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製品番号: 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 番号: 2220235-94-7
分子式: C₂₀H₄₀N₂O₃
分子量:356.54

保管条件:

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

CYD-1-79 構造式

CAS 番号: 2220235-94-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

5-HT_2C Receptor

D₃ Receptor

Alpha-2A adrenergic receptor

Alpha-2B adrenergic receptor

5-HT Receptor アイソフォーム固有の製品をすべて表示 :

Dopamine Receptor アイソフォーム固有の製品をすべて表示 :

Adrenergic Receptor アイソフォーム固有の製品をすべて表示 :

Calcium Channel アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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 %	/	/

体内実験

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.

化学情報

CAS 番号 2220235-94-7
分子量 356.54
分子式 C₂₀H₄₀N₂O₃
SMILES

O=C([C@H]1NCC[C@@H](CCCCCCCCCCC)C1)NCC(O)CO
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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

Minimum order quantity

100 mg

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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CYD-1-79

5-HT Receptor アイソフォーム固有の製品をすべて表示

Dopamine Receptor アイソフォーム固有の製品をすべて表示

Adrenergic Receptor アイソフォーム固有の製品をすべて表示

Calcium Channel アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

CYD-1-79 関連分類

HY-182091 関連分類