Target Information
| Target General Information | Top | |||||
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| Target ID |
T92609
(Former ID: TTDC00292)
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| Target Name |
Adrenergic receptor alpha-1A (ADRA1A)
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| Synonyms |
Alpha-adrenergic receptor 1c; Alpha-1C adrenergic receptor; Alpha-1A adrenoreceptor; Alpha-1A adrenoceptor; Alpha-1A adrenergic receptor; Alpha adrenergic receptor 1c; Alpha 1A-adrenoreceptor; Alpha 1A-adrenoceptor; ADRA1C
Click to Show/Hide
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| Gene Name |
ADRA1A
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Hypertension [ICD-11: BA00-BA04] | |||||
| 2 | Prostate hyperplasia [ICD-11: GA90] | |||||
| Function |
Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes. This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MVFLSGNASDSSNCTQPPAPVNISKAILLGVILGGLILFGVLGNILVILSVACHRHLHSV
THYYIVNLAVADLLLTSTVLPFSAIFEVLGYWAFGRVFCNIWAAVDVLCCTASIMGLCII SIDRYIGVSYPLRYPTIVTQRRGLMALLCVWALSLVISIGPLFGWRQPAPEDETICQINE EPGYVLFSALGSFYLPLAIILVMYCRVYVVAKRESRGLKSGLKTDKSDSEQVTLRIHRKN APAGGSGMASAKTKTHFSVRLLKFSREKKAAKTLGIVVGCFVLCWLPFFLVMPIGSFFPD FKPSETVFKIVFWLGYLNSCINPIIYPCSSQEFKKAFQNVLRIQCLCRKQSSKHALGYTL HPPSQAVEGQHKDMVRIPVGSRETFYRISKTDGVCEWKFFSSMPRGSARITVSKDQSSCT TARVRSKSFLQVCCCVGPSTPSLDKNHQVPTIKVHTISLSENGEEV Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A00273 ; BADD_A02979 ; BADD_A04075 | |||||
| HIT2.0 ID | T22XGJ | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 4 Approved Drugs | + | ||||
| 1 | NAFTOPIDIL | Drug Info | Approved | Hypertension | [2] | |
| 2 | SILODOSIN | Drug Info | Approved | Benign prostatic hyperplasia | [3], [4], [5] | |
| 3 | Tamsulosin | Drug Info | Approved | Benign prostatic hyperplasia | [6], [7] | |
| 4 | Xatral | Drug Info | Approved | Benign prostatic hyperplasia | [2] | |
| Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
| 1 | Besipirdine | Drug Info | Phase 3 | Cognitive impairment | [8] | |
| 2 | Dutasteride + tamsulosin | Drug Info | Phase 3 | Benign prostatic hyperplasia | [9] | |
| 3 | MEDETOMIDINE | Drug Info | Phase 2 | Pain | [10] | |
| Patented Agent(s) | [+] 2 Patented Agents | + | ||||
| 1 | PMID30124346-Compound-LDT66 | Drug Info | Patented | Benign prostatic hyperplasia | [11] | |
| 2 | PMID30124346-Compound-LDT8 | Drug Info | Patented | Benign prostatic hyperplasia | [11] | |
| Discontinued Drug(s) | [+] 11 Discontinued Drugs | + | ||||
| 1 | L-771688 | Drug Info | Discontinued in Phase 2 | Prostate disease | [12] | |
| 2 | RBx-2258 | Drug Info | Discontinued in Phase 2 | Prostate hyperplasia | [13] | |
| 3 | REC-15-2739 | Drug Info | Discontinued in Phase 2 | Prostate disease | [14] | |
| 4 | SOU-001 | Drug Info | Discontinued in Phase 2 | Urinary incontinence | [15] | |
| 5 | Taprizosin | Drug Info | Discontinued in Phase 2 | Prostate hyperplasia | [16] | |
| 6 | RS-100975 | Drug Info | Discontinued in Phase 1 | Prostate disease | [17], [18] | |
| 7 | SDZ-NVI-085 | Drug Info | Discontinued in Phase 1 | Major depressive disorder | [19] | |
| 8 | A-204176 | Drug Info | Terminated | Stress urinary incontinence | [21] | |
| 9 | KRG-3332 | Drug Info | Terminated | Glaucoma/ocular hypertension | [22] | |
| 10 | L-757464 | Drug Info | Terminated | Prostate hyperplasia | [23] | |
| 11 | SNAP-5089 | Drug Info | Terminated | Heart arrhythmia | [24], [25] | |
| Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
| 1 | CM-2236 | Drug Info | Preclinical | Post-traumatic stress disorder | [20] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Inhibitor | [+] 80 Inhibitor drugs | + | ||||
