5-HT1F receptor
5-HT1F receptor (5-hidroksitriptaminski (serotoninski) receptor 1F , HTR1F je 5-HT1 receptor . On je kodiran istoimenim humanim genom .[ 1] [ 2] [ 3] [ 4] [ 5]
Ligandi
Agonisti
5-n -Butirilokis-DMT[ 6] : >60-puta je selektivniji u odnosu na 5-HT1E receptor
BRL-54443 - mešoviti 5-HT1E/1F agonist
Eletriptan - mešoviti 5-HT1B/1D/1E/1F/2B/7 agonist
LY-334,370 [ 7] - kao i srodni benzamidi [ 8]
LY-344,864 (N-[(3R)-3-(Dimetilamino)-2,3,4,9-tetrahidro-1H-karbazol-6-il]-4-fluorobenzamid)
Naratriptan - mešoviti 5-HT1B/1D/1F agonist
Antagonisti
Selektivni antagonisti 5HT1F receptora nisu dostupni.
Povezano
Literatura
↑ „Entrez Gene: HTR1F 5-hydroxytryptamine (serotonin) receptor 1F” .
↑ Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek TA (January 1993). „Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase” . Proc. Natl. Acad. Sci. U.S.A. 90 (2): 408–12. DOI :10.1073/pnas.90.2.408 . PMC 45671 . PMID 8380639 .
↑ Lovenberg TW, Erlander MG, Baron BM, Racke M, Slone AL, Siegel BW, Craft CM, Burns JE, Danielson PE, Sutcliffe JG (March 1993). „Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes” . Proc. Natl. Acad. Sci. U.S.A. 90 (6): 2184–8. DOI :10.1073/pnas.90.6.2184 . PMC 46050 . PMID 8384716 .
↑ Erdmann J, Shimron-Abarbanell D, Shridhar V, Smith DI, Propping P, Nöthen MM (1997). „Assignment of the human serotonin 1F receptor gene (HTR1F) to the short arm of chromosome 3 (3p13-p14.1)”. Mol. Membr. Biol. 14 (3): 133–5. DOI :10.3109/09687689709048173 . PMID 9394293 .
↑ Maassen VanDenBrink A, Vergouwe MN, Ophoff RA, Naylor SL, Dauwerse HG, Saxena PR, Ferrari MD, Frants RR (June 1998). „Chromosomal localization of the 5-HT1F receptor gene: no evidence for involvement in response to sumatriptan in migraine patients”. Am. J. Med. Genet. 77 (5): 415–20. DOI :10.1002/(SICI)1096-8628(19980605)77:5<415::AID-AJMG12>3.0.CO;2-L . PMID 9632173 .
↑ PMID 21422162
↑ Wainscott DB, Krushinski JH, Audia JE, Schaus JM, Zgombick JM, Lucaites VL, Nelson DL (2005). „[3 H]-LY-334,370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties”. Naunyn Schmiedebergs Arch. Pharmacol. 371 (3): 169–77. DOI :10.1007/s00210-005-1035-9 . PMID 15900510 .
↑ Zhang D, Kohlman D, Krushinski J, Liang S, Ying BP, Reilly JE, Dinn SR, Wainscott DB, Nutter S, Gough W, Nelson DL, Schaus JM, Xu YC (2004). „Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists”. Bioorg. Med. Chem. Lett. 14 (24): 6011–6. DOI :10.1016/j.bmcl.2004.09.079 . PMID 15546719 .
Dodatna literatura
Hoyer D, Hannon JP, Martin GR (2002). „Molecular, pharmacological and functional diversity of 5-HT receptors.” . Pharmacol. Biochem. Behav. 71 (4): 533–54. DOI :10.1016/S0091-3057(01)00746-8 . PMID 11888546 .
Raymond JR, Mukhin YV, Gelasco A, et al. (2002). „Multiplicity of mechanisms of serotonin receptor signal transduction.”. Pharmacol. Ther. 92 (2-3): 179–212. DOI :10.1016/S0163-7258(01)00169-3 . PMID 11916537 .
Amlaiky N, Ramboz S, Boschert U, et al. (1992). „Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus.”. J. Biol. Chem. 267 (28): 19761–4. PMID 1328180 .
