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Art. -Nr.: HY-182091

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CYD-1-79

CYD-1-79 is a selective positive allosteric modulator of 5-HT2C receptor. CYD-1-79 potentiates 5-HT-evoked intracellular calcium release via a topographically distinct allosteric site. CYD-1-79 shows significant inhibition of binding at dopamine D3 receptor, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 modulates 5-HT2C receptor-mediated spontaneous ambulation in rodents and synergizes with a low dose of a 5-HT2C receptor agonist. CYD-1-79 attenuates relapse vulnerability of psychoactive substance in a rodent self-administration model. CYD-1-79 can be used for the research of neurological disease.

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CAS. Nr.: 2220235-94-7
Formel: C₂₀H₄₀N₂O₃
Molecular Weight:356.54

Speicherung:

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

CYD-1-79 Chemical Structure

CAS. Nr.: 2220235-94-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

5-HT_2C Receptor

D₃ Receptor

Alpha-2A adrenergic receptor

Alpha-2B adrenergic receptor

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Cellular Effect

Cell Line	Type	Value	Description	References
CHO	E_max	123.2 % Compound: 16	Positive allosteric modulation of human 5-HT2CR expressed in CHO cells assessed as 5-HT-induced intracellular calcium release at 1 nM preincubated for 15 mins followed by 5-HT addition by calcium-4 dye based FLIPR assay (Rvb = 100%) Positive allosteric modulation of human 5-HT2CR expressed in CHO cells assessed as 5-HT-induced intracellular calcium release at 1 nM preincubated for 15 mins followed by 5-HT addition by calcium-4 dye based FLIPR assay (Rvb = 100%)	[PMID: 29620897]
CHO	E_max	123.2 % Compound: 3; CYD-1-79	Positive allosteric modulation of human 5HT2CR expressed in CHO cells assessed as increase in 5-HT induced intracellular calcium release at 1 nM preincubated for 15 mins followed by 5-HT addition and measured at 1 secs interval for 360 secs by calcium 4 d Positive allosteric modulation of human 5HT2CR expressed in CHO cells assessed as increase in 5-HT induced intracellular calcium release at 1 nM preincubated for 15 mins followed by 5-HT addition and measured at 1 secs interval for 360 secs by calcium 4 d	[PMID: 32567857]

In Vitro

CYD-1-79 (Compound 16) (1 pM-1 μM; 15 min) promotes an upward shift of 5-HT-evoked Cai2+ release at multiple
concentrations without a leftward shift^[1].
CYD-1-79 (1 pM-1 μM; 15 min) does not modulate 5-HT₂A receptor-mediated intracellular calcium release in h5-HT₂A R-CHO cells, demonstrating subtype selectivity for 5-HT₂C receptors^[1].
CYD-1-79 (10 μM) does not significantly bind to orthosteric sites of 5-HT receptor subtypes, including 5-HT₂C, but shows significant inhibition of binding at dopamine D₃ receptor, DAT, and α₂A/α₂B adrenergic receptors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-inf	F	CL	V_ss
Rat^[1]	5 mg/kg	i.v.	6.59 ± 0.26 h	/	/	939 ± 108 ng·h/mL	/	5.37 ± 0.61 L/h/kg	35.07 ± 4.66 L/kg
Rat^[1]	10 mg/kg	p.o.	5.82 ± 0.37 h	3.3 ± 0.58 h	68.1 ± 6.8 ng/mL	737 ± 56 ng·h/mL	39.1 %	/	/

In Vivo

CYD-1-79 (Compound 16) (0.5-5 mg/kg; i.p.; single dose) significantly suppresses spontaneous ambulatory and vertical locomotor activity in male Sprague-Dawley rats within the first 30 minutes post-administration at the 5 mg/kg dose, while lower doses show no significant effects^[1].
CYD-1-79 (5 mg/kg; i.p.; single dose) allosterically potentiates the locomotor-suppressant effects of the 5-HT2C agonist WAY163909 (HY-15401) in male Sprague-Dawley rats, an effect mediated by 5-HT2C receptor activation^[1].
CYD-1-79 (0.125-1 mg/kg; i.p.; single dose) partially substitutes for the discriminative stimulus effects of the 5-HT2C agonist WAY163909 when administered alone, but synergizes with a low dose of WAY163909 (0.5 mg/kg) to produce full substitution for its discriminative stimulus effects in trained male Sprague-Dawley rats^[1].
CYD-1-79 (compound 16) (1 mg/kg; i.p.; single dose) significantly suppresses psychoactive substance cue reactivity in male Sprague-Dawley rats trained to self-administer psychoactive substance^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague-Dawley (male, 225-325 g)^[1]
Dosage:

0.5 mg/kg; 1 mg/kg; 5 mg/kg
Administration:

i.p.; single dose
Result:

Significantly reduced mean total ambulations and mean total vertical activity (±SEM) compared to saline at 5 mg/kg (p < 0.05).
Did not produce statistically significant changes in ambulations or vertical activity relative to saline at 0.5 mg/kg and 1 mg/kg.

Animal Model:

Sprague-Dawley (male, 250-275 g, trained to self-administer psychoactive substance)^[1]
Dosage:

1 mg/kg
Administration:

i.p.; single dose
Result:

Significantly reduced presses on the previously active lever during the 60-minute cue-reinforced component compared to vehicle (p < 0.05, with significant differences observed at multiple 5-minute time points).
Did not significantly alter inactive lever presses relative to vehicle.

Chemical Information

CAS. Nr. 2220235-94-7
Molecular Weight 356.54
Formel C₂₀H₄₀N₂O₃
SMILES

O=C([C@H]1NCC[C@@H](CCCCCCCCCCC)C1)NCC(O)CO
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Wild CT, et al. Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT_2C Receptor. J Med Chem. 2019;62(1):288-305. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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CYD-1-79

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

CYD-1-79 Related Classifications

HY-182091 Related Classifications