Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C29H35N7O3 |
| Molecular Weight | 529.6333 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
NC(=N)NCCC[C@@H](NC(=O)C(C1=CC=CC=C1)C2=CC=CC=C2)C(=O)NCC3=CC=C(CNC(N)=O)C=C3
InChI
InChIKey=TVMJSGGZULFVCZ-XMMPIXPASA-N
InChI=1S/C29H35N7O3/c30-28(31)33-17-7-12-24(26(37)34-18-20-13-15-21(16-14-20)19-35-29(32)39)36-27(38)25(22-8-3-1-4-9-22)23-10-5-2-6-11-23/h1-6,8-11,13-16,24-25H,7,12,17-19H2,(H,34,37)(H,36,38)(H4,30,31,33)(H3,32,35,39)/t24-/m1/s1
| Molecular Formula | C29H35N7O3 |
| Molecular Weight | 529.6333 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
BIBO-3304 is a subtype selective nonpeptide antagonist with subnanomolar affinity for the Y1 receptor subtype that significantly inhibits food intake induced by application of NPY or by fasting. BIBO-3304 is a NPY Y1 receptor antagonist (IC50 values are 0.38 and 0.72 nM at human and rat receptors respectively) that displays > 2600-fold selectivity over Y2, Y4 and Y5 receptors.
Approval Year
Sample Use Guides
Rats: Intracerebroventricular administration of BIBO-3304 (1, 10, 50 nmol) had no effect on locomotor activity as measured by number of rearings and number of squares visited in an open field test in rats, but at 50 nmol dose defecation was significantly increased. BIBO-3304 (10 nmol) reduced amphetamine-induced increases in horizontal and vertical activity whereas its S-configurated enantiomer BIBO-3457 was inactive. In an open field test BIBO-3304 (10 nmol) inhibited purposeless running in rats sensitized to direct dopaminergic agonist apomorphine (0.5 mg/kg, s.c.). BIBO-3304 (10 nmol but not 1 nmol, i.c.v.) reduced fighting in apomorphine-induced aggression paradigm.
Route of Administration:
Other
BIBO-3304 was evaluated in terms of its properties to
inhibit the NPY mediated signal transduction in SK-N-MC
cells. No agonistic properties were found with 1 uM BIBO-3304
in the cAMP assay. The NPY induced inhibition of cAMP
synthesis was antagonized by 100 nM BIBO-3304 with a pKb of
9.1+0.4.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:27:33 GMT 2023
by
admin
on
Sat Dec 16 09:27:33 GMT 2023
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| Record UNII |
QKC82E736Q
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| Record Status |
Validated (UNII)
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| Record Version |
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191868-13-0
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5311022
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