PMID- 33390452 OWN - NLM STAT- MEDLINE DCOM- 20210215 LR - 20210215 IS - 1347-5231 (Electronic) IS - 0031-6903 (Linking) VI - 141 IP - 1 DP - 2021 TI - [Effects of Histamine and Related Compounds on the Central Nervous System]. PG - 93-110 LID - 10.1248/yakushi.20-00197 [doi] AB - There has been little information about the role of histamine on the central nervous system (CNS), different from dopamine and serotonin. In the present study, therefore, the effects of histamine and related compounds on the CNS were studied using rats. Intracerebroventricular (i.c.v.) injection of histamine and 2-methylhistamine ameliorated memory deficit after long interrution of learning in active avoidance response. First generation H(1)-antagonists inhibited active avoidance response, whereas newly develpoed H(1)-antagonists showed little effect. alpha-Fluoromethylhistidine, an histidine decarboxylase inhibitor, also inhibited active avoidance response. In radial maze performance, almost the same findings were obtained. I.c.v. injection of histamine and H(1)-agonists inhibited amygdaloid kindled seizures. First generation H(1)-antagonists attenuated histamine-induced inhibition of amygdaloid kindled seizures. Both i.c.v. and intraperitoneal injections of H(3)-antagonist, thioperamide, resulted in a dose-related inhibition of amygdaloid kindled seizures. The effect of thioperamide was inhibited by an H(3)-agonists and H(1)-antagonists. Similar to nitrazepam, diphenhydramine and chlorpheniramine caused a shortening of sleep latency. On the other hand, no significant effects were observed with second generation H(1)-antagonists. These findings suggest that histamine plays an important role in learning and memory via H(1)-receptors, an inhibition of amygdaloid kindled seizures induced by histamine occurred through not only H(1)-receptors but also H(3)-receptors, and that classic H(1)-antagonists can be useful as a effective hypnotic for difficulty in falling asleep. FAU - Kamei, Chiaki AU - Kamei C AD - Department of Pharmacology, Faculty of Pharmaceutical Sciences, Yasuda Women's University. AD - Department of Medicinal Pharmacology, Graduate School of Medicine Dentistry and Pharmaceutical Sciences, Okayama University. LA - jpn PT - Journal Article PT - Review PL - Japan TA - Yakugaku Zasshi JT - Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan JID - 0413613 RN - 0 (Histamine H1 Antagonists) RN - 0 (Hypnotics and Sedatives) RN - 0 (Methylhistamines) RN - 0 (Methylhistidines) RN - 0 (Receptors, Histamine H3) RN - 70050-43-0 (alpha-fluoromethylhistidine) RN - 820484N8I3 (Histamine) RN - H5DHG2WBHM (2-methylhistamine) SB - IM MH - Animals MH - Avoidance Learning/drug effects MH - Central Nervous System/*drug effects MH - Histamine/administration & dosage/metabolism/*pharmacology/physiology MH - Histamine H1 Antagonists/*pharmacology/therapeutic use MH - Humans MH - Hypnotics and Sedatives MH - Injections, Intraventricular MH - Kindling, Neurologic/drug effects MH - Memory Disorders/drug therapy MH - Methylhistamines/administration & dosage/*pharmacology MH - Methylhistidines/administration & dosage/*pharmacology MH - Mice MH - Rats MH - Receptors, Histamine H3/metabolism/physiology MH - Seizures/drug therapy MH - Sleep/drug effects MH - Sleep Initiation and Maintenance Disorders/drug therapy OTO - NOTNLM OT - amygdaloid kindking OT - histamine OT - histamine agonist OT - histamine antagonist OT - learning behavior OT - sleep-wake cycle EDAT- 2021/01/05 06:00 MHDA- 2021/02/16 06:00 CRDT- 2021/01/04 05:24 PHST- 2021/01/04 05:24 [entrez] PHST- 2021/01/05 06:00 [pubmed] PHST- 2021/02/16 06:00 [medline] AID - 10.1248/yakushi.20-00197 [doi] PST - ppublish SO - Yakugaku Zasshi. 2021;141(1):93-110. doi: 10.1248/yakushi.20-00197.