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

doi:10.3748/wjg.v17.i40.4523

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Oct 28, 2011 (publication date) through Apr 25, 2024

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World Journal of Gastroenterology

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1007-9327

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Baishideng Publishing Group Inc, 7041 Koll Center Parkway, Suite 160, Pleasanton, CA 94566, USA

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World J Gastroenterol. Oct 28, 2011; 17(40): 4523-4531
Published online Oct 28, 2011. doi: 10.3748/wjg.v17.i40.4523

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

Krishan Kumar, Ritika Goyal, Annu Mudgal, Anita Mohan, Santosh Pasha

Krishan Kumar, Ritika Goyal, Annu Mudgal, Santosh Pasha, Peptide Synthesis Laboratory, Institute of Genomics and Integrative Biology, Delhi 110007, India

Krishan Kumar, Anita Mohan, University School of Basic and Applied Sciences, GGSIP University, Sector-16 C, Dwarka, Delhi 110075, India

Krishan Kumar, Department of Chemistry, Motilal Nehru College, University of Delhi, Delhi 110021, India

Author contributions: Kumar K, Mohan A and Pasha S designed the study; Kumar K performed the majority of experiments; Goyal R, Kumar K and Pasha S analyzed the data; Kumar K wrote the first draft of manuscript; Goyal R and Mudgal A contributed to the final version of the manuscript.

Supported by Council of Scientific and Industrial Research, Delhi

Correspondence to: Dr. Santosh Pasha, Scientist “G”, Peptide Synthesis Laboratory, Institute of Genomics and Integrative Biology, Mall Road, Delhi 110007, India. spasha@igib.res.in

Telephone: +91-11-27667439 Fax: +91-11-27667471

Received: April 19, 2011
Revised: June 16, 2011
Accepted: June 23, 2011
Published online: October 28, 2011

Abstract

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 norbinaltorphimine norBNI.

RESULTS: YFa did not demonstrate significant inhibition of GPI muscle contraction as compared with morphine (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 gastrointestinal transit. The study provides evidences for the involvement of κ and anti-opioid receptors in smooth muscle contraction.

Keywords: Opioid receptor, Guinea pig ileum, Mouse vas deferens, Smooth muscle contraction, Gastrointestinal motility