5-HT Receptors and Temperature Homeostasis
Abstract
:1. 5-HT1A Receptor
2. 5-HT2 Receptors
3. 5-HT3 Receptor
4. 5-HT7 Receptor
5. General Discussion and Conclusions
Funding
Institutional Review Board Statement
Informed Consent Statement
Acknowledgments
Conflicts of Interest
References
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Maximal Hypothermic Effect (°C) | Time of Its Achievements (min) | Object | Dose of 8-OH-DPAT | Route of Administration | References |
---|---|---|---|---|---|
3.5 | 10 | C57/B16 mice | 3.0 µg | i.c.v. | [54] |
2.2 | 30 | 0.5 mg/kg | s.c. | ||
2.9 | 30 | 2.5 mg/kg | |||
3 | 18 | 5.0 mg/kg | |||
3 | 18 | 10.0 mg/kg | |||
2.4 | 30 | Sprague-Dawley rats | 0.03–0.1 mg/kg | s.c. | [55] |
3 | 30 | Sprague-Dawley rats | 0.3 mg/kg | s.c. | [56] |
3 | 15 | C57Bl6 mice | 5 mg/kg | s.c. | [57] |
3.5 | 10 | 2 µg | i.c.v. | ||
2 | 30 | Sprague-Dawley rats | 0.3 mg/kg | s.c. | [58] |
2.5 | 30 | Sprague-Dawley rats | 1 mg/kg | s.c. | [59] |
2.5 | 10 | Hooded Lister rats | 2500 ng | into DRN | [60] |
0.5 | 60 | Wistar rats | 0.125 mg/kg | s.c. | [61] |
0.9 | 30 | 0.25 mg/kg | |||
1.5 | 60 | 0.5 mg/kg | |||
1.3 | 30 | Sprague-Dawley rats | 0.1 mg/kg | s.c. | [62] |
1.6 | 10 | ICR mice | 0.25mg/kg | s.c. | [63] |
3.0 | 15–30 | Female albino Tuck (T/O strain) mice | 3.0 mg/kg | s.c. | [64] |
2.3 | 30 | Sprague-Dawley rats | |||
1.3 | 20 | Wistar rats | 5 µg | into DRN | [9] |
no effect | into MRN | ||||
2.5 | 15 | Swiss-Webster mice | 2 mg/kg | s.c. | [65] |
2 | 20 | C57/Bl/6Ola mice | 5.0 mg/kg | s.c. | [66] |
1.3 | 0.5 mg/kg | ||||
2.5 | 30 | Wistar rats | 0.5 mg/kg | s.c. | [67] |
2 | 15–30 | Sprague-Dawley rats | 0.25 mg/kg | s.c. | [68] |
2.8 | 15–30 | T/O mice female | 0.5 mg/kg | ||
1.5 | 30 | Wistar rats | 0.3 mg/kg | s.c. | [69] |
4 | 20 | C57/Bl6Htr1a (+/+) | 1 mg/kg | s.c. | [70] |
3.3 | C57/Bl6 Htr1a (−/+) | ||||
no effect | C57/Bl6 Htr1a (−/−) | ||||
1.2 | C57/Bl6 Htr1a (+/+) | 0.2 mg/kg | |||
1.3 | C57/Bl6 Htr1a (−/+) | ||||
no effect | C57/Bl6 Htr1a (−/−) | ||||
5 | 45 | rats HDS * | 0.5 mg/kg | s.c. | [45] |
1.2 | rats RDS * | ||||
0.7 | rats LDS * | ||||
2.5 | 30 | rats HDS * | 20 µg | i.c.v. | |
no effect | rats LDS * | ||||
1.27 | 90 | Sprague-Dawley rats | 500 µg/kg | s.c. | [71] |
1.15 | 0.5 µg | into the hypothalamus | |||
1.6 | 30 | Sprague-Dawley rats | 0.05 mg/kg | s.c. | [72] |
3.5 | 0.1 mg/kg | ||||
2 | 30 | Sprague-Dawley rats | 0.1 mg/kg | i.p. | [50] |
3 | 0.3 mg/kg | ||||
3.5 | 1 mg/kg | ||||
2.1 | 30 | ♀♂mice 129rSv WT | 0.2 mg/kg | s.c. | [73] |
3.1 | 30 | ♀♂ Htr1b KO mice | 0.6 mg/kg | ||
2.5 | 30 | Sprague-Dawley rats | 0.1 mg/kg | s.c. | [74] |
2 | 30 | Sprague-Dawley rats | 0.3 mg/kg | i.p. | [75] |
0.5 | 30 | C57BL/6J mice | 0.3 mg/kg | i.p. | |
