| Version |
2.5 |
| Creation Date |
2005-06-13 13:24:05 |
| Update Date |
2009-02-19 16:04:59 |
| Primary Accession Number |
DB00457 |
| Secondary Accession Number |
|
| Name |
Prazosin |
| Drug Type |
|
| Description |
A selective adrenergic alpha-1 antagonist used in the treatment of heart failure, hypertension, pheochromocytoma, Raynaud's syndrome, prostatic hypertrophy, and urinary retention. [PubChem] |
| Synonyms |
- Prazocin
- Prazosin HCl
- Prazosin Hydrochloride
- Prazosina [INN-Spanish]
- Prazosine [INN-French]
- Prazosinum [INN-Latin]
|
| Brand Names |
- Furazosin
- Lentopres
- Minipress
- Minipress Xl
- Vasoflex
|
| Brand Mixtures |
Not Available |
| Chemical IUPAC Name |
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-furan-2-ylmethanone |
| Chemical Formula |
C19H21N5O4 |
| Chemical Structure |
 |
| CAS Registry Number |
19216-56-9 |
| InChI Identifier |
InChI=1/C19H21N5O4/c1-26-15-10-12-13(11-16(15)27-2)21-19(22-17(12)20)24-7-5-23(6-8-24)18(25)14-4-3-9-28-14/h3-4,9-11H,5-8H2,1-2H3,(H2,20,21,22)/f/h20H2 |
| InChI Key |
IENZQIKPVFGBNW-HPHMPNDVCR |
| KEGG Drug |
Not Available |
| KEGG Compound |
C07368  |
| PubChem Compound |
4893  |
| PubChem Substance |
9572  |
| ChEBI ID |
Not Available |
| PharmGKB ID |
PA451093  |
| HET ID |
Not Available |
| GenBank ID |
Not Available |
| Drug ID Number [DIN] |
01910302  |
| RxList Link |
http://www.rxlist.com/cgi/generic3/prazosin.htm  |
| PDRhealth Link |
Not Available |
| Wikipedia Link |
http://en.wikipedia.org/wiki/Prazosin  |
| FDA Label |
Not Available |
| Material Safety Data Sheet (MSDS) |
|
| Synthesis Reference |
Not Available |
| Average Molecular Weight |
383.4011 |
| Monoisotopic Molecular Weight |
383.1594 |
| State |
Solid |
| Melting Point |
279 oC |
| Experimental Water Solubility |
0.5 mg/mL (HCl salt) [Sigma Aldrich]
Source: PhysProp
|
| Predicted Water Solubility |
6.93e-01 mg/mL
Calculated using ALOGPS
|
| Experimental LogP/Hydrophobicity |
1.3
Source: PhysProp
|
| Predicted LogP |
1.93
Calculated using ALOGPS
|
| Experimental LogS |
Not Available |
| Predicted LogS |
-2.74
Calculated using ALOGPS
|
| Experimental Caco2 Permeability |
-4.36 [ADME Research, USCD] |
| pKa/Isoelectric Point |
Not Available |
| Mass Spectrum |
Not Available
|
| MOL File |
Show | Download  |
| SDF File |
Show | Download  |
| PDB File |
Show | Download  |
| 2D Structure |
|
| 3D Structure |
|
| Experimental PDB ID |
Not Available |
| Isomeric SMILES |
COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1=CC=CO1 |
| Canonical SMILES |
COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1=CC=CO1 |
| Drug Category |
- Adrenergic alpha-Antagonists
- Alpha-adrenergic Blocking Agents
- Antihypertensive Agents
|
| ATC Codes |
|
| AHFS Codes |
|
| Indication |
For treatment of hypertension and chronic heart failure. |
| Pharmacology |
