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| 1 | The Aggression Scale: A self-- report measure of aggressive behavior for young adolescenls 显示文摘 | Orpinas P and Frankowski R | 2001 | J Early Adolesc2001，21，1： | 1 |
| 2 | High-dose barbiturate control of elevated intracranial pressure in patients with severe head injury显示文摘 | Eisneberg H M Frankowski R F Contant C F | 1988 | J Neurosurg1988，69，1： | 1 |
| 3 | Outcome evaluation of a multi -component violence- prevention program for middle schools: the Students for Peace Project显示文摘 | Orpinas P Kelder S Frankowski R | 2000 | Health Educ Res2000，15，1： | 1 |
| 4 | A clinical prediction model for long - term functional outcome after traumatic spinal cord injury based on acute clinical and imaging factors 显示文摘 | WILSON J R GROSSMAN R G FRANKOWSKI R F | 2012 | J Neurotrauma2012，29，13： | 1 |
| 5 | Riluzole for the treatment of acute traumatic spinal cord injury:rationale for and design of the NACTN Phase I clinical trial显示文摘 | Michael G Fehlings Jefferson R Wilson Ralph F Frankowski | | 0，，： | 1 |
| 6 | Coupling en- doplasmie reticu|um stress to the cell death program:an apaf-1-independent intrinsic pathway显示文摘 | Rao R V Castro Obregon S Frankowski H | 2002 | J Biol Chem2002，277，21： | 1 |
| 7 | Evaluation of a pumping assist lung that uses a rotating fiber bundle显示文摘 | SVITEK R G FRANKOWSKI B J FEDERSPIEL W J | 2005 | ASAIO J2005，51，6： | 1 |
| 8 | Highdose barbiturate control of elevated intracranial pressure in patients with severe head injury显示文摘 | Eisenberg H M Frankowski R F Contant C F | 1988 | J Neurosurg1988，69，1： | 1 |
| 9 | Sense of coherence, nega: rive life events and appraisal of physical heakh among university stu- dents显示文摘 | Jorgensen R S Frankowski J J Carey M P | 1999 | Personality and Individual Differences1999，27，6： | 1 |
| 10 | PPARG F388L, a transactivation-deficient mutant, in familial'partial lipodystrophy显示文摘 | Hegele R A Cao H Frankowski C | 2002 | Diabetes2002，51，13： | 1 |
| 11 | Effect de quelques substance herbicides communes sur le champignon nematophage 'R350'显示文摘 | CAYOL J C R FRANKOWSKI J P | 1981 | P H M REV Hortic1981，219，： | 1 |
| 12 | Outcome evaluation of a multi-component violence-prevention program for middle schools:the Students for Peace project显示文摘 | Orpinas P Kelder S Frankowski R | 2000 | Health Educ Res2000，15，1： | 1 |
| 13 | The development and validation of a dysphagia-specific quality-of- life questionnaire for patients with head and neck cancer: the MD Adnerson dysphagia inventory 显示文摘 | Chen AY Frankowski R Bishop-Lenone J | 2001 | Arch Otolaryngol Head Neck Surg2001，127，7： | 1 |
| 14 | Surgical treatment for intracerebral hemorrhage(STICH): a single-center randomized clinical trial 显示文摘 | Morgenstern L B Frankowski R F Shedden P | 1998 | Neurology1998，51，7： | 1 |
| 15 | Incidence and severity of acute complications after spinal cord injury 显示文摘 | Grossman R G Frankowski R F Burau K D Toups E G Crommett J W Johnson M M | 2012 | J Neurosurg Spine2012，17，1： | 1 |
| 16 | Identification and optimization of a potent and highly selective D3 dopamine receptor agonist显示文摘OBJECTIVE Dopamine receptors(DRs) are involved in the development and treatment of many neuropsychiatric disorders.Currently available dopaminergic drugs modulate both DRD2 and DRD3,leading to side effects and uncertainty as to the roles each DR subtype plays physiologically.Our lab employed high throughput screening paradigms to discover highly selective modulators for the DRD3.METHODS The NIH Molecular Libraries Program 400,000 + small molecule library was screened using the Discove Rx Path Hunter?β-arrestin assay for compounds that activate the DRD3 without effects on the DRD2.Confirmation and counter-screens assessed selectivity and mechanisms of action.We identified 62 potential agonists,and chose the most promising to perform a structure-activity relationship(SAR) study to increase potency while maintaining selectivity.The lead compound identified through this process,ML417,was also characterized using bioluminescence resonance energy transfer(BRET)-based β-arrestin recruitment and G-protein activation assays as well as p-ERK assays.Potential neuroprotective properties of this compound were assessed using a SHSY5 Y neuronal cell model.RESULTS ML417 displays potent,DRD3-selective agonist activity in multiple functional assays.Binding and functional GPCR screens(>165 receptors) show ML417 has limited cross-reactivity with other GPCRs.ML417 also displays superior(compared to the reference compound pramipexole),dose-dependent protection against a decrease in neurite length induced by 10 μmol·L^(-1) of the neurotoxin,6-hydroxydopamine,in the SHSY5 Y cell model.CONCLUSION We have discovered and characterized ML417,a potent and highly selective DRD3 agonist.This compound will be useful as a research tool,and may prove useful as a therapeutic drug lead. | Amy E MORITZ R Benjamin FREE Warren WEINER Muzna BACHANI Trevor DOYLE Noel SOUTHALL Marc FERRER Jonathan A JAVITCH Joseph STEINER Ara ABRAMYAN Lei SHI Jeffrey AUBé Kevin FRANKOWSKI David R SIBLEY | 2017 | 中国药理学与毒理学杂志2017，31，10： | 0 |
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