1.2 | 0.6 mg/kg | ||||
1.5 | 0.1 mg/kg | ||||
1.58 | 30 | non aggressive rats | 0.5 mg/kg | i.p. | [47] |
no effect | aggressive rats | ||||
no effect | 30 | aggressive rats | 0.5 mg/kg | i.p. | [76] |
2.2 | non-aggressive rats | ||||
0.75 | 20 | Tg8 mice | 2 mg/kg | i.p. | |
2 | C3H mice | ||||
1.75 | 20 | CBA/Lac mice | 0.5 mg/kg | i.p. | [48] |
2.25 | 1 mg/kg | ||||
no effect | 20 | AKR mice | 0.5 mg/kg1 mg/kg | ||
1.4 | 30 | Sprague-Dawley rats | 0.2 mg/kg | i.p. | [77] |
1.57 | 10–20 | CBA/Lac mice | 1 mg/kg | i.n. | [78] |
1.1 | i.p. | ||||
1.9 | s.c. | ||||
0.71 | DBA/2 mice | i.n. | |||
1.37 | i.p. | ||||
1.44 | s.c. | ||||
1.8 | PT mice | i.n. | |||
1.91 | i.p. | ||||
0.98 | C57Bl mice | i.n. | |||
0.67 | i.p. | ||||
2.62 | s.c. | ||||
1.2 | 20 | CBA/Lac mice | 1 mg/kg | i.p. | [79] |
1 | C57/Bl6 mice | ||||
1 | DBA/2 mice | ||||
2.2 | BALB/C mice | ||||
0.5 | AKR mice | ||||
0.5 | ICR mice | ||||
3 | 20 | 1A-High mice | 0.5 mg/kg | i.p. | [51] |
1 | 10 | 1A-Low mice | |||
2.25 | 20 | CBA mice | 1 mg/kg | i.p. | [49] |
2.5 | ASC mice | ||||
0.4ns | AKR mice | ||||
1.25 | AKR.CBA-D13Mit76C mice | ||||
2.5 | 30 | CBA/Lac mice | 40 nM | i.c.v. | [80] |
1.2 | 20 | CBA/Lac mice | 1 mg/kg | i.p. | [30] |
0.9 | C57/Bl6 mice | ||||
0.9 | DBA/2 mice | ||||
2.2 | BALB/C mice | ||||
0.5ns | AKR mice | ||||
0.5ns | ICR mice | ||||
1.2 | C3H mice | ||||
2.6 | Asn mice | ||||
3 | 20 | WT mice | 0.5 mg/kg | i.p. | [52] |
1.3 | KO Htr1a in DRN | ||||
1.5 | 20 | ♂ WT mice | 0.75 mg/kg | i.p. | [53] |
1.75 | ♀ WT mice | ||||
no effect | 1AcKO mice ♂♀ |
Conclusion | Argumentation | Object | References |
---|---|---|---|
Pre- | Hypothermic effect of 8-OH-DPAT was attenuated when 5-HT was depleted by repeated i.p. administration of pCPA or by injection of 5,7-DHT into the third ventricle | C57/B16/0la mice | [54] |
Post- | After pretreatment by pCPA the minimal dose of 8-OH-DPAT (0.03 mg/kg s.c.), ineffective earlier, deveined effective. It may be the result of receptor sensitization that appeared after pCPA reducing of the whole brain 5-HT level. | Sprague-Dawley rats | [55] |
Pre- | Hypothermic effect of 8-OH-DPAT was attenuated when 5-HT was depleted by repeated i.p. administration of pCPA or by injection of 5,7-DHT into the third ventricle | Sprague-Dawley rat | [58] |
Post- | pCPA tended to increase the hypothermic effect of 8-OH-DPAT (−3 °C in comparing with −2,5 °C) | Sprague-Dawley rats | [59] |
Post- | pCPA tended to increase the hypothermic effect of 8-OH-DPAT | ddY mice | [85] |
Pre- | Lesioning of central 5-HT neurones by 5,7-DHT abolished the hypothermic response to 8-OH-DPAT. Depletion of brain 5-HT levels with p-CPA markedly attenuated the hypothermic response. | Female albino Tuck (T/O strain) mice | [64] |
