| Version |
2.5 |
| Creation Date |
2005-06-13 13:24:05 |
| Update Date |
2009-02-19 16:04:58 |
| Primary Accession Number |
DB01162 |
| Secondary Accession Number |
|
| Name |
Terazosin |
| Drug Type |
|
| Description |
Terazosin is a selective alpha 1 antagonist used for treatment of symptoms of prostate enlargement (BPH). It also acts to lower blood pressure, so it is a drug of choice for men with hypertension and prostate enlargement. It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls. |
| Synonyms |
- Abbott 45975
- Terazosin HCl
- Terazosin hydrochloride
- Terazosina [INN-Spanish]
- Terazosine
- Terazosine [INN-French]
- Terazosinum [INN-Latin]
- Trazosin HCl
|
| Brand Names |
- Blavin
- Flumarc
- Fosfomic
- Heitrin
- Hytracin
- Hytrin
- Hytrinex
- Itrin
- Urodie
- Vasocard
- Vasomet
- Vicard
|
| Brand Mixtures |
Not Available |
| Chemical IUPAC Name |
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(oxolan-2-yl)methanone |
| Chemical Formula |
C19H25N5O4 |
| Chemical Structure |
 |
| CAS Registry Number |
63590-64-7 |
| InChI Identifier |
InChI=1/C19H25N5O4/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/h10-11,14H,3-9H2,1-2H3,(H2,20,21,22)/f/h20H2 |
| InChI Key |
VCKUSRYTPJJLNI-HPHMPNDVCS |
| KEGG Drug |
Not Available |
| KEGG Compound |
C07127  |
| PubChem Compound |
5401  |
| PubChem Substance |
9337  |
| ChEBI ID |
Not Available |
| PharmGKB ID |
PA451612  |
| HET ID |
Not Available |
| GenBank ID |
Not Available |
| Drug ID Number [DIN] |
02243749  |
| RxList Link |
http://www.rxlist.com/cgi/generic/teraz.htm  |
| PDRhealth Link |
Not Available |
| Wikipedia Link |
http://en.wikipedia.org/wiki/Terazosin  |
| FDA Label |
|
| Material Safety Data Sheet (MSDS) |
Not Available |
| Synthesis Reference |
M. Winn et al., U.S. Pat. 4,026,894 (1977) |
| Average Molecular Weight |
387.4329 |
| Monoisotopic Molecular Weight |
387.1907 |
| State |
Solid |
| Melting Point |
273 oC |
| Experimental Water Solubility |
29.7mg/mL
Source: PhysProp
|
| Predicted Water Solubility |
1.50e+00 mg/mL
Calculated using ALOGPS
|
| Experimental LogP/Hydrophobicity |
1
Source: PhysProp
|
| Predicted LogP |
1.12
Calculated using ALOGPS
|
| Experimental LogS |
Not Available |
| Predicted LogS |
-2.41
Calculated using ALOGPS
|
| Experimental Caco2 Permeability |
Not Available |
| 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)[C@H]1CCCO1 |
| Canonical SMILES |
COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1CCCO1 |
| Drug Category |
- Adrenergic alpha-Antagonists
- Antineoplastic Agents
- Platelet Aggregation Inhibitors
|
| ATC Codes |
|
| AHFS Codes |
|
| Indication |
For the treatment of symptomatic benign prostatic hyperplasia (BPH) and also for hypertension. |
| Pharmacology |
Terazosin, classified as a quinazoline, is similar to doxazosin and prazosin. As an alpha-adrenergic blocking agent, terazosin is used to treat hypertension and benign prostatic hypertrophy (BPH). Terazosin produces vasodilation and reduces peripheral resistance but in general has slight effect on cardiac output. Antihypertensive effect with chronic dosing is usually not accompanied by reflex tachycardia. |
| Mechanism of Action |
Terazosin selectively and competitively inhibits vascular postsynaptic alpha(1)-adrenergic receptors, resulting in peripheral vasodilation and a reduction of vascular resistance and blood pressure. Unlike the nonselective alph-adrenergic blockers phenoxybenzamine and phentolamine, terazosin does not block presynaptic alpha(2)-receptors and, hence, does not cause reflex activation of norepinephrine release to produce reflex tachycardia. |
| Absorption |
Essentially completely absorbed in man (90% bioavailability). |
| Toxicity |
LD50=259.3mg/kg (i.v. in mice) |
| Protein Binding |
90-94% |
| Biotransformation |
Hepatic. One of the four metabolites identified (piperazine derivative of terazosin) has antihypertensive activity. |
| Half Life |
12 hours |
| Dosage Forms |
|
| Patient Information |
Show  |
| Contraindications |
Show  |
| Interactions |
Show  |
| Drug Interactions |
| Drug |
Interaction |
| Acebutolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Alfuzosin |