Adham N, Kao HT, Schecter LE, et al. (1993). „Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.” . Proc. Natl. Acad. Sci. U.S.A. 90 (2): 408–12. DOI :10.1073/pnas.90.2.408 . PMC 45671 . PMID 8380639 .
Lovenberg TW, Erlander MG, Baron BM, et al. (1993). „Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes.” . Proc. Natl. Acad. Sci. U.S.A. 90 (6): 2184–8. DOI :10.1073/pnas.90.6.2184 . PMC 46050 . PMID 8384716 .
Maassen VanDenBrink A, Vergouwe MN, Ophoff RA, et al. (1999). „Chromosomal localization of the 5-HT1F receptor gene: no evidence for involvement in response to sumatriptan in migraine patients.”. Am. J. Med. Genet. 77 (5): 415–20. DOI :10.1002/(SICI)1096-8628(19980605)77:5<415::AID-AJMG12>3.0.CO;2-L . PMID 9632173 .
Strausberg RL, Feingold EA, Grouse LH, et al. (2003). „Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.” . Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. DOI :10.1073/pnas.242603899 . PMC 139241 . PMID 12477932 .
Bhatnagar A, Sheffler DJ, Kroeze WK, et al. (2004). „Caveolin-1 interacts with 5-HT2A serotonin receptors and profoundly modulates the signaling of selected Galphaq-coupled protein receptors.”. J. Biol. Chem. 279 (33): 34614–23. DOI :10.1074/jbc.M404673200 . PMID 15190056 .
Gerhard DS, Wagner L, Feingold EA, et al. (2004). „The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).” . Genome Res. 14 (10B): 2121–7. DOI :10.1101/gr.2596504 . PMC 528928 . PMID 15489334 .
Hannula-Jouppi K, Kaminen-Ahola N, Taipale M, et al. (2006). „The axon guidance receptor gene ROBO1 is a candidate gene for developmental dyslexia.” . PLoS Genet. 1 (4): e50. DOI :10.1371/journal.pgen.0010050 . PMC 1270007 . PMID 16254601 .
Spoljašnje veze
„5-HT1F ” . IUPHAR Database of Receptors and Ion Channels . International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2016-03-03.
Klasa A : Rodopsinu slični
Adenozinski (
A1 ,
A2A ,
A2B ,
A3 ) •
P2Y (
1 ,
2 ,
4 ,
5 ,
6 ,
8 ,
9 ,
10 ,
11 ,
12 ,
13 ,
14 )
Drugi
Acetilholin (
M1 ,
M2 ,
M3 ,
M4 ,
M5 ) •
Dopamin (
D1 ,
D2 ,
D3 ,
D4 ,
D5 ) •
Histamin (
H1 ,
H2 ,
H3 ,
H4 ) •
Melatonin (
1A ,
1B ,
1C ) •
TAAR (
1 ,
2 ,
3 ,
5 ,
6 ,
8 ,
9 )
Metaboliti i signalni molekuli
Drugi
Žučna kiselina •
Kanabinoidni (
CB1 ,
CB2 ,
GPR (
18 ,
55 ,
119 )) •
EBI2 •
Estrogen •
Slobodna masna kiselina (
1 ,
2 ,
3 ,
4 ) •
Laktat •
Lizofosfatidna kiselina (
1 ,
2 ,
3 ,
4 ,
5 ,
6 ) •
Lizofosfolipid (
1 ,
2 ,
3 ,
4 ,
5 ,
6 ,
7 ,
8 ) •
Niacin (
1 ,
2 ) •
Oksoglutarat •
PAF •
Sfingozin-1-fosfat (
1 ,
2 ,
3 ,
4 ,
5 ) •
Sukcinat
Peptid