Prazosin is an alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. Accordingly, Prazosin is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors. In the human prostate, Prazosin antagonizes phenylephrine (alpha1 agonist)-induced contractions, in vitro, and binds with high affinity to the alpha1c adrenoceptor, which is thought to be the predominant functional type in the prostate. Studies in normal human subjects have shown that Prazosin competitively antagonized the pressor effects of phenylephrine (an alpha1 agonist) and the systolic pressor effect of norepinephrine. The antihypertensive effect of Prazosin results from a decrease in systemic vascular resistance and the parent compound Prazosin is primarily responsible for the antihypertensive activity. |
| Mechanism of Action |
Prazosin acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation. |
| Absorption |
Well-absorbed from gastrointestinal tract; bioavailability is variable (50 to 85%). |
| Toxicity |
Not Available |
| Protein Binding |
97% |
| Biotransformation |
Primarily hepatic. Several metabolites have been identified in humans and animals (6- O -demethyl, 7- O -demethyl, 2-[1-piperazinyl]-4-amino-6, 7-dimethoxyquinazoline, 2,4-diamino-6,7-dimethoxyquinazoline). |
| Half Life |
2-3 hours |
| Dosage Forms |
|
| Patient Information |
Show  |
| Contraindications |
Show  |
| Interactions |
Show  |
| Drug Interactions |
| Drug |
Interaction |
| Acebutolol |
Risk of hypotension at the beginning of therapy |
| Atenolol |
Risk of hypotension at the beginning of therapy |
| Betaxolol |
Risk of hypotension at the beginning of therapy |
| Bevantolol |
Risk of hypotension at the beginning of therapy |
| Bisoprolol |
Risk of hypotension at the beginning of therapy |
| Carteolol |
Risk of hypotension at the beginning of therapy |
| Carvedilol |
Risk of hypotension at the beginning of therapy |
| Digoxin |
Prazosin increases the effect of digoxin |
| Esmolol |
Risk of hypotension at the beginning of therapy |
| Labetalol |
Risk of hypotension at the beginning of therapy |
| Metoprolol |
Risk of hypotension at the beginning of therapy |
| Nadolol |
Risk of hypotension at the beginning of therapy |
| Oxprenolol |
Risk of hypotension at the beginning of therapy |
| Penbutolol |
Risk of hypotension at the beginning of therapy |
| Pindolol |
Risk of hypotension at the beginning of therapy |
| Practolol |
Risk of hypotension at the beginning of therapy |
| Propranolol |
Risk of hypotension at the beginning of therapy |
| Sotalol |
Risk of hypotension at the beginning of therapy |
| Tadalafil |
Risk of significant hypotension with this association |
| Timolol |
Risk of hypotension at the beginning of therapy |
| Verapamil |
Risk of hypotension at the beginning of therapy |
|
| Food Interactions |
- Avoid alcohol.
- Avoid natural licorice.
- Take without regard to meals.
|
| Pathways |
Not Available
|
| General References |
