Nomenclature | MT1 | MT2 | MT3 |
---|---|---|---|
Previous names | MEL1A, ML1A, Mel1a | MEL1B, ML1B, Mel1b | ML2 |
Structural information | 7TM | 7TM | |
Gene/chromosome | |||
Human | 350 aa,a P48039; chr 4q 35.1 | 362 aa,b P49286; chr 11q21–22 | |
Mouse | 353 aa,c Q61184; chr 8 | 365 aa,d U57554; chr 9 | |
Selective agonists | S 26284e | IIK7 (10.3)f | N-Acetylserotonin,g–k 5MCA-NATk |
Selective antagonists | S 26131e | 4P-ADOT,l,m 4P-PDOT (8.8),l,m GR 128107l, K185 (9.3)f | Prazosinh |
Radioligands | [3H]MLT,n 2- [125I]IMLTo | [3H]MLT,n 2-[125I]IMLT,o [3H]4P-PDOTp | 2-[125I]5MCA-NAT,k 2-[125I]IMLTn |
Tissue Functions | Vascular vasoconstriction,q–u inhibition neuronal firing,v phase-shift circadian activity rhythmsu | Vascular vasodilation,t inhibition retinal dopamine release,l phase-shift circadian rhythms of neuronal firingm,w,v,x | Leukocyte adhesionu |
Comments | MT1 full-length cDNAs were cloned from human (350 aa),a mouse (353 aa),c sheep (366 aa),a rat (353 aa),y hamster (353 aa),z monkey (352),aa and partial cDNAs from cattle (257 aa) and pig (154 aa).bb | MT2 cDNA was cloned from human (362 aa),z rat (364 aa),y mouse (365 aa),d sheep (376 aa),cc monkey (362 aa),aa and partial cDNA from hamster.z | Endogenous ligands are MLT and N-acetylserotonin. A recent report identifies an MT3 binding site in hamster kidney as the enzyme quinone reductase-2.dd Antagonist potencies have not yet been established. |
aa, amino acid(s); chr, chromosome; 5MCA-NAT, 5-methoxycarbonylamino-N-acetyltryptamine.
↵a Reppert et al., 1994.
↵b Reppert et al., 1995a.
↵c Roca et al., 1996.
↵d Jin et al., 2003.
↵e Audinot et al., 2003.
↵f Faust et al., 2000.
↵g Dubocovich, 1988b.
↵h Lucchelli et al., 1997.
↵i Eison and Mullins, 1993.
↵j Popova and Dubocovich, 1995.
↵k Molinari et al., 1996.
↵l Dubocovich et al., 1997.
↵m Dubocovich et al., 1998b.
↵n Browning et al., 2000.
↵o Dubocovich and Takahashi, 1987.
↵p Dubocovich and Masana, 1999.
↵q Ting et al., 1999.
↵r Ting et al., 1997.
↵s Masana et al., 2002.
↵t Doolen et al., 1998.
↵u Lotufo et al., 2001.
↵v Liu et al., 1997.
↵w Dubocovich et al., 2005.
↵x Hunt et al., 2001.
↵y Audinot et al., 2008.
↵z Weaver et al., 1996.
↵aa Nishiyama et al., 2009.
↵bb Messer et al., 1997.
↵cc Cogé et al, 2009.
↵dd Nosjean et al., 2000.