ChemicalBook CAS DataBase List 186185-03-5

186185-03-5

Name	1,4-Dihydro-4-[3-[[[[3-[4-(3-methoxyphenyl)-1-piperidinyl]propyl]amino]carbonyl]amino]phenyl]-2,6-dimethyl-3,5-pyridinedicarboxylicacid3,5-dimethylesterL-Lactate
CAS	186185-03-5
Molecular Formula	C33H42N4O6
MDL Number	MFCD16878998
Molecular Weight	590.71
MOL File	186185-03-5.mol

Chemical Properties

Boiling point	707.5±60.0 °C(Predicted)
density	1.188±0.06 g/cm3(Predicted)
storage temp.	Desiccate at +4°C
solubility	DMSO: >10mg/mL
form	powder
pka	13.94±0.46(Predicted)
color	light yellow to yellow
InChIKey	WMYSXJSJXZFODY-UHFFFAOYSA-N
SMILES	COC(=O)C1=C(C)NC(C)=C(C1c2cccc(NC(=O)NCCCN3CCC(CC3)c4cccc(OC)c4)c2)C(=O)OC

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302
Precautionary statements	P264-P270-P301+P312-P330-P501
Hazard Codes	Xn
Risk Statements	22 less more
WGK Germany	3
Storage Class	11 - Combustible Solids
Hazard Classifications	Acute Tox. 4 Oral

Hazard Information

Uses

BMS 193885, is a potent, and competitive neuropeptide (NPY) Y1 antagonist, that has also displayed 160-fold selectivity over σ1, α1, Y2, Y4 and Y5 receptors respectively. BMS 193885, is also brain penetrant, and able to reduce food intake and body weight through central Y1 inhibition.

Biological Activity

BMS-193885 is a potentselective Y1 antagonist th at is active in both acute and chronic animal models of food intake. Although it is active in vivoit is not orally bioavailable due to poor intestinal absorptionso it is not being pursued for pharmaceutical development. BMS-193885 has been used as a pre-clinical proof of concept tool for showing efficacy of Y1 antagonism in treating obesity.

in vivo

Acute feeding suppression: BMS-193885 (30-50 μg/5 μL; i.c.v.; single dose) blocks NPY (5 μg, 10 μg)-induced feeding in satious Sprague-Dawley rats^[1].
Peripheral feeding suppression: BMS-193885 (10 mg/kg; i.p.; single dose) reduces NPY-induced 1-hour food intake and spontaneous nocturnal food intake in male Sprague-Dawley rats^[1]^[2].
Chronic weight loss: BMS-193885 (10 mg/kg; i.p.; once daily for 44 days) reduces cumulative food intake and weight gain in male Sprague-Dawley rats without tolerance^[1].
Cardiovascular safety: BMS-193885 (30 mg/kg; i.v.; single dose) had no serious adverse effects on heart rate and blood pressure in conscious rats and anesthetized dogs^[1].
BMS-193885 (5 mg/kg; i.p.; single dose) significantly blocked NPY Y1 receptors in Wistar rats and reduced the effects of NPY injection on cardiopulmonary function^[3].

Animal Model:	Male Sprague-Dawley rats (220-280 g), satiated, with i.c.v. cannula implantation^[1]
Dosage:	30-50 μg (10% DMSO in sterile Ringer)
Administration:	i.c.v. injection (5 μL), single dose
Result:	Significantly reduced NPY-induced 1-h food intake by 57% (30 μg) and 63% (50 μg) compared to vehicle controls. No effect was observed on basal food intake¹.

Animal Model:	Male Sprague-Dawley rats (220-280 g), satiated^[1]
Dosage:	10 mg/kg (40% PEG 400 + 60% saline)
Administration:	i.p. injection, single dose 30 min before dark cycle
Result:	Reduced NPY-induced 1-h food intake by 33-57% and spontaneous overnight food intake by 29-54% compared to vehicle.

Animal Model:	Male Sprague-Dawley rats (220-280 g), naive^[1]
Dosage:	10 mg/kg BMS-193885 (40% PEG 400 + 60% saline)
Administration:	i.p. injection daily for 44 days, 2 h before dark cycle
Result:	Reduced cumulative food intake by 12-15% and suppressed body weight gain by 8.5% compared to vehicle. No tolerance developed, but adhesive peritonitis occurred in some animals.

Animal Model:	Conscious male Sprague-Dawley rats (220-280 g); anesthetized dogs^[1]
Dosage:	30 mg/kg (rats), 10 mg/kg (dogs) (in sterile saline)
Administration:	i.v. injection, single dose
Result:	No significant changes in heart rate or blood pressure were observed in rats or dogs. Oral bioavailability was <0.1% due to poor absorption^[1]1.

IC 50

NPY Y₁ receptor; NPY Y₁ receptor: 3.3 nM (Ki)

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