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Important Notice: The Forum does not endorse any medical
product or therapy. ALL medications and supplements
should be taken ONLY under the supervision of a physician,
due to the possibility of side-effects, drug interactions,
etc.
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Name:
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Milameline
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Other Names:
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CI 979
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Primary Medical Role:
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Potential treatment for Alzheimer's disease.
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Role in Alzheimer's Disease:
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Enhances cognition. Appears to be well tolerated.
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Pharmacological Role:
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CI-979 ((E)-1,2,5,6-tetrahydro-1-methyl-3- pyridine-
carboxyaldehyde- O-methyl oxime, CAS139886-04-7) is a non-
subtype selective, partial muscarinic agonist that
enhances cognitive performance and increases central
cholinergic activity in rodents at doses below those
required to increase peripheral cholinergic tone. In
normal healthy volunteers, CI-979 is well tolerated at
single and multiple doses (q 6 h) up to 1.0 mg.
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Side Effects:
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n/a, but in early trials doses above 2.5-mg q6h resulted
in cholinergic symptoms including diaphoresis,
hypersalivation, nausea, diarrhea, hypotension, chills,
headache, flatulence, and urinary frequency and signs
suggestive of parkinsonism (cogwheeling, tremor,
pillrolling, posturing, and shuffling gait).
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Companies:
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Aventis Pharmaceuticals, Inc. (was Hoechst), Warner-Lambert
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Notes:
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Discontinued. The collaboration between Hoechst-Marion-
Roussel and Warner-Lamert on Milameline ended.
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Zheng XM. Detecting Regional Cerebral Blood Flow Changes
in Alzheimer's Patients After Milameline Treatment:
Activation or Baseline SPECT? J Nucl Med Technol. 2002
Sep ;30(3):118-22. Abstract
Schwarz RD, Callahan MJ, Coughenour LL, Dickerson MR,
Kinsora JJ, Lipinski WJ, Raby CA, Spencer CJ, Tecle H.
Milameline (CI-979/RU35926): a muscarinic receptor agonist
with cognition-activating properties: biochemical and in
vivo characterization. J Pharmacol Exp Ther. 1999 Nov;291
(2):812-22. Abstract
Callahan MJ. Combining tacrine with milameline reverses a
scopolamine-induced impairment of continuous performance
in rhesus monkeys. Psychopharmacology (Berl). 1999 Jun;144
(3):234-8.
Abstract
M'Harzi M, Palou AM, Oberlander C, Barzaghi F. Antagonism
of scopolamine-induced memory impairments in rats by the
muscarinic agonist RU 35,926 (CI-979). Pharmacol Biochem
Behav. 1995 May;51(1):119-24. Abstract
Sedman AJ, Bockbrader H, Schwarz RD. Preclinical and phase
1 clinical characterization of CI-979/RU35926, a novel
muscarinic agonist for the treatment of Alzheimer's
disease. Life Sci. 1995;56(11-12):877-82. Abstract
Sramek JJ, Sedman AJ, Reece PA, Hourani J, Bockbrader H,
Cutler NR. Safety and tolerability of CI-979 in patients
with Alzheimer's disease. Life Sci. 1995;57(5):503-10. Abstract
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