Post- | Lesioning of central 5-HT neurones by 5,7-DHT had no effect on the hypothermic responses to lower doses of 8-OH-DPAT. pCPA significantly increased hypothermic response. | Sprague-Dawley rats | [64] |
Pre- Post-(?) | Injection of 8-OH-DPAT directly into the DRN evoked a clear hypothermic effect. Injection of 8-OH-DPAT directly into the MRN produced no hypothermic effect. | Wistar rat | [9] |
? | pCPA pretreatment reduced the 5-HT level in cortex and hippocampus, but did not affect the hypothermia | Swiss-Webster mice | [65] |
Pre- | Destruction of 5-HT neurones with the neurotoxin 5,7-DHT abolished the hypothermic response to 8-OH-DPAT | C57/Bl/601a mice | [66] |
Post- | Dose–response curve shows that i.c.v. administration of 8-OH-DPAT was more potent than direct injection to the DRN to causing hypothermia. | Sprague-Dawley rats | [81] |
? | Correlation between the severity of hypothermic response to 8-OH-DPAT and radio ligand 5-HT1A binding sites in the brain regions associated with thermoregulation was not found | rats HDS * rats LDS * | [45] |
Post- | Buspirone produced the same significant increase in prolactin and growth hormone (effects mediated by post- 5HT1A receptors) in the tryptophan-depleted state as in the control condition. The degree of hypothermia produced by buspirone was not significantly different in the two experimental conditions. | healthy volunteers humen | [86] |
Pre- | Htr1a auto-KO mice displayed no detectable body temperature decrease in response to 8-OH-DPAT | Genetically modified mice | [53,87] |
Pre- | Htr1a hetero-KO mice displayed a full hypothermic response to 8-OH-DPAT | Genetically modified mice | [87] |
Change in Thermoregulatory Response | Change in Registered Parameter | Ambient Temperature Conditions | Object | Dose and Route of Administration | References |
---|---|---|---|---|---|
↓General metabolism | ↓O2 consumption | Room temperature | rat | 500 µg/kg s.c. | [71] |
rat | 0.5 µg into the hypothalamus | [71] | |||
mice | 40 nM left lateral ventricle | [80] | |||
↓excretion of CO2 increased via leptin injection | rat | 10 mM 60 nL raphe’ pallidus | [113] | ||
↓O2 consumption | Cooling | rat | 4 mg/mL 1 µL Nucleus raphe’ magnus | [120] | |
↓excretion of CO2 | rat | 10 mM 60 nL Rostral raphe’ pallidus | [115] | ||
rat | 100 µg/500 µL i.v. | [114] | |||
rat | 10 mM 60 nL Rostral raphe’ pallidus | [114] | |||
↑Heat loss | ↑skin temperature | Room temperature | rat | 500 µg/kg s.c. | [71] |
rat | 0.5 µg into the hypothalamus | [71] | |||
rat | 0.6 µmol/kg s.c. | [123] | |||
↑peripheral blood flow | rabbit | 0.1 mg/kg i.v. | [98] | ||
↑peripheral blood flow | Cooling | rabbit | 0.1 mg/kg i.v. | [99] | |
rabbit | 3–5 nmol rostral medullary raphe’ | [100] | |||