| 1 | NAFTOPIDIL | Drug Info | [26] | |||
| 2 | SILODOSIN | Drug Info | [26] | |||
| 3 | MEDETOMIDINE | Drug Info | [30] | |||
| 4 | Sunepitron | Drug Info | [31] | |||
| 5 | TIOSPIRONE | Drug Info | [32] | |||
| 6 | L-771688 | Drug Info | [26] | |||
| 7 | MAZAPERTINE | Drug Info | [33] | |||
| 8 | REC-15-2739 | Drug Info | [26] | |||
| 9 | A-131701 | Drug Info | [26] | |||
| 10 | ABANOQUIL | Drug Info | [41] | |||
| 11 | AGN-193080 | Drug Info | [42] | |||
| 12 | BMY-7378 | Drug Info | [43] | |||
| 13 | NIGULDIPINE | Drug Info | [46] | |||
| 14 | Siramesine | Drug Info | [47] | |||
| 15 | SK&F-104078 | Drug Info | [46] | |||
| 16 | SK&F-104856 | Drug Info | [46] | |||
| 17 | SNAP-5089 | Drug Info | [46] | |||
| 18 | SNAP-6201 | Drug Info | [26] | |||
| 19 | WB-4101 | Drug Info | [41] | |||
| 20 | (+/-)-nantenine | Drug Info | [48] | |||
| 21 | (-)-SNAP-5399 | Drug Info | [26] | |||
| 22 | (2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine | Drug Info | [49] | |||
| 23 | (2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine | Drug Info | [49] | |||
| 24 | 1',2',3',6'-Tetrahydro-[2,4']bipyridinyl | Drug Info | [50] | |||
| 25 | 1-(2-Chloro-phenyl)-piperazine | Drug Info | [51] | |||
| 26 | 1-(2-Methoxy-phenyl)-piperazine | Drug Info | [51] | |||
| 27 | 1-(3-Fluoro-pyridin-2-yl)-4-methyl-piperazine | Drug Info | [50] | |||
| 28 | 1-(pyridin-2-yl)piperazine | Drug Info | [50] | |||
| 29 | 2-(4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole | Drug Info | [52] | |||
| 30 | 2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [53] | |||
| 31 | 4-((E)-1-Naphthalen-1-yl-propenyl)-1H-imidazole | Drug Info | [54] | |||
| 32 | 4-((Z)-1-Naphthalen-1-yl-propenyl)-1H-imidazole | Drug Info | [54] | |||
| 33 | 4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole | Drug Info | [30] | |||
| 34 | 4-(1-Naphthalen-1-yl-propyl)-1H-imidazole | Drug Info | [54] | |||
| 35 | 4-(1-Naphthalen-1-yl-vinyl)-1H-imidazole | Drug Info | [54] | |||
| 36 | 4-(2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazole | Drug Info | [54] | |||
| 37 | 4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline | Drug Info | [53] | |||
| 38 | 4-(3-Hydroxy-piperidin-3-yl)-benzene-1,2-diol | Drug Info | [55] | |||
| 39 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [56] | |||
| 40 | 4-(4-chlorobenzyl)-2-allylphthalazin-1(2H)-one | Drug Info | [57] | |||
| 41 | 4-(4-chlorobenzyl)-2-methylphthalazin-1(2H)-one | Drug Info | [57] | |||
| 42 | 4-(4-chlorobenzyl)phthalazin-1(2H)-one | Drug Info | [57] | |||
| 43 | 4-(4-Isopropyl-morpholin-2-yl)-benzene-1,2-diol | Drug Info | [55] | |||
| 44 | 4-(4-Methyl-indan-1-yl)-1H-imidazole | Drug Info | [58] | |||
| 45 | 4-Benzo[b]thiophen-4-yl-1H-imidazole | Drug Info | [59] | |||
| 46 | 4-benzyl-2-methylphthalazin-1(2H)-one | Drug Info | [57] | |||
| 47 | 4-Morpholin-2-yl-benzene-1,2-diol | Drug Info | [55] | |||
| 48 | 5-Bromo-8-piperazin-1-yl-imidazo[1,2-a]pyrazine | Drug Info | [60] | |||
| 49 | 8-Piperazin-1-yl-imidazo[1,2-a]pyrazine | Drug Info | [60] | |||
| 50 | A-119637 | Drug Info | [26] | |||
| 51 | A-123189 | Drug Info | [26] | |||
| 52 | A-315456 | Drug Info | [26] | |||
| 53 | AGN-192172 | Drug Info | [42] | |||
| 54 | CORYNANTHEINE | Drug Info | [26] | |||
| 55 | FLUANISONE | Drug Info | [62] | |||
| 56 | Imidazolidin-2-ylidene-o-tolyl-amine | Drug Info | [42] | |||
| 57 | Imidazolidin-2-ylidene-quinoxalin-6-yl-amine | Drug Info | [42] | |||
| 58 | ISOCLOZAPINE | Drug Info | [64] | |||
