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Referencia número: 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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No. CAS: 2220235-94-7
Fòrmula: C₂₀H₄₀N₂O₃
Peso molecular:356.54

Almacenamiento:

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

CYD-1-79 Chemical Structure

No. CAS: 2220235-94-7

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Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
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Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

5-HT_2C Receptor

D₃ Receptor

Alpha-2A adrenergic receptor

Alpha-2B adrenergic receptor

Ver todos los productos específicos de isoformas 5-HT Receptor :

Ver todos los productos específicos de isoformas Dopamine Receptor :

Ver todos los productos específicos de isoformas Adrenergic Receptor :

Ver todos los productos específicos de isoformas Calcium Channel :

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

No. CAS 2220235-94-7
Peso molecular 356.54
Fòrmula C₂₀H₄₀N₂O₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[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]

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CYD-1-79

Ver todos los productos específicos de isoformas 5-HT Receptor

Ver todos los productos específicos de isoformas Dopamine Receptor

Ver todos los productos específicos de isoformas Adrenergic Receptor

Ver todos los productos específicos de isoformas Calcium Channel

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CYD-1-79 Related Classifications

HY-182091 Related Classifications