Drugi
Anafilatoksin (
C3a ,
C5a ) •
Angiotenzin (
1 ,
2 ) •
Apelin •
Bombezin (
BRS3 ,
GRPR ,
NMBR ) •
Bradikinin (
B1 ,
B2 ) •
Hemokin •
Holecistokinin (
A ,
B ) •
Endotelin (
A ,
B ) •
Formil peptid (
1 ,
2 ,
3 ) •
FSH •
Galanin (
1 ,
2 ,
3 ) •
GHB receptor •
Gonadotropin-oslobađajući hormon (
1 ,
2 ) •
Grelin •
Kispeptin •
Luteinizirajući hormon/horiogonadotropin •
MAS (
1 ,
1L ,
D ,
E ,
F ,
G ,
X1 ,
X2 ,
X3 ,
X4 ) •
Melanokortin (
1 ,
2 ,
3 ,
4 ,
5 ) •
MCHR (
1 ,
2 ) •
Motilin •
Opioidni (
δ ,
κ ,
μ ,
Nociceptin &
ζ , ali ne
σ ) •
Oreksin (
1 ,
2 ) •
Oksitocin •
Prokineticin (
1 ,
2 ) •
Prolaktin-oslobađajući peptid •
Relaksin (
1 ,
2 ,
3 ,
4 ) •
Somatostatin (
1 ,
2 ,
3 ,
4 ,
5 ) •
Tahikinin (
1 ,
2 ,
3 ) •
Tirotropin •
Tirotropin-oslobađajući hormon •
Urotenzin-II •
Vazopresin (
1A ,
1B ,
2 )
Razno
GPR (
1 ,
3 ,
4 ,
6 ,
12 ,
15 ,
17 ,
18 ,
19 ,
20 ,
21 ,
22 ,
23 ,
25 ,
26 ,
27 ,
31 ,
32 ,
33 ,
34 ,
35 ,
37 ,
39 ,
42 ,
44 ,
45 ,
50 ,
52 ,
55 ,
61 ,
62 ,
63 ,
65 ,
68 ,
75 ,
77 ,
78 ,
81 ,
82 ,
83 ,
84 ,
85 ,
87 ,
88 ,
92 ,
101 ,
103 ,
109A ,
109B ,
119 ,
120 ,
132 ,
135 ,
137B ,
139 ,
141 ,
142 ,
146 ,
148 ,
149 ,
150 ,
151 ,
152 ,
153 ,
160 ,
161 ,
162 ,
171 ,
173 ,
174 ,
176 ,
177 ,
182 ,
183 )
Drugi
Adrenomedulin •
Mirisni •
Opsin (
3 ,
4 ,
5 ,
1LW ,
1MW ,
1SW ,
RGR ,
RRH ) •
Proteazom-aktivirani (
1 ,
2 ,
3 ,
4 ) •
SREB (
1 ,
2 ,
3 )
Klasa B : Sekretinu slični
GPR (
56 ,
64 ,
97 ,
98 ,
110 ,
111 ,
112 ,
113 ,
114 ,
115 ,
116 ,
123 ,
124 ,
125 ,
126 ,
128 ,
133 ,
143 ,
144 ,
155 ,
157 )
Drugi
Moždano specifični angiogenezni inhibitor (
1 ,
2 ,
3 ) •
Cadherin (
1 ,
2 ,
3 ) •
Kalcitonin •
CALCRL •
CD97 •
Kortikotropin-oslobađajući hormon (
1 ,
2 ) •
EMR (
1 ,
2 ,
3 ) •
Glukagon (
GR ,
GIPR ,
GLP1R ,
GLP2R ) •
Hormon rasta oslobađajući hormon •
PACAPR1 •
GPR •
Latrofilin (
1 ,
2 ,
3 ,
ELTD1 ) •
Metuselah-slični proteini •
Paratiroidni hormon (
1 ,
2 ) •
Sekretin •
Vazoaktivni intestinalni peptid (
1 ,
2 )
Klasa C : Metabotropni glutamat / feromon
TAS1R (
1 ,
2 ,
3 ) •
TAS2R (
1 ,
3 ,
4 ,
5 ,
8 ,
9 ,
10 ,
12 ,
13 ,
14 ,
16 ,
19 ,
20 ,
30 ,
31 ,
38 ,
39 ,
40 ,
41 ,
42 ,
43 ,
45 ,
46 ,
50 )
Drugi
Kalcijum-detektujući receptor •
GABA B (
1 ,
2 ) •
Glutamatni receptor (
Metabotropni glutamat (
1 ,
2 ,
3 ,
4 ,
5 ,
6 ,
7 ,
8 )) •
GPRC6A •
GPR (
156 ,
158 ,
179 ) •
RAIG (
1 ,
2 ,
3 ,
4 )
Klasa F:Frizzled / Zaglađeni
B trdu : peptidi (nrpl /grfl /cytl /horl ), receptori (lgic , enzr , gprc , igsr , intg , nrpr /grfr /cytr ), itra (adap , gbpr , mapk ), calc , lipd , signalni putevi (hedp , wntp , tgfp +mapp , notp , jakp , fsap , hipp , tlrp )
