Rotigotine hydrochloride [Dopamine D2 Receptor; Dopamine D3 Receptor Agonist]
[CAT#: MOD2005ZP234]
Dopamine D2 and D3 receptor agonist
- Target:
- DRD2
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Lot Number
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Lot Number
Description
Rotigotine hydrochloride (N-0923 Hydrochloride) is a complete agonist of dopamine receptor, a partial agonist of 5-HT1A receptor and an antagonist of α2B-adrenergic receptor, Ki is 0.71 nM, 4-15 nM and 83 nM. Dopamine D3 receptor and D2, D5, D4 receptor and dopamine D1 receptor.
Synonyms
N 0923
Chemical Name
(6S)-5,6,7,8-Tetrahydro-6-[propyl[2 -(2-thienyl)ethyl]amino]-1-naphthalenol hydrochloride
Modulator Type
Agonist
Relevant Disease
Neurological Disorders
Assay Description
Rotigotine (N-0923) is 10 times more selective for D3 (pKi 9.2) receptors than D2, D4 and D5 (pKi 8.5-8.0), and 100% more selective for D1 receptors (pKi 7.2) Times. In functional studies, rotigotine (N-0923) is a complete agonist at all dopamine receptors, but it is worth noting that the stimulating ability of the D1 receptor is similar to the D2 and D3 receptors (pEC50 is 9.0, respectively), 9.4-8.6, 9.7) [1]. Rotigotine (N-0923) (10 µM) reduced the number of THir neurons in primary mesencephalic cell culture by 40%. Rotigotine (0.01 µM) can slightly protect dopaminergic neurons from MPP + toxicity, significantly protect dopaminergic neurons from rotenone-induced cell death, and significantly inhibit rotenone-induced ROS production [4].
Reference
[1]. Wood M, et al. Rotigotine is a potent agonist at dopamine D1 receptors as well as at dopamine D2 and D3 receptors. Br J Pharmacol. 2015 Feb;172(4):1124-35.
[2]. Scheller D, et al. The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):73-86.
[3]. Fenu S, et al. In vivo dopamine agonist properties of rotigotine: Role of D1 and D2 receptors. Eur J Pharmacol. 2016 Oct 5;788:183-91.
[4]. Radad K, et al. Neuroprotective effect of rotigotine against complex I inhibitors, MPP? and rotenone, in primary mesencephalic cell culture. Folia Neuropathol. 2014;52(2):179-86.
[2]. Scheller D, et al. The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):73-86.
[3]. Fenu S, et al. In vivo dopamine agonist properties of rotigotine: Role of D1 and D2 receptors. Eur J Pharmacol. 2016 Oct 5;788:183-91.
[4]. Radad K, et al. Neuroprotective effect of rotigotine against complex I inhibitors, MPP? and rotenone, in primary mesencephalic cell culture. Folia Neuropathol. 2014;52(2):179-86.
Assay Description
In sensitized rats, rotigotine (N-0923) (0.035, 0.1, and 0.35 mg/kg) induced contralateral turning behavior in a dose-dependent manner. In first-time drug-using rats, rotigotine alone or in combination with SCH 39166 reduced the turning behavior compared to the induced rats [1].
References
[1]. Fenu S, et al. In vivo dopamine agonist properties of rotigotine: Role of D1 and D2 receptors. Eur J Pharmacol. 2016 Oct 5;788:183-91.
Molecular Weight
351.93
Chemical Formula
C19H25NOS.HCl
SMILES
CCCN(CCC3=CC=CS3)[C@H]2CCC1=C(O)C=CC=C1C2.Cl
Solubility
Soluble in water (10mM) or DMSO (100mM)
IC50
Ki: 0.71 nM (dopamine D3 receptor), 4-15 nM (dopamine D2, D5, D4 receptors), 83 nM (dopamine D1 receptor)[1][2], 176 nM (α1A), 273 nM (α1B), 338 nM (α2A), 27 nM (α2B), 30 nM (5-HT1A), 86 nM (5-HT7)
CAS NO.
125572-93-2
PubChem Substance ID
59226
Purity
>98%
Shipping
Room Temperature
Research Use Only
For research use only
Target
DRD2
Official Name
DRD2
Alternative Names
The dopamine receptor D2, also known as D2R, is a protein encoded by the DRD2 gene in humans. The dopamine D2 receptor is the main receptor for most antipsychotic drugs. The structure of DRD2 combined with the atypical antipsychotic drug risperidone has been determined.
This gene encodes the D2 subtype of the dopamine receptor, which is coupled to the Gi subtype of the G protein-coupled receptor. This G protein-coupled receptor can inhibit the activity of adenylate cyclase.
In mice, the modulation and exploration of D2R surface expression by neurocalcium sensor 1 (NCS-1) in the dentate gyrus is related to synaptic plasticity and memory formation. A recent study showed that D2R has a potential role in restoring forearm cortical fear memory.
In Drosophila, activation of D2 autoreceptors protects dopamine neurons from MPP+-induced cell death, a toxin that mimics the pathology of Parkinson's disease.
This gene encodes the D2 subtype of the dopamine receptor, which is coupled to the Gi subtype of the G protein-coupled receptor. This G protein-coupled receptor can inhibit the activity of adenylate cyclase.
In mice, the modulation and exploration of D2R surface expression by neurocalcium sensor 1 (NCS-1) in the dentate gyrus is related to synaptic plasticity and memory formation. A recent study showed that D2R has a potential role in restoring forearm cortical fear memory.
In Drosophila, activation of D2 autoreceptors protects dopamine neurons from MPP+-induced cell death, a toxin that mimics the pathology of Parkinson's disease.
Biomaterials
Modulators
Neural Cell Lines
Neural Antibodies
Neural Assays
Neural Proteins & Peptides
For Research Use Only. Not For Clinical Use.
