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Exploring the role of sex in asthma and COPD pharmacological treatment. [PDF]

Curr Res Pharmacol Drug Discov
Calzetta L, Gholamalishahi S, Pistocchini E, Zerillo B, Matera MG, Rogliani P.   +5 more
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Regulation of muscarinic M2 receptors

Life Sciences, 1997
The molecular mechanisms involved in the regulation of muscarinic receptor gene expression are poorly understood. In an effort to gain a better understanding of the regulation of M2 receptors, we have investigated homologous and heterologous regulation of M2 muscarinic receptor protein and gene expression in human embryonic lung fibroblasts (HEL 299 ...
P J, Barnes, E B, Haddad, J, Rousell
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m2-Toxin: A Selective Ligand for M2 Muscarinic Receptors

Molecular Pharmacology, 1999
Selective ligands are needed for distinguishing the functional roles of M2 receptors in tissues containing several muscarinic receptor subtypes. Because the venom of the green mamba Dendroaspis angusticeps contains the most specific antagonists known for M1 and M4 receptors (m1-toxin and m4-toxin), it was screened for toxins that inhibit the binding of
J M, Carsi, H H, Valentine, L T, Potter
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Evidence of paired M2 muscarinic receptors.

Molecular Pharmacology, 1991
Binding assays involving various antagonists, including N-[3H] methylscopolamine, [3H]quinuclidinyl benzilate, AFDX-116, pirenzepine, and propylbenzilylcholine mustard, disclosed only a single population of M2 muscarinic receptors in membranes from the rat "brainstem" (medulla, pons, and colliculi).
L T, Potter, L A, Ballesteros, L H, Bichajian, C A, Ferrendelli, A, Fisher, H E, Hanchett, R, Zhang   +6 more
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Benzylidene ketal derivatives as M2 muscarinic receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2000
Benzylidene ketal derivatives were investigated as selective M2 receptor antagonists for the treatment of Alzheimer's disease. Compound 10 was discovered to have subnanomolar M2 receptor affinity and 100-fold selectivity against other muscarinic receptors. Also, 10 demonstrated in vivo efficacy in rodent models of muscarinic activity and cognition.
C D, Boyle, S, Chackalamannil, L Y, Chen, S, Dugar, P, Pushpavanam, W, Billard, H, Binch, G, Crosby, M, Cohen-Williams, V L, Coffin, R A, Duffy, V, Ruperto, J E, Lachowicz   +12 more
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Muscarinic M2-receptors in rat thoracic dorsal root ganglia

Neuroscience Letters, 1999
The occurrence and distribution of the muscarinic M2-receptor subtype (M2R) was investigated in rat thoracic dorsal root ganglia (DRG). Messenger RNA for M2R was demonstrated by RT-PCR in total RNA from DRG. Immunoreactivity to M2R-protein was localized to 26% of sensory neurons, the majority of them (85%) belonging to the size class of 25-40 microm in
R, Haberberger, M, Henrich, J Y, Couraud, W, Kummer   +3 more
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Astrocytes have both M1 and M2 muscarinic receptor subtypes

Brain Research, 1986
In astrocytes, carbachol evoked the turnover of membrane inositol phospholipids prelabelled with [3H]inositol, as revealed by [3H]inositol phosphate accumulation in the presence of 5 mM lithium. This effect was blocked by atropine and by pirenzepine (IC50 2.2 nM and 56 nM, respectively).
S, Murphy, B, Pearce, C, Morrow
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