26.4	26.4	16.2	5.4	0.7	0.0

Intervention	Percent of participants (Number)
SPD503-AM + Psychostimulant	69.8
SPD503-PM + Psychostimulant	67.7
Placebo + Psychostimulant	47.5

Intervention	Percent of participants (Number)
SPD503-AM + Psychostimulant	70.5
SPD503-PM + Psychostimulant	74.3
Placebo + Psychostimulant	57.9

Intervention	Units on a scale (Mean)
SPD503-AM + Psychostimulant	-16.7
SPD503-PM + Psychostimulant	-16.7
Placebo + Psychostimulant	-11.5

Intervention	Units on a scale (Mean)
SPD503-AM + Psychostimulant	-8.4
SPD503-PM + Psychostimulant	-9.6
Placebo + Psychostimulant	-6.9

Intervention	Units on a scale (Mean)
SPD503-AM + Psychostimulant	-8.2
SPD503-PM + Psychostimulant	-8.8
Placebo + Psychostimulant	-6.0

Intervention	Units on a scale (Mean)
SPD503-AM + Psychostimulant	-20.4
SPD503-PM + Psychostimulant	-21.0
Placebo + Psychostimulant	-16.0

Intervention	Units on a scale (Mean)
SPD503-AM + Psychostimulant	-6.6
SPD503-PM + Psychostimulant	-6.3
Placebo + Psychostimulant	-4.2

Intervention	Percent of participants (Number)
	Very poor	Poor	Average	Good	Very good
Placebo + Psychostimulant	0.0	3.3	33.3	40.5	22.9
SPD503-AM + Psychostimulant	0.7	6.7	26.8	40.3	25.5
SPD503-PM + Psychostimulant	0.7	6.8	29.7	41.2	21.6

Intervention	participants (Number)
	Worse	No Change	Improved
Guanfacine 0.1 mg	4	20	16
Guanfacine 0.5 mg	2	22	15
Placebo	3	25	12