D‐512, a novel dopamine D<sub>2/3</sub> receptor agonist, demonstrates greater anti‐Parkinsonian efficacy than ropinirole in Parkinsonian rats

Lindenbach, David; Das, Banibrata; Conti, Mary Anne; Meadows, Samantha M.; Dutta, Aloke K.; Bishop, Christopher

doi:10.1111/bph.13937

Cited by 23 publications

(11 citation statements)

References 53 publications

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“…Исследование на мышах с химически индуцированными фибромиалгическими симптомами, вызванными подкожным введением резерпина, позволило оценить эффективность препаратов СИОЗС вортиоксетина и АДР ропинирола на болевой порог, выраженность депрессии и тревоги, а также двигательные нарушения. Внутрибрюшинное введение вортиоксетина и ропинирола в дозе 10 мг/кг купировало тактильную аллодинию, при этом ропинирол проявлял свойства, подобные антидепрессантам, а вортиоксетинподобные анксиолитикам, что можно учитывать при определении ведущих симптомов болезни [21,22]. Интересен тот факт, что в другом исследовании у пациентов с ИКР часто в анамнезе был диагноз фибромиалгии, что вновь возвращает к мысли о возможной генетической предрасположенности к развитию такого симптомокомплекса на фоне врожденных особенностей нейромедиаторной передачи [23].…”

Section: терапия фибромиалгииunclassified

Dopamine receptor agonists: standard and non-standard applications in medicine

2022

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Dopamine receptor agonists (DRA) are a class of therapeutic drugs able to directly stimulate dopaminergic receptors facilitating a stronger effect of the endogenous dopamine, which is widely used in treatment of diseases that are accompanied with dopaminergic neurotransmission deficiency. A classical hypodopaminergic condition is Parkinson’s disease and DRA are traditionally associated with it. However, even the first DRA, Bromocriptine, widely adopted in PD treatment, was initially registered as a medication for treatment of prolactinaemia and associated pituitary adenomas and is still widely used in gynecology and endocrinology. In several countries DRA are used in treatment of diabetes, eating disorders, and addictions. Dopamine is the cardinal neurotransmitter of the emotional control and the main neurotransmitter of the reward system, and that defines the interest for researching the dopaminergic agents in treatment of primarily mental illnesses, as well as correction of secondary affective disorders. The experimental effectiveness of ADR in slowing down the rate of progression of the neurodegenerative process in severe incurable diseases, as well as potential neuroprotection in cerebrovascular insufficiency, will allow in the future to determine the criteria for the use of ADR in these non-standard situations, which may even lead to a change in clinical recommendations for the treatment of individual nosologies. Presented in this article are both traditional uses of DRA and an overview of non-standard applications of this class of medications with a discussion of recent studies. In the future, the likelihood of a rethinking of ADRs as a class of only antiparkinsonian drugs, with the expansion of their therapeutic indications.

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Section: терапия фибромиалгииunclassified

Dopamine receptor agonists: standard and non-standard applications in medicine

2022

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“…PD causes oxidative stress to damage brain tissue.D-512 has antioxidant properties [53].In an animal study, it was concluded that it carries a longer duration of action also helping in slowing disease progression. Also its antioxidant properties has a protective effect and decreases the oxidative stress in the brain [54].…”

Section: Antioxidant Propertiesmentioning

confidence: 99%

Parkinsonism and D-512, dopamine D2/3 receptor agonist; A review of literature

Waleed¹

2020

IJCCR

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In 1817, James Parkinson first coined the term Paralysis Agitans (An Essay on the Shaking Palsy), Jean-Marie Charcot was the first to coin term Parkinson’s disease (PD). Three most common and obvious symptoms in patients with PD are tremor, rigidity, and bradykinesia. A multidisciplinary team involving neurologists, primary care practitioners, nurses, physical therapists, social workers is used to diagnose PD. Nonpharmacological and pharmacological treatment is given to the patient. However, this disease demands more clinical translational and prognostic research, identifying biomarkers that can help in early diagnosis of the disease and on developing future disease-modifying interventions.

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“…Considering that D 3 -preferring agonists provide an additional neuroprotective effect compared with D 2 -preferring agonists [ 82 – 86 ], multifunctional agents with D 3 agonistic activity have been developed to not only alleviate motor dysfunction in PD patients but also delay disease progression by protecting DA neurons from progressive degeneration. The Dutta group initially developed novel multifunctional agents with D 2 /D 3 agonist activity along with antioxidant and iron chelating activities and the ability to modulate αSN aggregation, such as (−)-19 [ 87 ], D512 [ 88 – 91 ], D-520 [ 92 , 93 ], D593 [ 44 ], D-607 [ 94 , 95 ], D636 [ 96 ], D653 [ 96 ], and D656 (Table 4 ) [ 96 ]. Compared with ropinirole, (−)-19 , D-520, D-593, D607, D636, D653, D656, and (−)-21a all exhibit in vivo efficacy in significantly reversing akinesia in reserpine-induced PD rats for a longer duration and exhibit neuroprotective effects against various types of toxicity.…”

Section: Recent Advances In the Preclinical Study Of Dopaminergic Drumentioning

confidence: 99%

Recent advances in dopaminergic strategies for the treatment of Parkinson’s disease

et al. 2020

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s Parkinson’s disease (PD) is the second most common progressive neurodegenerative disease worldwide. However, there is no available therapy reversing the neurodegenerative process of PD. Based on the loss of dopamine or dopaminergic dysfunction in PD patients, most of the current therapies focus on symptomatic relief to improve patient quality of life. As dopamine replacement treatment remains the most effective symptomatic pharmacotherapy for PD, herein we provide an overview of the current pharmacotherapies, summarize the clinical development status of novel dopaminergic agents, and highlight the challenge and opportunity of emerging preclinical dopaminergic approaches aimed at managing the features and progression of PD.

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D‐512, a novel dopamine D_2/3 receptor agonist, demonstrates greater anti‐Parkinsonian efficacy than ropinirole in Parkinsonian rats

Abstract: Compared with ropinirole, D-512 showed greater peak-dose efficacy and a longer duration of action, despite a similar side-effect profile. Our results add to earlier data showing that D-512 is superior to available D agonists and could merit clinical investigation.

Cited by 23 publications

References 53 publications

Dopamine receptor agonists: standard and non-standard applications in medicine

Dopamine receptor agonists: standard and non-standard applications in medicine

Parkinsonism and D-512, dopamine D2/3 receptor agonist; A review of literature

Recent advances in dopaminergic strategies for the treatment of Parkinson’s disease

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D‐512, a novel dopamine D2/3 receptor agonist, demonstrates greater anti‐Parkinsonian efficacy than ropinirole in Parkinsonian rats

Abstract: Compared with ropinirole, D-512 showed greater peak-dose efficacy and a longer duration of action, despite a similar side-effect profile. Our results add to earlier data showing that D-512 is superior to available D agonists and could merit clinical investigation.

Cited by 23 publications

References 53 publications

Dopamine receptor agonists: standard and non-standard applications in medicine

Dopamine receptor agonists: standard and non-standard applications in medicine

Parkinsonism and D-512, dopamine D2/3 receptor agonist; A review of literature

Recent advances in dopaminergic strategies for the treatment of Parkinson’s disease

Contact Info

Product

Resources

About

D‐512, a novel dopamine D_2/3 receptor agonist, demonstrates greater anti‐Parkinsonian efficacy than ropinirole in Parkinsonian rats