- Bawaskar HS, Bawaskar PH: Utility of scorpion antivenin vs prazosin in the management of severe Mesobuthus tamulus (Indian red scorpion) envenoming at rural setting. J Assoc Physicians India. 2007 Jan;55:14-21. [PubMed
]
- Drugs.com

- [PubMed
]
- Wikipedia

- RxList

|
| Organisms Affected |
|
| Targets |
- Alpha-1A adrenergic receptor
- Alpha-1B adrenergic receptor
- Alpha-1D adrenergic receptor
|
|
Drug Target 1
[top]
|
| Target 1 ID |
556 |
| Target 1 Name |
Alpha-1A adrenergic receptor |
| Target 1 Synonyms |
- Alpha 1A- adrenoreceptor
- Alpha 1A-adrenoceptor
- Alpha adrenergic receptor 1c
- Alpha-1C adrenergic receptor
|
| Target 1 Gene Name |
ADRA1A |
| Target 1 Protein Sequence |
>Alpha-1A adrenergic receptor
MVFLSGNASDSSNCTQPPAPVNISKAILLGVILGGLILFGVLGNILVILSVACHRHLHSV
THYYIVNLAVADLLLTSTVLPFSAIFEVLGYWAFGRVFCNIWAAVDVLCCTASIMGLCII
SIDRYIGVSYPLRYPTIVTQRRGLMALLCVWALSLVISIGPLFGWRQPAPEDETICQINE
EPGYVLFSALGSFYLPLAIILVMYCRVYVVAKRESRGLKSGLKTDKSDSEQVTLRIHRKN
APAGGSGMASAKTKTHFSVRLLKFSREKKAAKTLGIVVGCFVLCWLPFFLVMPIGSFFPD
FKPSETVFKIVFWLGYLNSCINPIIYPCSSQEFKKAFQNVLRIQCLCRKQSSKHALGYTL
HPPSQAVEGQHKDMVRIPVGSRETFYRISKTDGVCEWKFFSSMPRGSARITVSKDQSSCT
TARVRSKSFLQVCCCVGPSTPSLDKNHQVPTIKVHTISLSENGEEV
|
| Target 1 Number of Residues |
473 |
| Target 1 Molecular Weight |
51487 |
| Target 1 Theoretical pI |
9.23 |
| Target 1 GO Classification |
|
Function
|
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha1-adrenergic receptor activity |
|
Process
|
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway |
|
Component
|
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 1 General Function |
Involved in alpha1-adrenergic receptor activity |
| Target 1 Specific Function |
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins |
| Target 1 Pathways |
Not Available
|
| Target 1 Reactions |
Not Available |
| Target 1 Pfam Domain Function |
|
| Target 1 Signals |
|
| Target 1 Transmembrane Regions |
- 28-51
- 65-88
- 100-122
- 144-167
- 182-205
- 274-297
- 306-329
|
| Target 1 Essentiality |
Non-Essential |
| Target 1 GenBank ID Protein |
433201  |
| Target 1 UniProtKB/Swiss-Prot ID |
P35348  |
| Target 1 UniProtKB/Swiss-Prot Entry Name |
ADA1A_HUMAN  |
| Target 1 PDB ID |
Not Available |
| Target 1 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| Target 1 Gene Sequence |
>1401 bp
ATGGTGTTTCTCTCGGGAAATGCTTCCGACAGCTCCAACTGCACCCAACCGCCGGCACCG
GTGAACATTTCCAAGGCCATTCTGCTCGGGGTGATCTTGGGGGGCCTCATTCTTTTCGGG
GTGCTGGGTAACATCCTAGTGATCCTCTCCGTAGCCTGTCACCGACACCTGCACTCAGTC
ACGCACTACTACATCGTCAACCTGGCGGTGGCCGACCTCCTGCTCACCTCCACGGTGCTG
CCCTTCTCCGCCATCTTCGAGGTCCTAGGCTACTGGGCCTTCGGCAGGGTCTTCTGCAAC
ATCTGGGCGGCAGTGGATGTGCTGTGCTGCACCGCGTCCATCATGGGCCTCTGCATCATC
TCCATCGACCGCTACATCGGCGTGAGCTACCCGCTGCGCTACCCAACCATCGTCACCCAG
AGGAGGGGTCTCATGGCTCTGCTCTGCGTCTGGGCACTCTCCCTGGTCATATCCATTGGA
CCCCTGTTCGGCTGGAGGCAGCCGGCCCCCGAGGACGAGACCATCTGCCAGATCAACGAG
GAGCCGGGCTACGTGCTCTTCTCAGCGCTGGGCTCCTTCTACCTGCCTCTGGCCATCATC
CTGGTCATGTACTGCCGCGTCTACGTGGTGGCCAAGAGGGAGAGCCGGGGCCTCAAGTCT