| 59 | L-765314 | Drug Info | [26] | |||
| 60 | LEVONORDEFRIN | Drug Info | [54] | |||
| 61 | N-(5-Bromo-quinoxalin-6-yl)-guanidine | Drug Info | [42] | |||
| 62 | OCTOCLOTHEPIN | Drug Info | [65] | |||
| 63 | R-226161 | Drug Info | [66] | |||
| 64 | Ro-11-04253 | Drug Info | [26] | |||
| 65 | RS-100329 | Drug Info | [26] | |||
| 66 | RS-513815 | Drug Info | [26] | |||
| 67 | RWJ-38063 | Drug Info | [26] | |||
| 68 | RWJ-68141 | Drug Info | [26] | |||
| 69 | RWJ-68157 | Drug Info | [26] | |||
| 70 | RWJ-69736 | Drug Info | [26] | |||
| 71 | SK&F-105854 | Drug Info | [26] | |||
| 72 | SK&F-106686 | Drug Info | [46] | |||
| 73 | SK&F-86466 | Drug Info | [46] | |||
| 74 | SNAP-5036 | Drug Info | [26] | |||
| 75 | SNAP-7915 | Drug Info | [26] | |||
| 76 | SNAP-8719 | Drug Info | [43] | |||
| 77 | SNAP-94847 | Drug Info | [68] | |||
| 78 | UH-301 | Drug Info | [69] | |||
| 79 | [3H]RX821002 | Drug Info | [70] | |||
| 80 | [3H]spiperone | Drug Info | [26] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | Tamsulosin | Drug Info | [27] | |||
| 2 | SOU-001 | Drug Info | [35] | |||
| Antagonist | [+] 12 Antagonist drugs | + | ||||
| 1 | Xatral | Drug Info | [1] | |||
| 2 | Besipirdine | Drug Info | [28] | |||
| 3 | Dutasteride + tamsulosin | Drug Info | [29] | |||
| 4 | PMID30124346-Compound-LDT8 | Drug Info | [11] | |||
| 5 | RBx-2258 | Drug Info | [34] | |||
| 6 | Taprizosin | Drug Info | [36] | |||
| 7 | RS-100975 | Drug Info | [37] | |||
| 8 | SDZ-NVI-085 | Drug Info | [38] | |||
| 9 | KRG-3332 | Drug Info | [44] | |||
| 10 | L-757464 | Drug Info | [45] | |||
| 11 | GG-818 | Drug Info | [63] | |||
| 12 | REC2615 | Drug Info | [67] | |||
| Agonist | [+] 3 Agonist drugs | + | ||||
| 1 | CM-2236 | Drug Info | [39] | |||
| 2 | A-204176 | Drug Info | [40] | |||
| 3 | Beta-methoxyamphetamine | Drug Info | [61] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Human Similarity Proteins
Human Pathway Affiliation
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| Calcium signaling pathway | hsa04020 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| cGMP-PKG signaling pathway | hsa04022 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| AMPK signaling pathway | hsa04152 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Adrenergic signaling in cardiomyocytes | hsa04261 | Affiliated Target |
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| Class: Organismal Systems => Circulatory system | Pathway Hierarchy | ||
| Vascular smooth muscle contraction | hsa04270 | Affiliated Target |
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| Class: Organismal Systems => Circulatory system | Pathway Hierarchy | ||
| Salivary secretion | hsa04970 | Affiliated Target |
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| Class: Organismal Systems => Digestive system | Pathway Hierarchy | ||
| Click to Show/Hide the Information of Affiliated Human Pathways | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 7 KEGG Pathways | + | ||||
| 1 | Calcium signaling pathway | |||||
| 2 | cGMP-PKG signaling pathway | |||||
| 3 | Neuroactive ligand-receptor interaction | |||||
| 4 | AMPK signaling pathway | |||||
| 5 | Adrenergic signaling in cardiomyocytes | |||||
| 6 | Vascular smooth muscle contraction | |||||
| 7 | Salivary secretion | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | Alpha adrenergic receptor signaling pathway | |||||
| Reactome | [+] 3 Reactome Pathways | + | ||||
| 1 | Adrenoceptors | |||||
| 2 | G alpha (q) signalling events | |||||
| 3 | G alpha (12/13) signalling events | |||||