Additive antihypertensive effects may occur. Increase risk of orthostatic hypotension and syncope. Concomitant therapy should be avoided. |
| Amifostine |
Terazosin may increase the hypotensive effect of Amifostine. At chemotherapeutic doses of Amifostine, Terazosin should be withheld for 24 hours prior to Amifostine administration. Use caution at lower doses of Amifostine. |
| Atenolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Betaxolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Bisoprolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Carteolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Carvedilol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Celiprolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Esmolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Labetalol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Metoprolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Nadolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Nebivolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Oxprenolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Penbutolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Pindolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Propranolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Rituximab |
Additive antihypertensive effects may occur. Increased risk of hypotension. Consider withholding Terazosin for 12 hours prior to administration of Rituximab. |
| Sildenafil |
Increased risk of hypotension. |
| Sotalol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Tadalafil |
Risk of significant hypotension with this association |
| Tamsulosin |
Additive antihypertensive effects may occur. Increase risk of orthostatic hypotension and syncope. Concomitant therapy should be avoided. |
| Timolol |
Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Vardenafil |
Increased risk of hypotension. |
| silodosin |
Additive antihypertensive effects may occur. Increase risk of orthostatic hypotension and syncope. Concomitant therapy should be avoided. |
|
| Food Interactions |
Not Available
|
| Pathways |
Not Available
|
| General References |
- Drugs.com

- 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 |
- Na YJ, Guo YL, Gu FL: Clinical comparison of selective and non-selective alpha 1A-adrenoceptor antagonists for bladder outlet obstruction associated with benign prostatic hyperplasia: studies on tamsulosin and terazosin in Chinese patients. The Chinese Tamsulosin Study Group. J Med. 1998;29(5-6):289-304. [PubMed
]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed
]
- Roehrborn CG, Schwinn DA: Alpha1-adrenergic receptors and their inhibitors in lower urinary tract symptoms and benign prostatic hyperplasia. J Urol. 2004 Mar;171(3):1029-35. [PubMed
]
- Michel MC, Grubbel B, Taguchi K, Verfurth F, Otto T, Kropfl D: Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned alpha 1-adrenoceptor subtypes and in human prostate. J Auton Pharmacol. 1996 Feb;16(1):21-8. [PubMed
]
- Lee E, Lee C: Clinical comparison of selective and non-selective alpha 1A-adrenoreceptor antagonists in benign prostatic hyperplasia: studies on tamsulosin in a fixed dose and terazosin in increasing doses. Br J Urol. 1997 Oct;80(4):606-11. [PubMed
]
- Chapple CR: Medical therapy and quality of life. Eur Urol. 1998;34 Suppl 2:10-7; discussion 46. [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 |
- Boyle P, Robertson C, Manski R, Padley RJ, Roehrborn CG: Meta-analysis of randomized trials of terazosin in the treatment of benign prostatic hyperplasia. Urology. 2001 Nov;58(5):717-22. [PubMed
]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed
]
- Vincent J, Dachman W, Blaschke TF, Hoffman BB: Pharmacological tolerance to alpha 1-adrenergic receptor antagonism mediated by terazosin in humans. J Clin Invest. 1992 Nov;90(5):1763-8. [PubMed
]
- Simpson P: Stimulation of hypertrophy of cultured neonatal rat heart cells through an alpha 1-adrenergic receptor and induction of beating through an alpha 1- and beta 1-adrenergic receptor interaction. Evidence for independent regulation of growth and beating. Circ Res. 1985 Jun;56(6):884-94. [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 |
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed
]
|