Effects of (±)-huprine Y and (±)-huprine Z, two new anticholinesterasic drugs, on muscarinic receptors

M. M. Alcalá; A. Maderuelo; N. M. Vivas; P. Camps; D. Muñoz-Torrero; M. V. Clos; A. Badia

doi:https://doi.org/10.1016/j.neulet.2004.12.044

Effects of (±)-huprine Y and (±)-huprine Z, two new anticholinesterasic drugs, on muscarinic receptors

M. M. Alcalá, A. Maderuelo, N. M. Vivas, P. Camps, D. Muñoz-Torrero, M. V. Clos, A. Badia

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Abstract

The cholinergic profile of (±)-huprine Y and (±)-huprine Z on muscarinic receptors has been determined. Displacement of [3H]- pirenzepine and [3H]-QNB plus pirenzepine was performed in rat hippocampus. Both compounds showed a higher degree of affinity to M1 muscarinic receptors (P < 0.01) than to M2 muscarinic receptors. To determine the M1 agonist or antagonist role of the two huprines, studies of inositol phosphates (IP) production were performed. Both huprines significantly stimulated IP accumulation in a concentration-dependent manner. The reversion of this effect by different antagonists showed that M1 muscarinic receptors were activated by (±)-huprine Y and (±)-huprine Z, but some other mechanisms, such as α1- adrenoceptors or nicotinic receptors, were involved. © 2004 Elsevier Ireland Ltd. All rights reserved.

Original language	English
Pages (from-to)	106-109
Journal	Neuroscience Letters
Volume	379
DOIs	https://doi.org/10.1016/j.neulet.2004.12.044
Publication status	Published - 6 May 2005

Keywords

(±)-Huprine Y
(±)-Huprine Z
AChE inhibitor
Alzheimer's disease
Huperzine A
Muscarinic receptors
Tacrine

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@article{6a550ecf696f47deb565de5986aab046,

title = "Effects of (±)-huprine Y and (±)-huprine Z, two new anticholinesterasic drugs, on muscarinic receptors",

abstract = "The cholinergic profile of (±)-huprine Y and (±)-huprine Z on muscarinic receptors has been determined. Displacement of [3H]- pirenzepine and [3H]-QNB plus pirenzepine was performed in rat hippocampus. Both compounds showed a higher degree of affinity to M1 muscarinic receptors (P < 0.01) than to M2 muscarinic receptors. To determine the M1 agonist or antagonist role of the two huprines, studies of inositol phosphates (IP) production were performed. Both huprines significantly stimulated IP accumulation in a concentration-dependent manner. The reversion of this effect by different antagonists showed that M1 muscarinic receptors were activated by (±)-huprine Y and (±)-huprine Z, but some other mechanisms, such as α1- adrenoceptors or nicotinic receptors, were involved. {\textcopyright} 2004 Elsevier Ireland Ltd. All rights reserved.",

keywords = "(±)-Huprine Y, (±)-Huprine Z, AChE inhibitor, Alzheimer's disease, Huperzine A, Muscarinic receptors, Tacrine",

author = "Alcal{\'a}, {M. M.} and A. Maderuelo and Vivas, {N. M.} and P. Camps and D. Mu{\~n}oz-Torrero and Clos, {M. V.} and A. Badia",

year = "2005",

month = may,

day = "6",

doi = "https://doi.org/10.1016/j.neulet.2004.12.044",

language = "English",

volume = "379",

pages = "106--109",

journal = "Neuroscience Letters",

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publisher = "Elsevier Ireland Ltd",

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TY - JOUR

T1 - Effects of (±)-huprine Y and (±)-huprine Z, two new anticholinesterasic drugs, on muscarinic receptors

AU - Alcalá, M. M.

AU - Maderuelo, A.

AU - Vivas, N. M.

AU - Camps, P.

AU - Muñoz-Torrero, D.

AU - Clos, M. V.

AU - Badia, A.

PY - 2005/5/6

Y1 - 2005/5/6

N2 - The cholinergic profile of (±)-huprine Y and (±)-huprine Z on muscarinic receptors has been determined. Displacement of [3H]- pirenzepine and [3H]-QNB plus pirenzepine was performed in rat hippocampus. Both compounds showed a higher degree of affinity to M1 muscarinic receptors (P < 0.01) than to M2 muscarinic receptors. To determine the M1 agonist or antagonist role of the two huprines, studies of inositol phosphates (IP) production were performed. Both huprines significantly stimulated IP accumulation in a concentration-dependent manner. The reversion of this effect by different antagonists showed that M1 muscarinic receptors were activated by (±)-huprine Y and (±)-huprine Z, but some other mechanisms, such as α1- adrenoceptors or nicotinic receptors, were involved. © 2004 Elsevier Ireland Ltd. All rights reserved.

AB - The cholinergic profile of (±)-huprine Y and (±)-huprine Z on muscarinic receptors has been determined. Displacement of [3H]- pirenzepine and [3H]-QNB plus pirenzepine was performed in rat hippocampus. Both compounds showed a higher degree of affinity to M1 muscarinic receptors (P < 0.01) than to M2 muscarinic receptors. To determine the M1 agonist or antagonist role of the two huprines, studies of inositol phosphates (IP) production were performed. Both huprines significantly stimulated IP accumulation in a concentration-dependent manner. The reversion of this effect by different antagonists showed that M1 muscarinic receptors were activated by (±)-huprine Y and (±)-huprine Z, but some other mechanisms, such as α1- adrenoceptors or nicotinic receptors, were involved. © 2004 Elsevier Ireland Ltd. All rights reserved.

KW - (±)-Huprine Y

KW - (±)-Huprine Z

KW - AChE inhibitor

KW - Alzheimer's disease

KW - Huperzine A

KW - Muscarinic receptors

KW - Tacrine

U2 - https://doi.org/10.1016/j.neulet.2004.12.044

DO - https://doi.org/10.1016/j.neulet.2004.12.044

M3 - Article

SN - 0304-3940

VL - 379

SP - 106

EP - 109

JO - Neuroscience Letters

JF - Neuroscience Letters

ER -

Effects of (±)-huprine Y and (±)-huprine Z, two new anticholinesterasic drugs, on muscarinic receptors

Abstract

Keywords

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