A dopamine D2 receptor agonist; selective for D2 over D1

Sumanirole (maleate) – 10 mg

Brand:
Cayman
CAS:
179386-44-8
Storage:
-20
UN-No:
Non-Hazardous - /

Sumanirole is a dopamine D2 receptor agonist that is selective for D2 over D1, D3, and D4 receptors (Kis = 9.0, >7,140, 1,940, and >2,190 nM, respectively).{22059} It inhibits forskolin-stimulated cAMP accumulation in CHO cells expressing human recombinant D2A receptors (EC50 = 17 nM). Sumanirole decreases plasma prolactin levels in rats when administered at doses greater than or equal to 3.1 µmol/kg and inhibits dopamine neuron firing in the substantia nigra pars compacta (SNPC) in anesthetized rats (ED50 = 2.3 µmol/kg). Sumanirole (≥12.5 µmol/kg, s.c.) increases horizontal locomotor activity in a reserpinized, α-methyl-para-tyrosine (AMPT) rat model of Parkinson’s disease. It also decreases time spent in the open arms of the elevated plus maze and time spent immobile in the forced swim test, indicating anxiolytic- and antidepressant-like activities, respectively, in mice with SNPC lesions when administered at a dose of 0.1 mg/kg.{31907} Sumanirole (≥0.1 mg/kg, s.c.) reduces premature responding, a measure of impulsivity, by rats in the 5-choice serial reaction time test (5CRTT) compared with untreated animals.{39871}  

 

Available on backorder

Add to quotes
SKU: 11984 - 10 mg Category:

Description

A dopamine D2 receptor agonist; selective for D2 over D1, D3, and D4 receptors (Kis = 9.0, >7,140, 1,940, and >2,190 nM, respectively); inhibits forskolin-stimulated cAMP accumulation in CHO cells expressing human recombinant D2A receptors (EC50 = 17 nM); decreases plasma prolactin levels in rats at ≥3.1 µmol/kg; inhibits dopamine neuron firing in the SNPC in anesthetized rats (ED50 = 2.3 µmol/kg); increases horizontal locomotor activity in a reserpinized, AMPT rat model of Parkinson’s disease at ≥12.5 µmol/kg; decreases time spent in the open arms of the elevated plus maze and time spent immobile in the forced swim test in mice with SNPC lesions at 0.1 mg/kg; reduces premature responding by rats in the 5CRTT compared with untreated animals at ≥0.1 mg/kg,

Formal name: (5R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one, 2Z-butenedioate

Synonyms:  PNU 95666

Molecular weight: 319.3

CAS: 179386-44-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Behavioral Neuroscience|Depression||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

Related products

  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 5 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 250 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 250 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 25 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 25 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 50 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page