BMS 181168 - CAS 123259-91-6
Catalog number: 123259-91-6
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C15H19F3N4O
Molecular Weight:
328.34
COA:
Inquire
Targets:
Others
Description:
This active molecular is an potential cognitive enhancer originated by Bristol-Myers Squibb. Mechanism of Action is not identified. Bmy 21502 is also a nootropic agent and it can protect rodents from ECS-induced amnesia in a step-down passive avoidance task. But clinical study for treatment of Alzheimer's disease was discontinued.
Purity:
98%
Appearance:
Powder
Synonyms:
Bmy 21502; Bmy21502; Bmy-21502; Bms-181168; Bms 181168; Bms181168. 1-((1-(2-(trifluoromethyl)pyrimidin-4-yl)piperidin-4-yl)methyl)pyrrolidin-2-one
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Alzheimer's disease
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
KEWFMWJJMGQBAN-UHFFFAOYSA-N
InChI:
InChI=1S/C15H19F3N4O/c16-15(17,18)14-19-6-3-12(20-14)21-8-4-11(5-9-21)10-22-7-1-2-13(22)23/h3,6,11H,1-2,4-5,7-10H2
Canonical SMILES:
C1CC(=O)N(C1)CC2CCN(CC2)C3=NC(=NC=C3)C(F)(F)F
Current Developer:
Originator:Bristol-Myers Squibb
1.The nootropic compound BMY-21502 improves spatial learning ability in brain injured rats.
Pierce JE;Smith DH;Eison MS;McIntosh TK Brain Res. 1993 Oct 8;624(1-2):199-208.
Although long-lasting cognitive dysfunction often follows clinical traumatic brain injury (TBI), few pharmacologic regimens have been developed to treat post-traumatic cognitive deficits. We have previously shown that, in the rat, experimental lateral fluid-percussion (FP) brain injury induces a profound impairment in retrograde memory. In the present study, we characterized alterations in the ability of rats to learn a novel task following lateral FP brain injury and examined the potential modulatory effects of the nootropic cognitive enhancer BMY-21502 on post-injury learning. Male Sprague-Dawley rats were subjected to lateral (parasagittal) FP brain injury of moderate severity (2.4 atm) or sham surgery (no injury). On days 7 and 8 post-injury, animals were tested in a Morris water maze for their ability to learn to navigate to a submerged, invisible platform using external visual cues. BMY-21502 (10 mg/kg) or vehicle was administered 30 min prior to the first trial on both days. A highly significant (P < 0.001) impairment in post-injury learning was observed in vehicle-treated brain-injured animals compared with vehicle-treated sham animals. Injured animals treated with BMY-21502 at one week post-injury showed significantly (P < 0.
2.Effects of BMY-21502 on anoxia in mice.
Amano M;Goto A;Takahashi N;Hasegawa T;Nabeshima T Jpn J Pharmacol. 1993 Mar;61(3):157-63.
The protective effects of BMY-21502 (1-[[1-[2-(trifluoromethyl)-4-pyrimidinyl]-4-piperidinyl]methyl]-2- pyrrolidinone) against cerebral anoxia were investigated using various models in mice, in comparison with those of other cerebroactive drugs. Oral administration of BMY-21502 (10-100 mg/kg) significantly prolonged the survival time in KCN (2.4 mg/kg, i.v.)-induced anoxia. Oxiracetam and idebenone exerted similar but weak protection at doses above 100 mg/kg, p.o. and only at a dose of 100 mg/kg, p.o., respectively. Significant protection by BMY-21502 against moderate hypobaric hypoxia was observed at doses of 30 and 100 mg/kg, p.o. Idebenone (100 and 300 mg/kg, p.o.) significantly prolonged the survival time of mice in this model, but oxiracetam (30-300 mg/kg, p.o.) did not. Oral administration of all of these drugs (BMY-21502, 3-300 mg/kg; Oxiracetam, 100-1000 mg/kg; Idebenone, 100-1000 mg/kg) failed to increase the number of gasps and the duration of gasping in the decapitated head of mice as a complete ischemic model. The anti-anoxic effect of BMY-21502 in the KCN-anoxia model was blocked by pretreatment with scopolamine. These findings suggest that BMY-21502 has an anti-anoxic action superior to those of the other cerebroactive drugs used, and activation of the CNS cholinergic system is involved as one of the causative mechanisms for the anti-anoxic effect of BMY-21502.
3.BMS-181168 for protection of the human brain against hypoxia: double-blind, placebo-controlled EEG mapping studies.
Saletu B;Schulz H;Herrmann WM;Anderer P;Shrotriya RC;Vanbrabant E Pharmacopsychiatry. 1994 Sep;27(5):189-97.
In a double-blind, placebo-controlled, cross-over trial, the antihypoxidotic properties of BMS-181168 (previously BMY 21502)--a 1-[[1-[2-(trifluoromethyl)-4-pyrimidinyl]-4-piperidinyl]methyl]-2- pyrrolidinone alleviating impairment of learning and memory in the animal--were studied utilizing EEG mapping under an experimental hypoxic hypoxidosis. The latter was induced by a fixed gas combination of 9.8% oxygen (O2) and 90.2% nitrogen (N2) (found at 6000 m altitude), which was inhaled for 23 minutes under normobaric conditions by 16 healthy male volunteers (aged 23-35 years, mean 27.2 years). After an adaptation session, they received in randomized order at weekly intervals oral single doses of placebo, or of 100 mg, 200 mg, and 400 mg BMS-181168. Evaluation of blood gases (PO2, PCO2, SO2), adverse events, and EEG mapping was carried out prior to drug administration and 2, 4, 6 and 8 hours post-drug, on each occasion under normoxic and transient hypoxic conditions. Hypoxemia was controlled by drawing arterialized capillary blood samples from the earlobes after hyperemization of the latter (after 0, 14, and 23 minutes of hypoxic gas inhalation) and by oximetry. After 23 minutes of inhalation, analysis showed a drop in PO2 from 98 to 48 mm Hg, in PCO2 from 41 to 31 mm Hg, and in SO2 from 97 to 80%.
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