GGCCTCAAGACCGACAAGTCGGACTCGGAGCAAGTGACGCTCCGCATCCATCGGAAAAAC
GCCCCGGCAGGAGGCAGCGGGATGGCCAGCGCCAAGACCAAGACGCACTTCTCAGTGAGG
CTCCTCAAGTTCTCCCGGGAGAAGAAAGCGGCCAAAACGCTGGGCATCGTGGTCGGCTGC
TTCGTCCTCTGCTGGCTGCCTTTTTTCTTAGTCATGCCCATTGGGTCTTTCTTCCCTGAT
TTCAAGCCCTCTGAAACAGTTTTTAAAATAGTATTTTGGCTCGGATATCTAAACAGCTGC
ATCAACCCCATCATATACCCATGCTCCAGCCAAGAGTTCAAAAAGGCCTTTCAGAATGTC
TTGAGAATCCAGTGTCTCCGCAGAAAGCAGTCTTCCAAACATGCCCTGGGCTACACCCTG
CACCCGCCCAGCCAGGCCGTGGAAGGGCAACACAAGGACATGGTGCGCATCCCCGTGGGA
TCAAGAGAGACCTTCTACAGGATCTCCAAGACGGATGGCGTTTGTGAATGGAAATTTTTC
TCTTCCATGCCCCGTGGATCTGCCAGGATTACAGTGTCCAAAGACCAATCCTCCTGTACC
ACAGCCCGGGTGAGAAGTAAAAGCTTTTTGGAGGTCTGCTGCTGTGTAGGGCCCTCAACC
CCCAGCCTTGACAAGAACCATCAAGTTCCAACCATTAAGGTCCACACCATCTCCCTCAGT
GAGAACGGGGAGGAAGTCTAG
|
| Target 1 GenBank Gene ID |
|
| Target 1 GeneCard ID |
ADRA1A  |
| Target 1 GenAtlas ID |
ADRA1A  |
| Target 1 HGNC ID |
HGNC:277  |
| Target 1 Chromosome Location |
8 |
| Target 1 Locus |
8p21-p11.2 |
| Target 1 SNPs |
SNPJam Report  |
| Target 1 General References |
- Hirasawa A, Shibata K, Horie K, Takei Y, Obika K, Tanaka T, Muramoto N, Takagaki K, Yano J, Tsujimoto G: Cloning, functional expression and tissue distribution of human alpha 1c-adrenoceptor splice variants. FEBS Lett. 1995 Apr 24;363(3):256-60. [PubMed
]
- Schwinn DA, Johnston GI, Page SO, Mosley MJ, Wilson KH, Worman NP, Campbell S, Fidock MD, Furness LM, Parry-Smith DJ, et al.: Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. J Pharmacol Exp Ther. 1995 Jan;272(1):134-42. [PubMed
]
- Weinberg DH, Trivedi P, Tan CP, Mitra S, Perkins-Barrow A, Borkowski D, Strader CD, Bayne M: Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c. Biochem Biophys Res Commun. 1994 Jun 30;201(3):1296-304. [PubMed
]
- Forray C, Bard JA, Wetzel JM, Chiu G, Shapiro E, Tang R, Lepor H, Hartig PR, Weinshank RL, Branchek TA, et al.: The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. Mol Pharmacol. 1994 Apr;45(4):703-8. [PubMed
]
- Hirasawa A, Horie K, Tanaka T, Takagaki K, Murai M, Yano J, Tsujimoto G: Cloning, functional expression and tissue distribution of human cDNA for the alpha 1C-adrenergic receptor. Biochem Biophys Res Commun. 1993 Sep 15;195(2):902-9. [PubMed
]
- Tseng-Crank J, Kost T, Goetz A, Hazum S, Roberson KM, Haizlip J, Godinot N, Robertson CN, Saussy D: The alpha 1C-adrenoceptor in human prostate: cloning, functional expression, and localization to specific prostatic cell types. Br J Pharmacol. 1995 Aug;115(8):1475-85. [PubMed
]
- Chang DJ, Chang TK, Yamanishi SS, Salazar FH, Kosaka AH, Khare R, Bhakta S, Jasper JR, Shieh IS, Lesnick JD, Ford AP, Daniels DV, Eglen RM, Clarke DE, Bach C, Chan HW: Molecular cloning, genomic characterization and expression of novel human alpha1A-adrenoceptor isoforms. FEBS Lett. 1998 Jan 30;422(2):279-83. [PubMed
]
|
| Target 1 Drug References |
- Suzuki Y, Kanada A, Okaya Y, Aisaka K: Effect of JTH-601, a novel alpha(1)-adrenoceptor antagonist, on prostate function in dogs. Eur J Pharmacol. 2000 Apr 7;394(1):123-30. [PubMed
