1. Drugs affecting autacoids

2. Autacoids: local hormones
A. Overview
Autacoids: local hormones
one of the regulatory mechanisms in the body

3. neurohormone secretion
neurotrasmitter
hormone secretion
neurohormone secretion

4. gap junction
paracrine 旁分泌
autocrine 自分泌
juxtacrine接触分泌

5. A. Overview Autacoids: Histamine 5-Hydroxytryptamine (serotonin, 5-HT)
Lipid-derived autocoids
Prostaglandins (PGs) Leukotrienes (LTs)
Platelet activating factor (PAF)
Vasoactive peptides
Substance P (SP)；Kinins (bradykinin, etc.)
Angiotensins (AT)；Natriuretic peptides (NP)
Vasoactive intestinal peptide (VIP)
Endothelins (ET)
Calcitonin gene related peptide (CGRP)
Nitric oxide (NO)
Adenosine

6. Lipid-derived autacoids and related drugs
PAF
Lipid-derived autacoids and related drugs
antagonists
inhibitors
antagonists

7. Prostaglandins (PGs)

8. Leukotrienes (LTs): LTB4; LTC4, LTD4, LTE4

9. B. Histamine receptor antagonists
H1 receptor agonists:
Histamine(组胺)
2-methyl histamine(2-甲基组胺)
Betahistine (培他司汀)
H2 receptor agonists:
Betazole (培他唑)
Impromidine(英普咪定)
H3 receptor agonists:
R()-methylhistamine(R ()-甲基组胺)

10. 3 principal physiological effects:
(1) it is a mediator of inflammation (swelling) associated with the immune response (2) it is a chemical that stimulates secretion of gastric acid (3) it is a transmitter amine in both the peripheral and the central nervous systems.

12. B. Histamine receptor antagonists

13. Pioneers in the discovery of histamine and the development of histamine antagonist drug research
Clin Pharmacol Drug Dev Jan;5(1):5-12. doi: /cpdd.236. Review

14. B. Histamine receptor antagonists First Generation agents
苯海拉明
氯苯那敏（扑尔敏）
Clin Pharmacol Drug Dev Jan;5(1):5-12. doi: /cpdd.236. Review

15. B. Histamine receptor antagonists
1. Pharmacological effects
(1) Inhibition of allergic inflammation:
mainly on microvascular leakage
(2) Central depression: diphenhydramine, promethazine (异丙嗪) > chlorpheniramine > astemzole (阿司咪唑，息斯敏)，phenindamine (苯茚胺)：stimulating
(3) Antiemesis: motion sickness
(4) Others: weak muscarinic block, local anesthetic, and quinidine-like effects

16. B. Histamine receptor antagonists
2. Clinical uses
(1) Allergic conditions: symptoms in skin and mucosa
(2) Motion sickness: diphenhydramine (苯海拉明), dimenhydrinate (茶苯海明), promethazine (异丙嗪), meclozine (美克洛嗪)
(3) Sedation and insomnia: using drugs with CNS depression

17. B. Histamine receptor antagonists
3. Adverse effects
(1) CNS depression
(2) GI reactions
(3) Others: arrhythmias, etc.

18. B. Histamine receptor antagonists
Second Generation agents
Alkylamines ( 烷基胺)
Acrivastine(阿伐斯汀)
Piperazines (哌嗪类)
Cetirizine (西替利嗪)
Phthalazinones
Azelastine(氮卓斯汀)
Piperidines
Levocabastine(左卡巴斯汀)
Loratadine(氯雷他定)
Fxofenadine(非索非那定)

19. B. Histamine receptor antagonists Second Generation agents
地氯雷他定
氯雷他定
非索非那定
特非那定
阿伐斯汀
西替利嗪
Clin Pharmacol Drug Dev Jan;5(1):5-12. doi: /cpdd.236. Review

20. B. Histamine receptor antagonists
H2 receptor antagonists
1. Pharmacological effects
(1) Inhibiting gastric acid secretion
(2) Cardiovascular effects: heart stimulating (weaker in therapeutic doses)
(3) Immunosuppressive effects
2. Clinical uses
(1) Peptic ulcers
(2) Adjuvant therapy for cancers
3. Adverse effects
GI, CNS, antiandrogen, etc.

21. H4 R antagonist JNJ 39758979 UR-63325 PF-3893787
toreforant (JNJ )

22. H4 receptor: fromorphantotheclinic. Front. Pharmacol.6:65.

23. Effects of H4R-deficient mice in selected animal models
H4 receptor: fromorphantotheclinic. Front. Pharmacol.6:65.