rat | 0.5 mg/kg, s.c. | [101] | |||
↑skin temperature | piglet | dialysis 30 mM 30 min medullary raphe’ | [122] | ||
rat | 0.6 µmol/kg s.c. | [123] | |||
↓Heat production | ↓BAT temperature increased via leptin injection | Room temperature | rat | 10 mM 60 nL raphe’ pallidus | [113] |
↓shivering, i.e., muscle electrical activity | Cooling | rat | 4 mg/mL 1 µL Nucleus raphe’ magnus | [120] | |
piglet | dialysis 30 mM 30 min medullary raphe’ | [122] | |||
piglet | dialysis 30 mM 30 min paragigantocellularis lateralis | [121] | |||
↓BAT temperature | rat | 10 mM 60 nL Rostral raphe’ pallidus | [115] | ||
rat | 0.5 mg/kg, s.c. | [101] | |||
rat | 100 µg/500 µL i.v. | [114] | |||
rat | 10 mM 60 nL Rostral raphe’ pallidus | [114] |
Compound | Dose and Route of Administration | Temperature Effect (Time of Its Achievement) | Object | Ambient Temperature Conditions | References |
---|---|---|---|---|---|
Effect of 5-HT2A/C agonists | |||||
MK-212 | 0.03; 0.1; mg/kg i.p. | no effect (30′) | Sprague- Dawley rats | 28–29.5 °C | [56] |
1.0 mg/kg i.p. | 0.8 °C (15′) | ||||
0.83 °C (30′) | |||||
3.0 mg/kg i.p. | 1.1 °C (30′) | ||||
MK-212 | 2.5 mg/kg i.p | 1.4 °C (30′) | Sprague- Dawley rats | 29 °C | [62] |
mCPP | 1.25 mg/kg i.p. | 0.5 °C (30′) | Wistar rats | 25 °C | [158] |
2.5 mg/kg i.p. | 0.75 °C (15′); | ||||
1.1 °C (30′); | |||||
1.1 °C (45′) | |||||
5 mg/kg i.p. | 0.75 °C (15′); | ||||
1.1 °C (30′); | |||||
1.2 °C (45′); | |||||
1.3 °C (60′); | |||||
1.3 °C (90′) | |||||
mCPP | 0.5 mg/kg oral | 0.48 °C (≈190′) | Health volunteers | [159] | |
0.1 mg/kg i.v. | 0.32 °C (≈57′) | ||||
DOI | 0.1 mg/kg i.p. | 0.4 °C (30′) | Sprague- Dawley rats | 29 °C | [160] |
0.3 mg/kg i.p | 1.3 °C (30′) | ||||
1.0 mg/kg i.p. | 1.8 °C (30′) | ||||
DOI | 3 mg/kg s.c. | 1.5 °C (30′) | Sprague- Dawley rats | 20 °C | [161] |
DOI | 0.8 mg/kg i.v. | 0.9 °C (5′); 1.5 °C (10′); 2 °C (15′); 2.5 °C (20′); 3 °C (30′) Malignant hyperthermia | pigs | [162] | |
TFMPP | 1 mg/kg i.p. | 0.7 °C (30′); 0.6 °C (60′); | Wistar rats | 28 °C | [163] |
5 mg/kg i.p. | 0.9 °C (30′); 1.0 °C (60′); 0.9 °C (90′); 0.6 °C (120′); | ||||
10 mg/kg i.p. | 1.0 °C (30′); 1.3 °C (60′); 1.4 °C (90′); 1.1 °C (120′); | ||||
20 mg/kg i.p. | 0.8 °C (30′); 1.1 °C (60′); 1.3 °C (90′); 1.3 °C (120′); | ||||
mCPP | 1 mg/kg i.p. | 0.6 °C (60′); −0.5 °C (90′) | |||
5 mg/kg i.p. | 0.6 °C (60′); 0.9 °C (90′) | ||||
10 mg/kg i.p. | 1.1 °C (30′); 1.2 °C (60′); | ||||
1.1 °C (90′); 0.9 °C (120′); | |||||
20 mg/kg i.p. | 1.3 °C (30′); 1.3 °C (60′); 1.2 °C (90′); 1.2 °C (120′); | ||||
DOI | 1 mg/kg i.p. | 1.5 °C (60′) | Wistar rats | 21 °C | [164] |
DOI | 2.5 mg/kg i.p. | 1.5 °C (60′) | Wistar rats | 22 °C | [165] |
0.6 °C (60′) | Fawn- Hooded rats | ||||
