Effects of novel 5-HT1A receptor antagonists on measures of postsynaptic 5-HT1A receptor activation in vivo |
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| Affiliation: | 1. Department of Pharmacology, University of Texas Health Science Center at San Antonio, USA;2. Department of Veterans Affairs Medical Center, San Antonio, TX, USA;1. Division of Clinical Pharmacology and Toxicology, Department of Biomedicine, University Hospital Basel and University of Basel, Basel, Switzerland;2. Neuroscience Research, pRED, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd, Basel, Switzerland;1. Department of Occupational Health Engineering, Iranshahr University of Medical Sciences, Iranshahr, Iran;2. Department of Occupational Health Engineering, School of Public Health, Iran University of Medical Sciences, Tehran, Iran;3. Department of Occupational Health Engineering, Occupational Health Research Center, Qom University of Medical Sciences, Qom, Iran;4. Department of Biostatistics, School of Public Health, Iran University of Medical Sciences, Tehran, Iran;1. Xfi Centre for Finance and Investment, University of Exeter Business School, Rennes Drive, Exeter EX4 4ST, UK;2. Xfi Centre for Finance and Investment, University of Exeter Business School, Rennes Drive, Exeter EX4 4PU, UK;1. Department of Psychiatry, University of California San Diego, La Jolla, CA, United States;2. Research Service, VA San Diego Healthcare System, San Diego, CA, United States |
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| Abstract: | The effects of two putative 5-HT1A antagonists, 4-(2′-methoxyphenyl)-1-[2′-[N-(2″-pyridinyl)-p-iodobenzamido]ethyl]piperazine (p-MPPI) and 4-(2′-methoxyphenyl)-1-[2′-[N-(2″-pyridinyl)-p-flourobenzamido]ethyl]piperazine (p-MPPF), were examined in vivo in two tests of postsynaptic 5-HT1A receptor activation, hypothermia and reciprocal forepaw treading, in the rat. Both p-MPPI (10 mg/Kg, I.p.) and p-MPPF (10 mg/Kg, I.p.) antagonized the hypothermia induced by the 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) (0.5 mg/Kg, S.c.). Neither p-MPPI nor p-MPPF administered alone at a dose of 10 mg/kg (i.p.) induced hypothermia. Similarly, both p-MPPI (10 mg/Kg, I.p.) and p-MPPF (2.5 mg/Kg, I.p.) completely antagonized 8-OH-DPAT (2 mg/Kg, S.c.)-induced forepaw treading in rats pretreated with reserpine (1 mg/Kg, S.c., 18–24 hours prior to the experiment). p-MPPI and p-MPPF, at doses of 10 mg/kg (i.p.) did not induce forepaw treading in reserpine pretreated animals. The results of the present study demonstrate that p-MPPI and p-MPPF act as 5-HT1A receptor antagonists in these measures of postsynaptic 5-HT1A a receptor activation. |
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