BIBP3226 TFA is a novel, selective non-peptide neuropeptide Y Y1 receptor antagonist, with Ki values of 1.1, 79, and 108 nM for rNPY Y1, hNPFF2, and rNPFF, respectively. NPY Y(1) antagonist BIBP3226 is able to displace with low affinity, 50 -- 100 nM, the specific binding on NPFF receptors expressed in CHO cells as well as in rat dorsal spinal cord, an affinity however superior to those determined against Y(2), Y(4) or Y(5) receptors. BIBP3226 (0.5 and 5 micrograms, i.c.v.) induced an anxiogenic-like effect at the higher dose tested.
| Molecular Weight | 587.59 |
| Formula | C29H32F3N5O5 |
| CAS Number | 1068148-47-9 |
| Solubility (25°C) | DMSO 120 mg/mL Water >1 mg/mL |
| Storage | Store at ≤-20°C, protect from light, dry, sealed |
| 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.
[2] P Zhang, et al. BIBP 3226 inhibition of nicotinic receptor mediated chromaffin cell secretion
| Related Neuropeptide Receptor Products |
|---|
| 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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