Agonisti :
Azapironi :
Alnespiron •
Binospiron •
Buspiron •
Enilospiron •
Eptapiron •
Gepiron •
Ipsapiron •
Perospiron •
Revospiron •
Tandospiron •
Tiospiron •
Umespiron •
Zalospiron ;
Antidepresivi :
Etoperidon •
Nefazodon •
Trazodon ;
Antipsihotici :
Aripiprazol •
Asenapin •
Klozapin •
Kvetiapin •
Ziprasidon ;
Ergolini :
Dihidroergotamin •
Ergotamin •
Lisurid •
Metisergid •
LSD ;
Triptamini :
5-CT •
5-MeO-DMT •
5-MT •
Bufotenin •
DMT •
Indorenat •
Psilocin •
Psilocibin ;
Drugi :
8-OH-DPAT •
Adatanserin •
Bay R 1531 •
Befiradol •
BMY-14802 •
Kanabidiol •
Dimemebfe •
Ebalzotan •
Eltoprazin •
F-11,461 •
F-12,826 •
F-13,714 •
F-14,679 •
F-15,063 •
F-15,599 •
Flesinoksan •
Flibanserin •
Lesopitron •
Lu AA21004 •
LY-293,284 •
LY-301,317 •
MKC-242 •
NBUMP •
Osemozotan •
Oksaflozan •
Pardoprunoks •
Piklozotan •
Rauvolscin •
Repinotan •
Roksindol •
RU-24,969 •
S 14,506 •
S-14,671 •
S-15,535 •
Sarizotan •
SSR-181,507 •
Sunepitron •
U-92,016-A •
Urapidil •
Vilazodon •
Ksaliproden •
Johimbin Antagonisti :
Antipsihotici :
Iloperidon •
Risperidon •
Sertindol ;
Beta blokatori :
Alprenolol •
Cianopindolol •
Jodocianopindolol •
Oksprenolol •
Pindobind •
Pindolol •
Propranolol •
Tertatolol ;
Drugi :
AV965 •
BMY-7,378 •
CSP-2503 •
Dotarizin •
Flopropion •
GR-46611 •
Isamoltan •
Lekozotan •
Metitepin/Metiotepin •
MPPF •
NAN-190 •
PRX-00023 •
Robalzotan •
S-15535 •
SB-649,915 •
SDZ 216-525 •
Spiperon •
Spiramid •
Spiroksatrin •
UH-301 •
WAY-100,135 •
WAY-100,635 •
Ksilamidin Agonisti :
Lisergamidi :
Dihidroergotamin •
Metisergid ;
Triptani :
Almotriptan •
Avitriptan •
Eletriptan •
Frovatriptan •
Naratriptan •
Rizatriptan •
Sumatriptan •
Zolmitriptan ;
Triptamini :
5-CT •
5-Etil-DMT •
5-MT •
5-(Noniloksi)triptamin ;
Drugi :
CP-135,807 •
CP-286,601 •
GR-46611 •
L-694,247 •
L-772,405 •
PNU-109,291 •
PNU-142,633 Antagonisti :
Lisergamidi :
Metergolin ;
Drugi :
Alniditan •
BRL-15,572 •
Elzasonan •
GR-127,935 •
Ketanserin •
LY-310,762 •
LY-367,642 •
LY-456,219 •
LY-456,220 •
Metitepin/Metiotepin •
Ritanserin •
Johimbin •
Ziprasidon
Agonisti :
Fenetilamini :
2C-B •
2C-E •
2C-I •
2C-T-2 •
2C-T-7 •
2C-T-21 •
DOB •
DOC •
DOI •
DOM •
MDA •
MDMA •
Meskalin ;
Piperazini :
Aripiprazol •
mCPP •
TFMPP ;
Triptamini :
5-CT •
5-MeO-α-ET •
5-MeO-α-MT •
5-MeO-DET •
5-MeO-DiPT •
5-MeO-DMT •
5-MeO-DPT •
5-MT •
α-ET •
α-Metil-5-HT •
α-MT •
Bufotenin •
DET •
DiPT •
DMT •
DPT •
Psilocin •
Psilocibin ;
Drugi :
A-372,159 •
AL-38022A •
CP-809,101 •