]
- Chang HK, Hsu FL, Liu IM, Cheng JT: Stimulatory effect of cinnamic acid analogues on alpha1A-adrenoceptors in-vitro. J Pharm Pharmacol. 2003 Jun;55(6):833-7. [PubMed
]
- Zacharia J, Hillier C, MacDonald A: Alpha1-adrenoceptor subtypes involved in vasoconstrictor responses to exogenous and neurally released noradrenaline in rat femoral resistance arteries. Br J Pharmacol. 2004 Mar;141(6):915-24. Epub 2004 Feb 23. [PubMed
]
- Morris DP, Price RR, Smith MP, Lei B, Schwinn DA: Cellular trafficking of human alpha1a-adrenergic receptors is continuous and primarily agonist-independent. Mol Pharmacol. 2004 Oct;66(4):843-54. Epub 2004 Jul 16. [PubMed
]
- Tomiyama Y, Kobayashi K, Tadachi M, Kobayashi S, Inada Y, Kobayashi M, Yamazaki Y: Expressions and mechanical functions of alpha(1)-adrenoceptor subtypes in hamster ureter. Eur J Pharmacol. 2007 Nov 14;573(1-3):201-5. Epub 2007 Jul 6. [PubMed
]
|
|
Drug Target 2
[top]
|
| Target 2 ID |
632 |
| Target 2 Name |
Alpha-1B adrenergic receptor |
| Target 2 Synonyms |
- Alpha 1B- adrenoreceptor
- Alpha 1B-adrenoceptor
|
| Target 2 Gene Name |
ADRA1B |
| Target 2 Protein Sequence |
>Alpha-1B adrenergic receptor
MNPDLDTGHNTSAPAHWGELKNANFTGPNQTSSNSTLPQLDITRAISVGLVLGAFILFAI
VGNILVILSVACNRHLRTPTNYFIVNLAMADLLLSFTVLPFSAALEVLGYWVLGRIFCDI
WAAVDVLCCTASILSLCAISIDRYIGVRYSLQYPTLVTRRKAILALLSVWVLSTVISIGP
LLGWKEPAPNDDKECGVTEEPFYALFSSLGSFYIPLAVILVMYCRVYIVAKRTTKNLEAG
VMKEMSNSKELTLRIHSKNFHEDTLSSTKAKGHNPRSSIAVKLFKFSREKKAAKTLGIVV
GMFILCWLPFFIALPLGSLFSTLKPPDAVFKVVFWLGYFNSCLNPIIYPCSSKEFKRAFV
RILGCQCRGRGRRRRRRRRRLGGCAYTYRPWTRGGSLERSQSRKDSLDDSGSCLSGSQRT
LPSASPSPGYLGRGAPPPVELCAFPEWKAPGALLSLPAPEPPGRRGRHDSGPLFTFKLLT
EPESPGTDGGASNGGCEAAADVANGQPGFKSNMPLAPGQF
|
| Target 2 Number of Residues |
528 |
| Target 2 Molecular Weight |
56837 |
| Target 2 Theoretical pI |
9.79 |
| Target 2 GO Classification |
|
Function
|
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha1-adrenergic receptor activity |
|
Process
|
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway |
|
Component
|
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 2 General Function |
Involved in alpha1-adrenergic receptor activity |
| Target 2 Specific Function |
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system |
| Target 2 Pathways |
Not Available
|
| Target 2 Reactions |
Not Available |
| Target 2 Pfam Domain Function |
|
| Target 2 Signals |
|
| Target 2 Transmembrane Regions |
- 46-70
- 84-105
- 116-141
- 162-182
- 202-224
- 296-319
- 327-340
|
| Target 2 Essentiality |
Non-Essential |
| Target 2 GenBank ID Protein |
Not Available |
| Target 2 UniProtKB/Swiss-Prot ID |
P35368  |
| Target 2 UniProtKB/Swiss-Prot Entry Name |
ADA1B_HUMAN  |
| Target 2 PDB ID |
Not Available |
| Target 2 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| Target 2 Gene Sequence |
Not Available |
| Target 2 GenBank Gene ID |
|