mCPP | 2.5 mg/kg i.p. | 1 °C (30′) | Wistar rats | ||
0.3 °C (30′) | Fawn- Hooded rats | ||||
mCPP | 2.5 mg/kg i.p. | 1.2 °C (30′) | Wistar rats | 21 °C | [166] |
0.4 °C (60′) | Fawn- Hooded rats | ||||
1.25 mg/kg i.p. | 0.5 °C (30′) | Wistar rats | |||
no effect | Fawn- Hooded rats | ||||
DOI | 2.5 mg/kg i.p. | 2 °C (60′) | Wistar rats | [167] | |
mCPP | 1.2 °C (30′) | ||||
DOI | 1 mg/kg s.c. | 1.2 °C (30′) | Wistar rats | 23 °C | [69] |
DOI | Intrahypothalamic administration 0.2 µg | 1.38 °C (45′) | Sprague- Dawley rats | room temperature | [71] |
DOI | 0.025; 0.1 mg/kg s.c. | no effect (20′) | Sprague- Dawley rats | 21 °C | [168] |
0.4; 1.6 mg/kg s.c. | 1.0 °C (20′) | ||||
DOI | 5 µg/kg i.v. | 0.25 °C (20′–60′) | rabbits | 23–25 °C | [169] |
50 µg/kg i.v. | 1.0 °C (40′–60′) | ||||
100 µg/kg i.v. | >2 °C (90′–120′) | ||||
100 µg/kg s.c. | 1.0 °C (90′) | Sprague- Dawley rats | 27 °C | ||
YM348 | 0.3 mg/kg per os | 0.9 °C (60′) | Zucker rats | [170] | |
1 mg/kg per os | 1.1 °C (60′) | ||||
3 mg/kg per os | 1.3 °C (60′) | ||||
DOI | 0.1 mg/kg s.c. | 1.4 °C (30′) | Sprague- Dawley rats | 25–28 °C | [101] |
DOI | 0.05 mg/kg s.c. | 0.29 °C ns | Sprague- Dawley rats | 22 °C | [171] |
0.1 mg/kg s.c;. | 0.64 °C (30′; 45′; 60′) | ||||
0.5 mg/kg s.c. | 0.79 °C (15′; 30′; 45′; 60′; 90′) | ||||
0.05 mg/kg s.c. | 0.5 °C ns | 32 °C | |||
0.1 mg/kg s.c. | 0.5 °C (15′); 1.7 °C (75′) | ||||
0.5 mg/kg s.c. | 1.2 °C (15′); 2.7 °C (75′) | ||||
0.1 mg/kg s.c. | 0.1°C ns | 12 °C | |||
0.1 mg/kg s.c. | 0.99 °C (30′; 45′; 60′) | 27 °C | |||
25B-NBOMe | 0.25 mg/kg i.p. | no effect | Sprague- Dawley rats | 23 °C | [172] |
0.25 mg/kg i.p. | 0.8 °C (30′); 1 °C (60′); 1.2 °C (90′); 0.9 °C (120′) | 29 °C | |||
Effect of 5-HT2A/C antagonists | |||||
pirenpirone | 0.01; 0.03; 0.1; 0.3 mg/kg i.p. | −0.15 °C ?s; −0.5 °C; −0.85 °C; −0.9 °C (<60′) | Sprague- Dawley rats | 28–29.5 °C | [56] |
ketanserin | 0.1; 0.3; 1; 3 mg/kg i.p. | −0.2 °C ?s; −0.5 °C; −0.7 °C; −1.2 °C (<60′) | |||
ritanserin | 0.63 mg/kg i.p. | no effect | Wistar rats | 25 °C | [158] |
ritanserin | 0.5; 1; 2 mg/kg i.p | no effect alone, but dose-dependently reduces hyperthermic effect of mCPP and TFMPP | Wistar rats | 28 °C | [163] |
ketanserin | 0.6; 1.25; 2.5 mg/kg i.p | ||||
LY53857 | 1 mg/kg i.p. | −0.55 °C (90′) | Wistar rats | 21 °C | [164] |
ketanserin | 1 mg/kg i.p. | no effect | |||
ritanserin | 1 mg/kg s.c. | no effect (30′) | Sprague- Dawley rats | 21 °C | [168] |
amperozide | 2 mg/kg s.c. | no effect (30′) | |||
ketanserin | 5 mg/kg i.p | no effect | Sprague- Dawley rats | 22 °C | [171] |
no effect alone, but blocks DOI | 32 °C | ||||
ketanserin | 0.2 µg into preoptic anterior hypothalamus | 0.58 °C (180′) | rabbit | 2 °C | [173] |
