Protein Information

Name 5 HT 3 receptor
Synonyms 5 HT 3; 5 hydroxytryptamine 3 receptor; serotonin receptor; HTR 3; HTR3; 5 HT3; 5 HT3A; 5 HT3R…

Compound Information

Name copper sulfate
CAS sulfuric acid copper(2+) salt (1:1)

Reference List

PubMed Abstract RScore(About this table)
8282015 Fukui H, Yamamoto M, Sasaki S, Sato S: Involvement of 5-HT3 receptors and vagal afferents in copper sulfate- and cisplatin-induced emesis in monkeys. Eur J Pharmacol. 1993 Nov 2;249(1):13-8.
224(2,4,4,4) Details
8846809 Ito C, Isobe Y, Kijima H, Kiuchi Y, Ohtsuki H, Kawamura R, Tsuchida K, Higuchi S: The anti-emetic activity of GK-128 in Suncus murinus. Eur J Pharmacol. 1995 Oct 4;285(1):37-43.

The 5-HT3 receptor agonist, 2-methyl-5-HT, and copper sulfate also induced emesis of short duration.
84(1,1,1,4) Details
9085045 Minami M, Endo T, Tamakai H, Ogawa T, Hamaue N, Hirafuji M, Monma Y, Yoshioka M, Hagihara K: Antiemetic effects of N-3389, a newly synthesized 5-HT3 and 5-HT4 receptor antagonist, in ferrets. Eur J Pharmacol. 1997 Mar 5;321(3):333-42.

The antiemetic activity of N-3389 (endo-3,9-dimethyl-3,9-diazabicyclo [3,3,1] non-7-yl-1 H-indazole-3-carboxamide dihydrochloride), a new 5-HT3 and 5-HT4 receptor antagonist, against cisplatin-, cyclophosphamide- and copper sulfate-induced emesis was investigated using ferrets.
83(1,1,1,3) Details
16079468 Nakayama H, Yamakuni H, Higaki M, Ishikawa H, Imazumi K, Matsuo M, Mutoh S: Antiemetic activity of FK1052, a 5-HT3- and 5-HT4-receptor antagonist, in Suncus murinus and ferrets. J Pharmacol Sci. 2005 Aug;98(4):396-403. Epub 2005 Jul 29.

We investigated the effect of FK1052 [(+)-8,9-dihydro-10-methyl-7-[(5-methyl-1H-imidazol-4-yl) methyl] pyrido [1,2 -a] indol-6 (7H)-one hydrochloride], a 5-HT3- and 5-HT4-receptor antagonist, on the emesis induced by motion stimuli, copper sulfate, or cisplatin in either Suncus murinus or ferrets and also clarified the role of the 5-HT3 and 5-HT4 receptors in these models.
32(0,1,1,2) Details
8082706 Fukui H, Yamamoto M, Sasaki S, Sato S: Possible involvement of peripheral 5-HT4 receptors in copper sulfate-induced vomiting in dogs. Eur J Pharmacol. 1994 May 12;257(1-2):47-52.

The involvement of visceral afferent fibers and 5-HT3 or 5-HT4 receptors in the vomiting induced by oral administration of copper sulfate was investigated in beagle dogs.
31(0,1,1,1) Details
1548679 Youssefyeh RD, Campbell HF, Airey JE, Klein S, Schnapper M, Powers M, Woodward R, Rodriguez W, Golec S, Studt W, et al.: Development of high-affinity 5-HT3 receptor antagonists. 2. J Med Chem. 1992 Mar 6;35(5):903-11.

However, it was inactive against apomorphine or copper sulfate-induced vomiting.
5(0,0,0,5) Details
2041220 Torii Y, Saito H, Matsuki N: Selective blockade of cytotoxic drug-induced emesis by 5-HT3 receptor antagonists in Suncus murinus. Jpn J Pharmacol. 1991 Jan;55(1):107-13.

Veratrine, nicotine, copper sulfate, cisplatin, cyclophosphamide and motion sickness were used as emetic stimuli.
4(0,0,0,4) Details
12087874 Yamamoto K, Matsunaga S, Matsui M, Takeda N, Yamatodani A: Pica in mice as a new model for the study of emesis. . Methods Find Exp Clin Pharmacol. 2002 Apr;24(3):135-8.

However, emetogenic stimuli such as anticancer drugs, apomorphine, copper sulfate and rotation induced pica, a behavior characterized by eating nonfood substances such as kaolin, in rats.
Cisplatin (5 mg/kg) caused a significant increase in kaolin consumption (saline: 0.15 +/- 0.08 g vs. cisplatin: 0.45 +/- 0.16 g) and pretreatment with the 5-HT3 receptor antagonist, ondansetron (2 mg/kg), suppressed the increased consumption (vehicle: 0.33 +/- 0.05 g vs. ondansetron: 0.13 +/- 0.04 g).
1(0,0,0,1) Details
1972549 Costall B, Domeney AM, Naylor RJ, Owera-Atepo JB, Rudd JA, Tattersall FD: Fluphenazine, ICS 205-930 and dl-fenfluramine differentially antagonise drug-induced emesis in the ferret. Neuropharmacology. 1990 May;29(5):453-62.


The data indicate that dopamine and/or 5-HT3 receptor systems are involved in drug-induced emesis but that emesis caused by gastric irritation induced by copper sulphate is mediated by different receptor mechanisms.
1(0,0,0,1) Details
8415820 Takeda N, Hasegawa S, Morita M, Matsunaga T: Pica in rats is analogous to emesis: an animal model in emesis research. Pharmacol Biochem Behav. 1993 Aug;45(4):817-21.

Oral administration of copper sulfate and intraperitoneal injection of cisplatin also induced dose-dependent kaolin consumption.
These findings suggest that pica in rats was induced through 1) dopamine D2 receptors in the chemoreceptor trigger zone, and 2) the stomach, partly via 5-HT3 receptors in the visceral afferents in the stomach wall.
1(0,0,0,1) Details
10688616 Yamakuni H, Sawai H, Maeda Y, Imazumi K, Sakuma H, Matsuo M, Mutoh S, Seki J: Probable involvement of the 5-hydroxytryptamine (4) receptor in methotrexate-induced delayed emesis in dogs. J Pharmacol Exp Ther. 2000 Mar;292(3):1002-7.

The emetic episodes induced by MTX were also inhibited by another 5-HT (3/4) receptor antagonist, tropisetron (1 mg/kg).
Copper sulfate-induced emesis in dogs was also prevented by FK1052, tropisetron, and CP-122,721 but not by ondansetron.
1(0,0,0,1) Details
9258999 Matsuki N, Wang CH, Okada F, Tamura M, Ikegaya Y, Lin SC, Hsu YN, Chaung LJ, Chen SJ, Saito H: Male/female differences in drug-induced emesis and motion sickness in Suncus murinus. Pharmacol Biochem Behav. 1997 Aug;57(4):721-5.

In order to elucidate possible male/female differences in emesis, the effects of various emetogenic drugs (cisplatin, copper sulfate, veratrine, nicotine, serotonin) and motion stimulus were compared between male and female Suncus murinus.
The ID50 values for tropisetron, a 5-HT3 receptor antagonist, to block serotonin-induced emesis were also similar between male and female animals.
1(0,0,0,1) Details