JNJ-31020028 was demonstrated to be an antagonist (pK(B) = 8.04 +/- 0.13) in functional assays. JNJ-31020028 occupied Y(2) receptor binding sites (approximately 90% at 10 mg/kg) after subcutaneous administration in rats. Neither systemic (0, 15, 30, and 40 mg/kg, subcutaneously [s.c.]) nor intracerebroventricular (0.0, 0.3, and 1.0 nmol/rat) administration of JNJ-31020028 affected alcohol-reinforced lever pressing or relapse to alcohol seeking behavior following stress exposure. JNJ-31020028 (15 mg/kg, s.c.) did reverse the anxiogenic effects of withdrawal from a single bolus dose of alcohol on the elevated plus-maze, confirming the anxiolytic-like properties of NPY Y2 antagonism. Chronic administration of JNJ-31020028 induced a decrease in immobility time in the forced swim test in OBX while had no effect in control animals.
| Molecular Weight | 565.68 |
| Formula | C34H36FN5O2 |
| CAS Number | 1094873-14-9 |
| Solubility (25°C) | DMSO: ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Neuropeptide Receptor Products |
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| Neuropeptide Y (human, rat, mouse) TFA
Neuropeptide Y (human, rat, mouse) TFA is involved in Alzheimer's disease (AD) and protects rat cortical neurons against β-Amyloid toxicity. |
| N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36)
N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) is a selective agonist of neuropeptide Y Y2 receptor. |
| Neuropeptide Y (13-36), amide, human
Neuropeptide Y (13-36), amide, human is a selective neuropeptide Y2 receptor agonist. |
| Neuropeptide FF
Neuropeptide FF (NPFF), an octapeptide belonging to the RF-amide family of peptides, interacts with two distinct G-protein-coupled receptors, NPFF(1) and NPFF(2). |
| CART(55-102) (human)
CART(55-102)(human) is an endogenous satiety factor with potent appetite-suppressing activity. |
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