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YFa and analogs:Investigation of opioid receptors in smooth muscle contraction

World Journal of Gastroenterology 2011年第40期17卷 4523-4531页

作者： Krishan Kumar Ritika Goyal Annu Mudgal Anita Mohan santosh pasha Peptide Synthesis Laboratory Institute of Genomics and Integrative Biology Delhi 110007 India University School of Basic and Applied Sciences GGSIP University Sector-16 C Dwarka Delhi 110075 India Department of Chemistry Motilal Nehru College University of Delhi Delhi 110021 India

AIM:To study the pharmacological profile and inhibition of smooth muscle contraction by YFa and its analogs in conjunction with their receptor selectivity. METHODS:The effects of YFa and its analogs (D-Ala2) YFa, Y (D-Ala2) GFMKKKFMRF amide and Des-Phe-YGGFMKKKFMR amide in guinea pig ileum (GPI) and mouse vas deferens (MVD) motility were studied using an isolated tissue organ bath system, and morphine and DynA (1-13) served as controls. Acetylcholine was used for muscle stimulation. The observations were validated by specific antagonist pretreatment experiments using naloxonazine, naltrindole and norbinaltor-phimine norBNI. RESULTS:YFa did not demonstrate significant inhibition of GPI muscle contraction as compared with mor-phine (15% vs 62%, P = 0.0002), but moderate inhibition of MVD muscle contraction, indicating the role of κ opioid receptors in the contraction. A moderate inhibition of GPI muscles by (Des-Phe) YFa revealed the role of anti-opiate receptors in the smooth muscle contraction. (D-Ala-2) YFa showed significant inhibition of smooth muscle contraction, indicating the involvement of mainly δ receptors in MVD contraction. These results were supported by specific antagonist pretreatment assays. CONCLUSION:YFa revealed its side-effect-free analgesic properties with regard to arrest of gastroin-testinal transit. The study provides evidences for the involvement of κ and anti-opioid receptors in smooth muscle contraction.

关键词： Opioid receptor Guinea pig ileum Mousevas deferens Smooth muscle contraction Gastrointestinal motility

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Role of opioid receptor heterodimerization in pain modulation and tolerance development

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World Journal of Pharmacology 2015年第1期4卷 144-159页

作者： Annu Mudgal santosh pasha Peptide Synthesis Laboratory CSIR/Institute of Genomics and Integrative Biology Academy of Scientific and Innovative Research

Protein to protein interactions leading to homo/heteromerization of receptor is well documented in literature. These interactions leading to dimeric/oligomers formation of receptors are known to modulate their function, particularly in case of G-protein coupled receptors. The opioid receptor heteromers having changed pharmacological properties than the constituent protomers provides preferences for novel drug targets that could lead to potential analgesicactivity devoid of tolerance and physical dependence. Heterodimerization of opioid receptors appears to generate novel binding properties with improved specificity and lack of side effects. Further the molecules which can interact simultaneously to both the protomers of the heteromer, or to both the binding sites(orthosteric and allosteric) of a receptor protein could be potential therapeutic molecules. This review highlights the recent advancements in exploring the plausible role of heteromerization of opioid receptors in induction of tolerance free antinociception.

关键词： Opioid receptors Receptor heterodimers G-protein coupled receptors oligomerization G protein coupled receptors Opioid tolerance G-protein coupled receptors Allosteric regulation Antinociception

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