Age-related changes in human muscarinic acetylcholine receptors measured by positron emission tomography

Suhara, Tetsuya; Ito, Osamu; Kobayashi, Keiko; Suzuki, Kazutoshi; Tateno, Yukio

doi:10.1016/0304-3940(93)90777-i

Cited by 59 publications

(38 citation statements)

References 12 publications

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“…Data on other neurotransmitter suggest there are similar age-related changes to those seen in the dopaminergic system (McGeer et al, 1977;Petkov et al, 1988;Suhara et al, 1993;Meltzer et al, 1998;Miguez et al, 1999;Gross-Isseroff et al, 2000;Ishida et al, 2000;Segovia et al, 2001). Studies also provide evidence for both linear (Pirker et al, 2000) and non-linear (Kohen et al, 2000) models to explain these changes.…”

Section: Functional Implicationsmentioning

confidence: 81%

Ageing and the nigrostriatal dopaminergic system

Reeves

Bench

Howard

2002

Int J Geriat Psychiatry

116

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Section: Functional Implicationsmentioning

confidence: 81%

Ageing and the nigrostriatal dopaminergic system

Reeves

Bench

Howard

2002

Int J Geriat Psychiatry

116

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“…After i.v. injection of [N-n C-methyl]benztropine [12], [n C]scopolamine [13] or [MC]NMPB [14] a 2-to 3-fold higher radioactivity has been demonstrated in the neocortex than in the cerebellum.…”

Section: Discussionmentioning

confidence: 99%

“…Using positron emission tomography (PET) radioli gand binding to muscarinic receptors has been examined in the human brain in vivo [12][13][14], Xanomeline and sev eral of the substituted TZTP have high affinity for the Mi subtype and potential as radioligands for PET [8]. Xa nomeline and butylthio-TZTP have recently been labelled with the positron emitting radionuclide n C [15],…”

Section: Kargermentioning

confidence: 99%

PET Study of the M1-Agonists [11C]Xanomeline and [11C]Butylthio-TZTP in Monkey and Man

Farde

Suhara

Halldin

et al. 1996

Dement Geriatr Cogn Disord

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Xanomeline, a substituted TZTP, is a new M₁ selective muscarinic agonist in clinical trials for Alzheimer''s disease. The brain uptake of [¹¹C]xanomeline and the analog [¹¹C]butylthio-TZTP was examined by positron emission tomography (PET). Radioactivity accumulated most markedly in the neocortex and the striatum. Pharmacological characterization in vitro and in cynomolgus monkeys in vivo by PET indicated specific [¹¹C]butylthio-TZTP binding to muscarinic receptors and to sigma-1 recognition sites. More than 5% of the radioactivity was in the human brain 5 min after i.v. injection of [¹¹C]xanomeline or [¹¹C]butylthio-TZTP. This high brain uptake may be clinically advantageous in the sense that substituted TZTP may induce central muscarinic agonist effects at a dose level for which there is a low risk of peripheral side-effects.

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“…Carbon-ll labelled Nmethyl 4-piperidyl benzilate ([llC]NMPB) is a particularly useful ligand because of its high affinity for mAChR and high uptake into the brain in vivo (Otto et al, 1989;Tejani-Butt et al, 1990;Koeppe et al, 1992;Suhara et al, 1993).…”

Section: Introductionmentioning

confidence: 99%

Effects of trihexyphenidyl and L-dopa on brain muscarinic cholinergic receptor binding measured by positron emission tomography

Shinotoh

Asahina

Ito³

et al. 1994

J Neural Transm Gen Sect

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The effects of pharmacological intervention on brain muscarinic cholinergic receptor (mAChR) binding were assessed in seven patients with Parkinson's disease by positron emission tomography and carbon-11 labelled N-methyl-4-piperidyl benzilate ([11C]NMPB). [11C]NMPB was injected twice, approximately 2 hours apart, in each patient, to assess the effect of single doses of 4 mg of trihexyphenidyl (n = 5) or 400 mg of L-dopa with 57 mg of benserazide (n = 2) on the binding parameter of mAChRs (K3). There was a mean 28% inhibition of K3 values in the brain in the presence of trihexyphenidyl, which was assumed to reflect mAChR occupancy. No significant change in K3 was observed in the presence of L-dopa. This study demonstrates the feasibility of measuring mAChR occupancy by an anticholinergic medication with PET.

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Age-related changes in human muscarinic acetylcholine receptors measured by positron emission tomography

Cited by 59 publications

References 12 publications

Ageing and the nigrostriatal dopaminergic system

Ageing and the nigrostriatal dopaminergic system

PET Study of the M<sub>1</sub>-Agonists [<sup>11</sup>C]Xanomeline and [<sup>11</sup>C]Butylthio-TZTP in Monkey and Man

Effects of trihexyphenidyl and L-dopa on brain muscarinic cholinergic receptor binding measured by positron emission tomography

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