1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor Dopamine Receptor
  3. D3/5-HT receptor modulator-1

D3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and 5-HT2A receptor antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile.

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D3/5-HT receptor modulator-1 Chemical Structure

D3/5-HT receptor modulator-1 Chemical Structure

CAS No. : 898532-85-9

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Based on 1 publication(s) in Google Scholar

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Description

D3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and 5-HT2A receptor antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile[1].

IC50 & Target[1]

D3 Receptor

4.5 nM (Ki)

5-HT1A Receptor

11.9 nM (Ki)

5-HT2A Receptor

15.3 nM (Ki)

5-HT2C Receptor

206 nM (Ki)

D2 Receptor

263 nM (Ki)

D1 Receptor

3290 nM (Ki)

hERG Channels

930 nM (Ki)

Molecular Weight

391.51

Formula

C24H29N3O2

CAS No.
SMILES

O=C(C1=CC2=CC=CC=C2O1)NCCCCN3CCN(C4=CC=CC(C)=C4)CC3

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (127.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5542 mL 12.7711 mL 25.5421 mL
5 mM 0.5108 mL 2.5542 mL 5.1084 mL
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Purity & Documentation
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Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5542 mL 12.7711 mL 25.5421 mL 63.8553 mL
5 mM 0.5108 mL 2.5542 mL 5.1084 mL 12.7711 mL
10 mM 0.2554 mL 1.2771 mL 2.5542 mL 6.3855 mL
15 mM 0.1703 mL 0.8514 mL 1.7028 mL 4.2570 mL
20 mM 0.1277 mL 0.6386 mL 1.2771 mL 3.1928 mL
25 mM 0.1022 mL 0.5108 mL 1.0217 mL 2.5542 mL
30 mM 0.0851 mL 0.4257 mL 0.8514 mL 2.1285 mL
40 mM 0.0639 mL 0.3193 mL 0.6386 mL 1.5964 mL
50 mM 0.0511 mL 0.2554 mL 0.5108 mL 1.2771 mL
60 mM 0.0426 mL 0.2129 mL 0.4257 mL 1.0643 mL
80 mM 0.0319 mL 0.1596 mL 0.3193 mL 0.7982 mL
100 mM 0.0255 mL 0.1277 mL 0.2554 mL 0.6386 mL
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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D3/5-HT receptor modulator-1
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HY-10861
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