Dimemebfe •
Lorkaserin •
Medifoksamin •
MK-212 •
Org 12,962 •
ORG-37,684 •
Oksaflozan •
PNU-22394 •
Ro60-0175 •
Ro60-0213 •
Vabicaserin •
WAY-629 •
WAY-161,503 •
YM-348 Antagonisti :
Atipični antipsihotici :
Klozapin •
Iloperidon •
Melperon •
Olanzapin •
Paliperidon •
Pimozid •
Hetiapin •
Risperidon •
Sertindol •
Ziprasidon •
Zotepin ;
Tipični antipsihotici :
Hlorpromazin •
Loksapin •
Pipamperon ;
Antidepresivi :
Agomelatin •
Amitriptilin •
Amoksapin •
Aptazapin •
Etoperidon •
Fluoksetin •
Mianserin •
Mirtazapin •
Nefazodon •
Nortriptilin •
Trazodon ;
Drugi :
Adatanserin •
Cinanserin •
Ciproheptadin •
Deramciklan •
Dotarizin •
Eltoprazin •
Esmirtazapin •
FR-260,010 •
Ketanserin •
Ketotifen •
Latrepirdin •
Lu AA24530 •
Metitepin/Metiotepin •
Metisergid •
Pizotifen •
Ritanserin •
RS-102,221 •
S-14,671 •
SB-200,646 •
SB-206,553 •
SB-221,284 •
SB-228,357 •
SB-242,084 •
SB-243,213 •
SDZ SER-082 •
Ksilamidin
Agonisti :
Lisergamidi :
Dihidroergotamin •
Ergotamin •
Lisurid •
LSD •
Mesulergin •
Metergolin •
Metisergid ;
Triptamini :
2-Metil-5-HT •
5-BT •
5-CT •
5-MT •
Bufotenin •
E-6801 •
E-6837 •
EMD-386,088 •
EMDT •
LY-586,713 •
N -Metil-5-HT •
Triptamin ;
Drugi :
WAY-181,187 •
WAY-208,466 Antagonisti :
Antidepresanti :
Amitriptilin •
Amoksapin •
Klomipramin •
Doksepin •
Mianserin •
Nortriptilin ;
Atipični antipsihotici :
Aripiprazol •
Asenapin •
Klozapin •
Fluperlapin •
Iloperidon •
Olanzapin •
Tiospiron ;
Tipični antipsihotici :
Hlorpromazin •
Loksapin ;
Drugi :
BGC20-760 •
BVT-5182 •
BVT-74316 •
EGIS-12,233 •
GW-742,457 •
Ketanserin •
Latrepirdin •
Lu AE58054 •
Metitepin/Metiotepin •
MS-245 •
PRX-07034 •
Ritanserin •
Ro04-6790 •
Ro 63-0563 •
SB-258,585 •
SB-271,046 •
SB-357,134 •
SB-399,885 •
SB-742,457 Agonisti :
Lisergamidi :
LSD ;
Triptamini :
5-CT •
5-MT •
Bufotenin ;
Drugi :
8-OH-DPAT •
AS-19 •
Bifeprunoks •
LP-12 •
LP-44 •
RU-24,969 •
Sarizotan Antagonisti :
Lisergamidi :
2-Bromo-LSD •
Bromokriptin •
Dihidroergotamin •
Ergotamin •
Mesulergin •
Metergolin •
Metisergid ;
Antidepresanti :
Amitriptilin •
Amoksapin •
Klomipramin •
Imipramin •
Maprotilin •
Mianserin ;
Atipični antipsihotici :
Amisulprid •
Aripiprazol •
Klozapin •
Olanzapin •
Risperidon •
Sertindol •
Tiospiron •
Ziprasidon •
Zotepin ;
Tipični antipsihotici :
Hlorpromazin •
Loksapin ;
Drugi :
Butaklamol •
EGIS-12,233 •
Ketanserin •
LY-215,840 •
Metitepin/Metiotepin •
Pimozid •
Ritanserin •
SB-258,719 •
SB-258,741 •
SB-269,970 •
SB-656,104 •
SB-656,104-A •
SB-691,673 •
SLV-313 •
SLV-314 •
Spiperon •
SSR-181,507