1. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  2. 5-HT Receptor Dopamine Receptor Dopamine Transporter Adrenergic Receptor Calcium Channel
  3. 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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CYD-1-79

CYD-1-79 Chemical Structure

CAS No. : 2220235-94-7

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Description

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[1].

IC50 & Target[1]

5-HT2C Receptor

 

D3 Receptor

 

Alpha-2A adrenergic receptor

 

Alpha-2B adrenergic receptor

 

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 T1/2 Tmax Cmax AUC0-inf F CL Vss
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.
Molecular Weight

356.54

Formula

C20H40N2O3

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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CYD-1-79
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HY-182091
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