0.54 °C (180′) | 22 °C | ||||
0.57 °C (180′) | 32°C | ||||
0.4 µg into preoptic anterior hypothalamus | 1.13 °C (180′) | 2 °C | |||
1.0 °C (180′) * | 22 °C | ||||
1.09 °C (180′) | 32 °C | ||||
2 µg into preoptic anterior hypothalamus | 1.42 °C (180′) | 2 °C | |||
1.37 °C (180′) | 22 °C | ||||
1.43 °C (180′) | 32°C |
Compound | Dose and route of Administration | Temperature Effect (Time of Its Achievement) | Object | Ambient Temperature Conditions | References |
---|---|---|---|---|---|
Effect of 5-HT2A/C agonists | |||||
TFMPP | 1 mg/kg s.c. | no effect alone(10′), but reduces the effect of 8-OH-DPAT | ICR | 21 °C | [63] |
mCPP | |||||
MK-212 | |||||
DOI | 0.1 mg/kg s.c. | ||||
MK-212 | |||||
DOI | 0.5, 1.0, 2.5 mg/kg i.p. | no effect (15′, 30′, 45′, 60′, 90′, 120′) | ICR | 24 °C | [174] |
5 mg/kg i.p. | −1 °C (30′, 45′, 60′, 90′) | ||||
DOI | 1 mg/kg i.p; 5 mg/kg i.p. | no effect | Ddy | 24 °C | [175] |
DV-7028 | 10 mg/kg per os | ||||
TCB-2 | 0.1; 0.5; 1.0; 2.5; mg/kg i.p. | no effect (15′, 30′, 45′) | C57Bl6J | plexiglass containers 20 °C | [176] |
5.0 mg/kg i.p. | −4 °C ( ‘) | ||||
DOI | 0.1; 0.5; 1.0; 2.5; 5.0 mg/kg i.p. | no effect (15′, 30′, 45′) | |||
DOI | 1 mg/kg i.p. | no effect (each 5′ over 24 h) | C57BL/6J | 22.5–23.5 °C | [177] |
25CN-NBOH | 1.5 mg/kg, s.c. | no effect | Mice Mix genetic background | Temperature of heat-pad = 37 °C | [178] |
1 °C (15′) | Temperature of heat-pad = 41 °C | ||||
Effect of 5-HT2A/C antagonists | |||||
ritanserin | 1 mg/kg per os 10 mg/kg per os | no effect | Ddy | 24 °C | [175] |
ketanserin | 1 mg/kg per os | no effect | |||
10 mg/kg per os | −2.2 °C (60′) | ||||
MDL 11,939 | (1.0 mg/kg), i.p. | no effect (30′) | C57Bl6J | [176] | |
ketanserin | 1.0 mg/kg i.p. (180 µM). | −2 °C | CBA/Lac | [179] | |
2.0 mg/kg i.p. (360 µM) | −2.3 °C | ||||
20 nM i.c.v. | −2.3 °C | ||||
40 nM i.c.v. | −3.5 °C | ||||
ketanserin | 1 mg/kg i.p. | no effect (each 5′ over 24 h) | C57BL/6J | 22.5–23.5 °C | [177] |
40 nmol i.c.v. | no effect (60′) | ||||
ketanserin | 1 mg/kg i.p. | no effect (60′) | AKR/J | [180] | |
CBA/Lac | |||||
AKR.CBA- D13Mit76 |
Change in Thermoregulatory Response | Change in Registered Parameter | Ambient Temperature Conditions | Object | Ligand (Dose and Route of Administration) | Reference |
---|---|---|---|---|---|
↑General metabolism | ↑O2 consumption | Room temperature | Sprague- Dawley rat | DOI (0.2 µg into the hypothalamus) | [71] |
↑O2 consumption; CO2 excretion | Zucker fa/fa rats | YM348 (0.3; 1; 3 mg/kg per os) | [170] | ||
↑ Heat production | ↑BAT temperature | 25–28 °C | Sprague- Dawley rat | DOI (0.1 mg/kg s.c) | [101] |
↑BAT temperature | 29 °C | Sprague- Dawley rat | 25B-NBOMe (0.25 mg/kg i.p.) | [172] | |
