Sigma Receptors: Chemistry, Cell Biology and Clinical by Dr. Rae R. Matsumoto (auth.), Tsung-Ping Su, Rae R.

By Dr. Rae R. Matsumoto (auth.), Tsung-Ping Su, Rae R. Matsumoto, Wayne D. Bowen (eds.)

Sigma receptors are promising drug improvement pursuits for a bunch of neurological, psychiatric, oncological, immunological, cardiovascular, ophthalmological, and gastrointestinal issues. they're structurally precise proteins which are specific from classical G protein-coupled receptors, ionotropic receptors, or receptor tyrosine kinases. With subtypes at the moment recognized, they modulate mobilephone survival and excitability, and subserve many severe services within the physique. Endogenous ligands for those receptors are unknown, even though present clues element to neurosteroids.

This publication offers a well timed replace at the medicinal chemistry, mobilephone biology, and scientific implications of sigma receptors. It places the knowledge in a ancient standpoint to assist new comers to the sector effectively navigate the complicated early background surrounding those proteins, and offers a launching aspect for the improvement of fascinating, new research.

Sigma Receptors: Chemistry, cellphone Biology and scientific Implications could be a necessary software for pharmacologists, medicinal chemists, cellphone biologists, molecular biologists, clinicians, and others attracted to a concise, cutting-edge assessment of the sigma receptor box with a specific view in the direction of novel healing advances.

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Extra resources for Sigma Receptors: Chemistry, Cell Biology and Clinical Implications

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66. Matsumoto RR, Hewett KL, Pouw B, Bowen WD, Husbands SM, Cao JJ, Newman AH. Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters. Neuropharmacology 2001a, 41:878-886. 67. Romieu P, Phan V, Martin-Pardon R, Maurice T. Involvement of the sigma-1 receptor in cocaine-induced conditioned place preference: possible dependence on dopamine uptake blockade. Neuropsychopharmacology 2002, 26:444-455. 44 Chapter 2 68.

Brain Res 1996, 725:155-165. 106. Harada Y, Hara H, Sukamoto T, Characterization of specific ( + ) - [ ' H ] N allylnormetazocine and [•'H]l,3-di(2-tolyl)guanidine binding sites in porcine gastric fundic mucosa. J Pharmacol Exp Ther 1994, 269:905-910. 107. Hara H, Tanaka K, Harada Y, Sukamoto T. Sigma receptor-mediated effects of a new antiulcer agent, KB-5492, on experimental gastric mucosal lesions and gastric alkaline secretion in rats. J Pharmacol Exp Ther 1994, 269:799-805. 108. Roman F, Pascaud X, Chomette G, Bueno L, Junien JL.

It was discovered that in general, substitutions on the carbazole ring system of rimcazole served to decrease binding affinities at bothCTIreceptors and the DAT (57,59). Data for other rimcazole analogues is shown in Table 2-1. N-methylation of the terminal piperazine nitrogen (SH 1-73) resulted in a small increase in binding affinity at (5\ receptors (Kj = 552 nM) but in a slightly less active DAT compound (Kj = 436 nM) (59). Alternatively, placing a propylphenyl group, on the terminal piperazine nitrogen (SH 3-28), as seen with GBR 12909, served to improve and restore ai receptor and DAT binding affinities, respectively.

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