1Overview: 
1-Adrenoceptors (nomenclature as agreed by NC-IUPHAR Subcommittee on Adrenoceptors, Bylund et al., 1994) are 7TM receptors activated by the endogenous agonists adrenaline and noradrenaline with equal potency. Phenylephrine, methoxamine and cirazoline are agonists selective for 1-adrenoceptors relative to 2-adrenoceptors, while prazosin (8.5–10.5) and corynanthine (6.5–7.5) are considered selective for 1-adrenoceptors relative to 2-adrenoceptors. [3H]-Prazosin (0.25 nM) and [125I]-HEAT (0.1 nM; also known as BE2254) are relatively selective radioligands. Numerous splice variants of the 1-adrenoceptors exist, some of which may display a different spectrum of signalling properties. One polymorphism of the 1A-adrenoceptor has been described but is not associated with disease.
The clone originally called the 1C-adrenoceptor corresponds to the pharmacologically defined 1A-adrenoceptor (see Ford et al., 1994; Hieble et al., 1995). Some tissues possess 1-adrenoceptors that display relatively low affinity in functional and binding assays for prazosin (pKi <9) that might represent different receptor states (termed 1L-adrenoceptors, Ford et al., 1997; Morishima et al., 2007). 1A-Adrenoceptor C-terminal splice variants form homo and heterodimers, but fail to generate a functional 1L adrenoceptor (Ramsay et al., 2004). 1D-Adrenoceptors form heterodimers with 1B- or 
2-adrenoceptors that show increased cell-surface expression (Uberti et al., 2005). Heterodimers formed between 1D- and 1B-adrenoceptors have distinct functional properties (Hague et al., 2004). (+)Niguldipine also has high affinity for L-type Ca2+ channels.
Keywords:
1-Adrenoceptors, adrenaline, noradrenaline, Phenylephrine, methoxamine, cirazoline, prazosin, corynanthine, [3H]-Prazosin, [125I]-HEAT, A61603, KMD3213, (+)niguldipine, SNAP5089, RS17053, SNAP5272, BMY7378, Silodosin, tamsulosin, dabuzalgron
Abbreviations:
A61603, N-(5-[4,5-dihydro-1H-imidazol-2-y]-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)methanesulfonamide hydrobromide; BMY7378, 8-(2-[4-{2methoxyphenyl}-1-piperazinyl]ethyl)-8-azaspiro[4,5]decane-7,9-dione dihydrochloride; HEAT, 2--4-hydroxy-3-iodophenylethylaminomethyltetralone; ICI118551, (-)-1-(2,3-[dihydro-7-methyl-1H-inden-4-yl]oxy)-3-([1-methylethyl]-amino)-2-butanol; KMD3213, (-)-(R)-1-(3-hydroxypropyl)-5-(2-[2-{2-(2,2,2-trifluoroethoxy)phenoxyl}ethylamino]propyl)indoline-7-carboxamide, also known as silodosin; RS17053, N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-,-dimethyl-1H-indole-3-ethanamide; SNAP5089, 2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate-N-[3-(4,4-diphenylpiperidin-1-yl)propyl]amide methyl ester; SNAP5272, carboxamide-2,6-diethyl-1,4-dihydro-3-[N-(3-[4-hydroxy-4-phenylpiperidinyl]propyl)]carboxamido-4-(4-nitrophenyl)
References
Further Reading
- Bylund DB, Eikenberg DC, Hieble JP, Langer SZ, Lefkowitz RJ, Minneman KP et al. (1994). International Union of Pharmacology IV. Nomenclature of adrenoceptors. Pharmacol Rev 46: 121–136. | PubMed | ISI | ChemPort |
- Cotecchia S (2007). Constitutive activity and inverse agonism at the 1adrenoceptors. Biochem Pharmacol 73: 1076–1083.
- Ford APDW, Williams TJ, Blue DR, Clarke DE (1994). 1-Adrenoceptor classification: sharpening Occam's razor. Trends Pharmacol Sci 15: 167–170. | Article | PubMed | ChemPort |
- Hein L (2006). Adrenoceptors and signal transduction in neurons. Cell Tissue Res 326: 541–551.
- Hieble JP, Bylund DB, Clarke DE, Eikenburg DC, Langer SZ, Lefkowitz RJ et al. (1995). International Union of Pharmacology. X. Recommendation for nomenclature of 1-adrenoceptors: consensus update. Pharmacol Rev 47: 267–270. | PubMed | ISI | ChemPort |
- Koshimizu TA, Tanoue A, Tsujimoto G (2007). Clinical implications from studies of 1 adrenergic receptor knockout mice. Biochem Pharmacol 73: 1107–1112.
- Tanoue A, Koshimizu TA, Shibata K, Nasa Y, Takeo S, Tsujimoto G (2003). Insights into 1 adrenoceptor function in health and disease from transgenic animal studies. Trends Endocrinol Metab 14: 107–113. | PubMed | ChemPort |
References
- Blue DR et al. (2004). BJU Int 93: 162–170. | Article | ISI | ChemPort |
- Ford APDW et al. (1997). Br J Pharmacol 121: 1127–1135. | Article | PubMed | ISI | ChemPort |
- Hague C et al. (2004). J Pharmacol Exp Ther 309: 388–397. | Article | ISI | ChemPort |
- Morishima S et al. (2007). J Urol 177: 377–381. | Article | PubMed | ChemPort |
- Ramsay D et al. (2004). Mol Pharmacol 66: 228–239. | Article | PubMed | ChemPort |
- Uberti MA et al. (2005). J Pharmacol Exp Ther 313: 16–23.
