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AB144611

Terguride, Partial D2 agonist

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(2 Publications)

MW 340.5 Da, Purity >98%. Partial D2 agonist. Potent, non-competitive and non-selective 5-HT2 antagonist. Shows antiparkinsonism and antidepressant effects in vivo. Blood-brain barrier permeable. Orally active.
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Chemical Structure - Terguride, Partial D2 agonist (AB144611)
  • Chemical Structure

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Chemical Structure - Terguride, Partial D2 agonist (AB144611)

2D chemical structure image of ab144611, Terguride, Partial D2 agonist

Key facts

CAS number

37686-84-3

Purity

>98%

Form

Solid

form

Molecular weight

340.5 Da

Molecular formula

C<sub>2</sub><sub>0</sub>H<sub>2</sub><sub>8</sub>N<sub>4</sub>O

PubChem

443951

Nature

Synthetic

Solubility

Soluble in DMSO

Soluble in ethanol

Biochemical name

Terguride

Biological description

Partial D2 agonist. Potent, non-competitive and non-selective 5-HT2 antagonist. Shows antiparkinsonism and antidepressant effects in vivo. Blood-brain barrier permeable. Orally active.

Canonical smiles

CCN(CC)C(=O)NC1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)C

Isomeric smiles

CCN(CC)C(=O)N[C@H]1C[C@H]2[C@@H](CC3=CNC4=CC=CC2=C34)N(C1)C

InChi

InChI=1S/C20H28N4O/c1-4-24(5-2)20(25)22-14-10-16-15-7-6-8-17-19(15)13(11-21-17)9-18(16)23(3)12-14/h6-8,11,14,16,18,21H,4-5,9-10,12H2,1-3H3,(H,22,25)/t14-,16+,18+/m0/s1

InChiKey

JOAHPSVPXZTVEP-YXJHDRRASA-N

IUPAC Name

3-[(6aR,9S,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]-1,1-diethylurea

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
Ambient
Appropriate long-term storage conditions
Ambient
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

The 5-HT2A receptor and dopamine D2 receptor are important in neurotransmission. The 5-HT2A receptor also termed serotonin receptor 2A is part of the G protein-coupled receptor family which is approximately 70 kDa in mass. It is predominantly expressed in the central nervous system especially in the cortex basal ganglia and limbic regions. The dopamine D2 receptor also widely distributed in the brain is important for modulating neurotransmitter release and synaptic plasticity. Like 5-HT2A the D2 receptor is also a G protein-coupled receptor and interacts significantly with dopamine neurotransmission.
Biological function summary

Neurotransmitter receptors like 5-HT2A and dopamine D2 are integral in signal transduction. These receptors do not function in isolation but form part of larger receptor complexes that influence many physiological processes. The 5-HT2A receptor modulates cognitive functions mood and hallucinations via serotonin signaling. The dopamine D2 receptor influences motor control and reward-related behavior. These receptors also display agonistic and antagonistic interactions— a partial D2 agonist or partial antagonist can modulate signaling pathways by fine-tuning receptor activity.

Pathways

Neurotransmitter receptors play roles in signal modulation pathways specifically the serotonin and dopamine systems. The 5-HT2A receptor participates in the phosphatidylinositol signaling pathway and interacts with proteins like PLC and PKC to modulate calcium release and neurite development. Meanwhile the dopamine D2 receptor is integral to the dopaminergic synapse pathway associating with adenylate cyclase and inhibiting cyclic AMP production. Both receptors converge in interacting with proteins that influence synapses and neurotransmitter release dynamics impacting numerous neural processes.

Alterations in 5-HT2A and dopamine D2 receptor function link to several neuropsychiatric conditions. Schizophrenia for example involves dysregulation of dopamine D2 receptor-linked signaling impacting brain regions associated with cognitive and emotional processing. Additionally they relate to depression where serotonin imbalance affects the 5-HT2A receptor's role in mood regulation. These receptor's interactions with other proteins such as those involved in stress response and signal regulation underline their influence in such disorders highlighting potential therapeutic targets for intervention.

Product protocols

Publications (2)

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Scientific reports 11:8288 PubMed33859231

2021

New phosphosite-specific antibodies to unravel the role of GRK phosphorylation in dopamine D receptor regulation and signaling.

Applications

Unspecified application

Species

Unspecified reactive species

Anika Mann,Alastair C Keen,Hanka Mark,Pooja Dasgupta,Jonathan A Javitch,Meritxell Canals,Stefan Schulz,J Robert Lane

Transplant immunology 49:43-53 PubMed29649585

2018

Effects of different serotonin receptor subtype antagonists on the development of cardiac allograft vasculopathy in murine aortic allografts.

Applications

Unspecified application

Species

Unspecified reactive species

Annika Gocht,Jörg H W Distler,Bernd Spriewald,Martina Ramsperger-Gleixner,Michael Weyand,Stephan M Ensminger,Christian Heim
View all publications

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