↓Heat loss | ↓skin temperature | Room temperature | Sprague- Dawley rat | DOI (0.2 µg into the hypothalamus) | [71] |
↓peripheral blood flow | 23–25 °C | Rabbits | DOI (5; 50; 100 µg/kg, i.v.) | [169] | |
27 °C | Sprague- Dawley rat | DOI (100 µg/kg s.c.) | |||
↓peripheral blood flow | rabbits | DOI (50 µg/kg, i.v.) | [183] | ||
↓peripheral blood flow | 25–28 °C | Sprague- Dawley rat | DOI (0.1 mg/kg s.c) | [101] | |
↓skin temperature | 29 °C | Sprague- Dawley rat | 25B-NBOMe (0.25 mg/kg i.p.) | [172] |
Compound | Dose (Route of Administration) | Maximal Effect (°C) | Time of Its Achievements | Object | References |
---|---|---|---|---|---|
mCPBG | 0.1 mg/kg (i.p.) | no effect | Wistar rats | [218] | |
1 mg/kg (i.p.) | 0.5 | ≈30′ | |||
10 mg/kg (i.p.) | 0.6 | ≈30′ | |||
MDL72222 | 0.1; 1; 10 mg/kg (i.p.) | no effect | |||
ondansetron | 0.1; 1 mg/kg(i.p.) | no effect | |||
2-Me-5-HT | 5 µg (i.c.v.) | ≈−0.62 | 45′ | Sprague- Dawley rats | [219] |
10 µg (i.c.v.) | −1.1 | 45′ | |||
20 µg (i.c.v.) | −1.5 | 45′ | |||
1–5 mg/kg (i.p.) | no effect | During 2 h | |||
ondansetron | 5, 10, 20 µg (i.c.v.) | no effect | During 150′ | ||
50, 100, 300 mg/kg (i.p.) | no effect | ||||
tropisetron | 50, 100, 300 mg/kg (i.p.) | no effect | |||
5, 10, 20 µg (i.c.v.) | no effect | ||||
2-Me-5-HT | 4 mg/kg (i.p.) | no effect | During 6 h | Sprague- Dawley rats | [220] |
mCPBG | 160 nmol (i.c.v.) | −4 | 30′ | AKR/J mice | [79] |
80 nmol (i.c.v.) | −2 | ||||
40 nmol (i.c.v.) | −2 | ||||
20 nmol (i.c.v.) | no effect | ||||
0.5; 1; 5; 10 mg/kg (i.p.) | no effect | ||||
mCPBG | 40 nmol (i.c.v.) | −4 | 30′ | DBA/2J mice | |
−5.5 | CBA/Lac mice | ||||
−2.6 | AKR/J mice | ||||
−5.1 | C57Bl/6 mice | ||||
−3.1 | BALB/c mice | ||||
−3.2 | ICR mice | ||||
mCPBG | 40 nmol (i.c.v.) | −2.3 | 30′ | CBA/Lac mice | [80] |
mCPBG | 40 nmol (i.c.v.) | −5 | 30′ | C57Bl/6 mice | [30] |
−5 | C3H mice | ||||
−4 | DBA mice | ||||
−5.9 | Asn mice | ||||
−3 | BALB mice | ||||
−5.1 | CBA mice | ||||
−3.2 | ICR mice | ||||
−2.5 | AKR mice |
Hypothermia-Inducing Compound | Dosa (mg/kg) | ΔT Body (Time of Effect) | Object | Reference |
---|---|---|---|---|
5-HT | 5 | −3.1 °C (30′) | WT | [242] |
−2 °C (60′) | ||||
no change | Htr7 KO | |||
5-CT | 0.5 | −2 °C (30′) | WT | |
3 | −4.5 °C (120′) | |||
0.5 | no change | Htr7 KO | ||
3 | −1.2 °C (120′) | |||
5-CT | 0.1 | −1.2 °C ns | WT | [241] |
0.3 | −2.8 °C | |||
1 | −3.9 °C | |||
0.1; 0.3; 1 | no change | Htr7 KO * | ||
8-OH-DPAT | 0.3 | −0.7 °C (30′) | WT | [75] |
0.6 | −1.2 °C (30′) | |||
1 | −1.5 °C (30′) | |||
0.3 | no change | Htr7 KO | ||
0.6 | no change | |||
1 | −1.1 °C (30′) |
Pretreatment | Main Hypothermic Effect | Joint Effect of Two Compaunds ΔT Body | Object | References | ||||
---|---|---|---|---|---|---|---|---|