| Target 2 GeneCard ID |
ADRA1B  |
| Target 2 GenAtlas ID |
ADRA1B  |
| Target 2 HGNC ID |
HGNC:278  |
| Target 2 Chromosome Location |
5 |
| Target 2 Locus |
5q23-q32 |
| Target 2 SNPs |
SNPJam Report  |
| Target 2 General References |
- Ramarao CS, Denker JM, Perez DM, Gaivin RJ, Riek RP, Graham RM: Genomic organization and expression of the human alpha 1B-adrenergic receptor. J Biol Chem. 1992 Oct 25;267(30):21936-45. [PubMed
]
- Schwinn DA, Johnston GI, Page SO, Mosley MJ, Wilson KH, Worman NP, Campbell S, Fidock MD, Furness LM, Parry-Smith DJ, et al.: Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. J Pharmacol Exp Ther. 1995 Jan;272(1):134-42. [PubMed
]
- Forray C, Bard JA, Wetzel JM, Chiu G, Shapiro E, Tang R, Lepor H, Hartig PR, Weinshank RL, Branchek TA, et al.: The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. Mol Pharmacol. 1994 Apr;45(4):703-8. [PubMed
]
|
| Target 2 Drug References |
- Al-Damluji S, Shen WB, White S, Barnard EA: alpha(1B) adrenergic receptors in gonadotrophin-releasing hormone neurones: relation to Transport-P. Br J Pharmacol. 2001 Jan;132(1):336-44. [PubMed
]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed
]
- Ishiguro M, Futabayashi Y, Ohnuki T, Ahmed M, Muramatsu I, Nagatomo T: Identification of binding sites of prazosin, tamsulosin and KMD-3213 with alpha(1)-adrenergic receptor subtypes by molecular modeling. Life Sci. 2002 Oct 11;71(21):2531-41. [PubMed
]
- Sharpe IA, Thomas L, Loughnan M, Motin L, Palant E, Croker DE, Alewood D, Chen S, Graham RM, Alewood PF, Adams DJ, Lewis RJ: Allosteric alpha 1-adrenoreceptor antagonism by the conopeptide rho-TIA. J Biol Chem. 2003 Sep 5;278(36):34451-7. Epub 2003 Jun 24. [PubMed
]
|
|
Drug Target 3
[top]
|
| Target 3 ID |
789 |
| Target 3 Name |
Alpha-1D adrenergic receptor |
| Target 3 Synonyms |
- Alpha 1D- adrenoreceptor
- Alpha 1D-adrenoceptor
- Alpha adrenergic receptor 1a
- Alpha-1A adrenergic receptor
|
| Target 3 Gene Name |
ADRA1D |
| Target 3 Protein Sequence |
>Alpha-1D adrenergic receptor
MTFRDLLSVSFEGPRPDSSAGGSSAGGGGGSAGGAAPSEGPAVGGVPGGAGGGGGVVGAG
SGEDNRSSAGEPGSAGAGGDVNGTAAVGGLVVSAQGVGVGVFLAAFILMAVAGNLLVILS
VACNRHLQTVTNYFIVNLAVADLLLSATVLPFSATMEVLGFWAFGRAFCDVWAAVDVLCC
TASILSLCTISVDRYVGVRHSLKYPAIMTERKAAAILALLWVVALVVSVGPLLGWKEPVP
PDERFCGITEEAGYAVFSSVCSFYLPMAVIVVMYCRVYVVARSTTRSLEAGVKRERGKAS
EVVLRIHCRGAATGADGAHGMRSAKGHTFRSSLSVRLLKFSREKKAAKTLAIVVGVFVLC
WFPFFFVLPLGSLFPQLKPSEGVFKVIFWLGYFNSCVNPLIYPCSSREFKRAFLRLLRCQ
CRRRRRRRPLWRVYGHHWRASTSGLRQDCAPSSGDAPPGAPLALTALPDPDPEPPGTPEM
QAPVASRRKPPSAFREWRLLGPFRRPTTQLRAKVSSLSHKIRAGGAQRAEAACAQRSEVE
AVSLGVPHEVAEGATCQAYELADYSNLRETDI
|
| Target 3 Number of Residues |
581 |
| Target 3 Molecular Weight |
60463 |
| Target 3 Theoretical pI |
9.44 |
| Target 3 GO Classification |
|
Function
|
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha1-adrenergic receptor activity |
|
Process
|
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway |
|
