Alvameline - CAS 120241-31-8
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Alvameline, also known as Lu25-109, is a partial M1agonist and M2/M3antagonist that was progressed into clinical studies for the treatment of Alzheimer's disease and Urinary incontinence but was subsequently discontinued.
Brife Description:
A partial M1 agonist and M2/M3 antagonist
5-(2-ethyltetrazol-5-yl)-1-methyl-3,6-dihydro-2H-pyridine; 5-(2-ethyl-2H-tetrazol-5-yl)-1,2,3,6-tetrahydro-1-methylpyridine tartrate; LU 25-109; LU 25-109-T; LU-25-109-T
Store in a cool and dry place (or refer to the Certificate of Analysis).
Boiling Point:
342.1±52.0 ℃ at 760 Torr
1.25±0.1 g/cm3
Canonical SMILES:
1.Activating the posttraumatic cholinergic system for the treatment of cognitive impairment following traumatic brain injury.
Pike BR;Hamm RJ Pharmacol Biochem Behav. 1997 Aug;57(4):785-91.
Cognitive impairment after traumatic brain injury (TBI) is correlated with decreased cholinergic markers of neuronal viability. The purpose of this experiment was to test the hypothesis that pharmacological activation of the muscarinic cholinergic system during the recovery period after TBI will improve cognitive performance. LU 25-109-T is a partial muscarinic M1 agonist that also acts as an antagonist at presynaptic M2 autoreceptors (thus increasing ACh release). Injured rats were injected subcutaneously daily for 15 days with either 0.0, 3.6, or 15 mumol/kg of LU 25-109-T beginning 24 h after a receiving a moderate (2.1 +/- 0.1 atm) level of central fluid percussion brain injury. Cognitive performance was assessed on days 11-15 postinjury in a Morris water maze (MWM). Injured rats treated with 15 mumol/kg, but not those treated with 3.6 mumol/kg, showed a significant improvement (p < 0.01) in MWM performance as compared with injured vehicle-treated rats. This result supports the hypotheses that a decrease in posttraumatic cholinergic neurotransmission contributes to TBI-induced cognitive deficits and that increasing cholinergic tone during the recovery period following TBI will improve cognitive performance.
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CAS 120241-31-8 Alvameline

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