Pretreatment Compound | Dose (Route of Administration) | Time Interval | Compound | Dose (Route of Administration) | ΔT body (Time of Effect) | |||
5-CT | 0.3 mg/kg (i.p.) | −1.8 °C (75′) | Guinea pig | [239] | ||||
SB-269970-A | 3 mg/kg (i.p.) | 60′ | 5-CT | −0.4 °C | ||||
5-CT | 0.3 mg/kg (i.p.) | −1.9 °C | Guinea pig | [240] | ||||
SB-656104-A | 3 mg/kg (i.p.) | 60′ | 5-CT | −0.7 °C | ||||
5-CT | 0.3 mg/kg (i.p.) | ≈−1.8 °C | Swiss Webster mice | [241] | ||||
WAY100635 | 0.1; 0.3; 1 mg/kg (i.p.) | 30′ | 5-CT | 0.3 mg/kg (i.p.) | ≈−1.4 °C | |||
SB 258719 | 5; 10 mg/kg (i.p.) | 30′ | 5-CT | 0.3 mg/kg (i.p.) | ≈−1.7 °C | |||
20 mg/kg (i.p.) | ≈−0.2 °C | |||||||
SB-269970 | 1 mg/kg (i.p.) | 30′ | 5-CT | 0.3 mg/kg (i.p.) | −1.2 °C | |||
3 mg/kg (i.p.) | −0.6 °C | |||||||
10; 30 mg/kg (i.p.) | −0.4 °C | |||||||
8-OH-DPAT | 0.3 mg/kg (i.p.) | -2°C (30′) | Sprague–Dawley rats | [75] | ||||
WAY-100135 | 1 mg/kg (i.p.) | 20′ | 8-OH-DPAT | 0.3 mg/kg (i.p.) | −1.6 °C | |||
10 mg/kg (i.p.) | −0.5 °C | |||||||
SB-269970 | 0.3 mg/kg (i.p.) | 20′ | −1.2 °C | |||||
3 mg/kg (i.p.) | −1.1 °C | |||||||
DR-4004 | 3 mg/kg (i.p.) | 20′ | −1.2 °C | |||||
10 mg/kg (i.p.) | −1.1 °C | |||||||
8-OH-DPAT | 0.3 mg/kg (i.p.) | −0.7 °C (30′) | C57Bl6+/+ | |||||
0.6 mg/kg (i.p.) | −1.2 °C (30′) | |||||||
1 mg/kg (i.p.) | −1.5 °C (30′) | |||||||
0.3 mg/kg (i.p.) | no change | C57Bl6−/− | ||||||
0.6 mg/kg (i.p.) | no change | |||||||
1 mg/kg (i.p.) | −1.1 °C (30′) | |||||||
WAY-100135 | 10 mg/kg (i.p.) | 30′ | 8-OH-DPAT | 0.3 mg/kg (i.p.); 0.6mg/kg (i.p.); 1 mg/kg (i.p.) | no change | C57Bl6+/+ | ||
no change | C57Bl6−/− | |||||||
SB-269970 | 10 mg/kg (i.p.) | 30′ | 8-OH-DPAT | 0.3 mg/kg (i.p.) | no change | C57Bl6+/+ | ||
0.6 mg/kg (i.p.) | −0.7 °C (30′) | |||||||
1 mg/kg (i.p.) | −1.9 °C (30′) | |||||||
0.3 mg/kg (i.p.) | no change | C57Bl6−/− | ||||||
0.6 mg/kg (i.p.) | −0.6 °C (30′) | |||||||
1 mg/kg (i.p.) | −1.2 °C (30′) | |||||||
8-OH-DPAT | 0.1 mg/kg (s.c.) | −3.4 °C (30′) | Sprague–Dawley rats | [245] | ||||
WAY-100635 | 0.005 mg/kg, s.c.) | 8-OH-DPAT | −2 °C | |||||
SB-269970 | 0.1 mg/kg (i.p.) | 8-OH-DPAT | −3.4 °C | |||||
0.5 mg/kg (i.p.) | −2.7 °C | |||||||
1 mg/kg (i.p.) | −2.3 °C | |||||||
WAY-100635 (0.005 mg/kg, s.c.) + SB-269970(1 mg/kg, i.p.) | 8-OH-DPAT | −1 °C |
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Voronova, I.P. 5-HT Receptors and Temperature Homeostasis. Biomolecules 2021, 11, 1914. https://doi.org/10.3390/biom11121914
Voronova IP. 5-HT Receptors and Temperature Homeostasis. Biomolecules. 2021; 11(12):1914. https://doi.org/10.3390/biom11121914
Chicago/Turabian StyleVoronova, Irina P. 2021. "5-HT Receptors and Temperature Homeostasis" Biomolecules 11, no. 12: 1914. https://doi.org/10.3390/biom11121914