Component
|
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 3 General Function |
Carbohydrate transport and metabolism |
| Target 3 Specific Function |
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium |
| Target 3 Pathways |
Not Available
|
| Target 3 Reactions |
Not Available |
| Target 3 Pfam Domain Function |
|
| Target 3 Signals |
|
| Target 3 Transmembrane Regions |
- 96-121
- 134-159
- 170-192
- 214-238
- 252-275
- 349-373
- 381-405
|
| Target 3 Essentiality |
Non-Essential |
| Target 3 GenBank ID Protein |
177807  |
| Target 3 UniProtKB/Swiss-Prot ID |
P25100  |
| Target 3 UniProtKB/Swiss-Prot Entry Name |
ADA1D_HUMAN  |
| Target 3 PDB ID |
Not Available |
| Target 3 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| Target 3 Gene Sequence |
>1719 bp
ATGACTTTCCGCGATCTCCTGAGCGTCAGTTTCGAGGGACCCCGCCCGGACAGCAGCGCA
GGGGGCTCCAGCGCGGGCGGCGGCGGGGGCAGCGCGGGCGGCGCGGCCCCCTCGGAGGGC
CCGGCGGTGGGCGGCGTGCCGGGGGGCGCGGGCGGCGGCGGCGGCGTGGTGGGCGCAGGC
AGCGGCGAGGACAACCGGAGCTCCGCGGGGGAGCCGGGGAGCGCGGGCGCGGGCGGCGAC
GTGAATGGCACGGCGGCCGTCGGGGGACTGGTGGTGAGCGCGCAGGGCGTGGGCGTGGGC
GTCTTCCTGGCAGCCTTCATCCTTATGGCCGTGGCAGGTAACCTGCTTGTCATCCTCTCA
GTGGCCTGCAACCGCCACCTGCAGACCGTCACCAACTATTTCATCGTGAACCTGGCCGTG
GCCGACCTGCTGCTGAGCGCCACCGTACTGCCCTTCTCGGCCACCATGGAGGTTCTGGGC
TTCTGGGCCTTTGGCCGCGCCTTCTGCGACGTATGGGCCGCCGTGGACGTGCTGTGCTGC
ACGGCCTCCATCCTCAGCCTCTGCACCATCTCCGTGGACCGGTACGTGGGCGTGCGCCAC
TCACTCAAGTACCCAGCCATCATGACCGAGCGCAAGGCGGCCGCCATCCTGGCCCTGCTC
TGGGTCGTAGCCCTGGTGGTGTCCGTAGGGCCCCTGCTGGGCTGGAAGGAGCCCGTGCCC
CCTGACGAGCGCTTCTGCGGTATCACCGAGGAGGCGGGCTACGCTGTCTTCTCCTCCGTG
TGCTCCTTCTACCTGCCCATGGCGGTCATCGTGGTCATGTACTGCCGCGTGTACGTGGTC
GCGCGCAGCACCACGCGCAGCCTCGAGGCAGGCGTCAAGCGCGAGCGAGGCAAGGCCTCC
GAGGTGGTGCTGCGCATCCACTGTCGCGGCGCGGCCACGGGCGCCGACGGGGCGCACGGC
ATGCGCAGCGCCAAGGGCCACACCTTCCGCAGCTCGCTCTCCGTGCGCCTGCTCAAGTTC
TCCCGTGAGAAGAAAGCGGCCAAGACTCTGGCCATCGTCGTGGGTGTCTTCGTGCTCTGC
TGGTTCCCTTTCTTCTTTGTCCTGCCGCTCGGCTCCTTGTTCCCGCAGCTGAAGCCATCG
GAGGGCGTCTTCAAGGTCATCTTCTGGCTCGGCTACTTCAACAGCTGCGTGAACCCGCTC
ATCTACCCCTGTTCCAGCCGCGAGTTCAAGCGCGCCTTCCTCCGTCTCCTGCGCTGCCAG
TGCCGTCGTCGCCGGCGCCGCCGCCCTCTCTGGCGTGTCTACGGCCACCACTGGCGGGCC
TCCACCAGCGGCCTGCGCCAGGACTGCGCCCCGAGTTCGGGCGACGCGCCCCCCGGAGCG
CCGCTGGCCCTCACCGCGCTCCCCGACCCCGACCCCGAACCCCCAGGCACGCCCGAGATG
CAGGCTCCGGTCGCCAGCCGTCGAAAGCCACCCAGCGCCTTCCGCGAGTGGAGGCTGCTG
GGGCCGTTCCGGAGACCCACGACCCAGCTGCGCGCCAAAGTCTCCAGCCTGTCGCACAAG
ATCCGCGCCGGGGGCGCGCAGCGCGCAGAGGCAGCGTGCGCCCAGCGCTCAGAGGTGGAG
GCTGTGTCCCTAGGCGTCCCACACGAGGTGGCCGAGGGCGCCACCTGCCAGGCCTACGAA
TTGGCCGACTACAGCAACCTACGGGAGACCGATATTTAA
|
| Target 3 GenBank Gene ID |
|
| Target 3 GeneCard ID |
ADRA1D  |
| Target 3 GenAtlas ID |
ADRA1D  |
| Target 3 HGNC ID |
HGNC:280  |
| Target 3 Chromosome Location |
20 |
| Target 3 Locus |
20p13 |
| Target 3 SNPs |
SNPJam Report  |
| Target 3 General References |
- Deloukas P, Matthews LH, Ashurst J, Burton J, Gilbert JG, Jones M, Stavrides G, Almeida JP, Babbage AK, Bagguley CL, Bailey J, Barlow KF, Bates KN, Beard LM, Beare DM, Beasley OP, Bird CP, Blakey SE, Bridgeman AM, Brown AJ, Buck D, Burrill W, Butler AP, Carder C, Carter NP, Chapman JC, Clamp M, Clark G, Clark LN, Clark SY, Clee CM, Clegg S, Cobley VE, Collier RE, Connor R, Corby NR, Coulson A, Coville GJ, Deadman R, Dhami P, Dunn M, Ellington AG, Frankland JA, Fraser A, French L, Garner P, Grafham DV, Griffiths C, Griffiths MN, Gwilliam R, Hall RE, Hammond S, Harley JL, Heath PD, Ho S, Holden JL, Howden PJ, Huckle E, Hunt AR, Hunt SE, Jekosch K, Johnson CM, Johnson D, Kay MP, Kimberley AM, King A, Knights A, Laird GK, Lawlor S, Lehvaslaiho MH, Leversha M, Lloyd C, Lloyd DM, Lovell JD, Marsh VL, Martin SL, McConnachie LJ, McLay K, McMurray AA, Milne S, Mistry D, Moore MJ, Mullikin JC, Nickerson T, Oliver K, Parker A, Patel R, Pearce TA, Peck AI, Phillimore BJ, Prathalingam SR, Plumb RW, Ramsay H, Rice CM, Ross MT, Scott CE, Sehra HK, Shownkeen R, Sims S, Skuce CD, Smith ML, Soderlund C, Steward CA, Sulston JE, Swann M, Sycamore N, Taylor R, Tee L, Thomas DW, Thorpe A, Tracey A, Tromans AC, Vaudin M, Wall M, Wallis JM, Whitehead SL, Whittaker P, Willey DL, Williams L, Williams SA, Wilming L, Wray PW, Hubbard T, Durbin RM, Bentley DR, Beck S, Rogers J: The DNA sequence and comparative analysis of human chromosome 20. Nature. 2001 Dec 20-27;414(6866):865-71. [PubMed
]
- Bruno JF, Whittaker J, Song JF, Berelowitz M: Molecular cloning and sequencing of a cDNA encoding a human alpha 1A adrenergic receptor. Biochem Biophys Res Commun. 1991 Sep 30;179(3):1485-90. [PubMed
]
- Esbenshade TA, Hirasawa A, Tsujimoto G, Tanaka T, Yano J, Minneman KP, Murphy TJ: Cloning of the human alpha 1d-adrenergic receptor and inducible expression of three human subtypes in SK-N-MC cells. Mol Pharmacol. 1995 May;47(5):977-85. [PubMed
]
- Schwinn DA, Johnston GI, Page SO, Mosley MJ, Wilson KH, Worman NP, Campbell S, Fidock MD, Furness LM, Parry-Smith DJ, et al.: Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. J Pharmacol Exp Ther. 1995 Jan;272(1):134-42. [PubMed
]
- Weinberg DH, Trivedi P, Tan CP, Mitra S, Perkins-Barrow A, Borkowski D, Strader CD, Bayne M: Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c. Biochem Biophys Res Commun. 1994 Jun 30;201(3):1296-304. [PubMed
]
- Forray C, Bard JA, Wetzel JM, Chiu G, Shapiro E, Tang R, Lepor H, Hartig PR, Weinshank RL, Branchek TA, et al.: The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. Mol Pharmacol. 1994 Apr;45(4):703-8. [PubMed
]
|
| Target 3 Drug References |
- Yamamoto Y, Koike K: alpha(1)-Adrenoceptor subtypes in the mouse mesenteric artery and abdominal aorta. Br J Pharmacol. 2001 Nov;134(5):1045-54. [PubMed
]
- Nagaoka Y, Ahmed M, Hossain M, Bhuiyan MA, Ishiguro M, Nakamura T, Watanabe M, Nagatomo T: Amino acids of the human alpha1d-adrenergic receptor involved in antagonist binding. J Pharmacol Sci. 2008 Jan;106(1):114-20. Epub 2008 Jan 11. [PubMed
]
|