| WikiPathways | [+] 8 WikiPathways | + | ||||
| 1 | Monoamine GPCRs | |||||
| 2 | Calcium Regulation in the Cardiac Cell | |||||
| 3 | GPCRs, Class A Rhodopsin-like | |||||
| 4 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| 5 | Endothelin Pathways | |||||
| 6 | GPCR ligand binding | |||||
| 7 | GPCR downstream signaling | |||||
| 8 | AMPK Signaling | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Pharma & Vaccines. Product Development Pipeline. April 29 2009. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 493). | |||||
| REF 4 | 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6. | |||||
| REF 5 | Silodosin: a selective alpha1A-adrenergic receptor antagonist for the treatment of benign prostatic hyperplasia. Clin Ther. 2009 Nov;31(11):2489-502. | |||||
| REF 6 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 488). | |||||
| REF 7 | Alpha blockers for the treatment of benign prostatic hyperplasia. Rev Urol. 2007 Fall;9(4):181-90. | |||||
| REF 8 | Clinical pipeline report, company report or official report of UroGene. | |||||
| REF 9 | ClinicalTrials.gov (NCT00090103) Benign Prostatic Hyperplasia Trial With Dutasteride And Tamsulosin Combination Treatment. U.S. National Institutes of Health. | |||||
| REF 10 | Sedative and cardiopulmonary effects of medetomidine hydrochloride and xylazine hydrochloride and their reversal with atipamezole hydrochloride in calves. Am J Vet Res. 2008 Mar;69(3):319-29. | |||||
| REF 11 | 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689. | |||||
| REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014018) | |||||
| REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011920) | |||||
| REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003537) | |||||
| REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014478) | |||||
| REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017098) | |||||
| REF 17 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 497). | |||||
| REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013213) | |||||
| REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001726) | |||||
| REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029346) | |||||
| REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013646) | |||||
| REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018805) | |||||
| REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010051) | |||||
| REF 24 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 498). | |||||
| REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006771) | |||||
| REF 26 | Pharmacophore identification of alpha(1A)-adrenoceptor antagonists. Bioorg Med Chem Lett. 2005 Feb 1;15(3):657-64. | |||||
| REF 27 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 28 | Alpha-Adrenergic activity and cardiovascular effects of besipirdine HCl (HP 749) and metabolite P7480 in vitro and in the conscious rat and dog. J Pharmacol Exp Ther. 1997 Apr;281(1):337-46. | |||||
| REF 29 | Clinical pipeline report, company report or official report of GlaxoSmithKline (2009). | |||||
| REF 30 | A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic recep... J Med Chem. 1994 Jul 22;37(15):2328-33. | |||||
| REF 31 | An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment o... J Med Chem. 2006 Jun 1;49(11):3116-35. | |||||
| REF 32 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. J Med Chem. 1996 Jan 5;39(1):143-8. | |||||
| REF 33 | A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. J Med Chem. 1994 Apr 15;37(8):1060-2. | |||||
| REF 34 | Drug Metabolism and Pharmacokinetics. Indian J Pharmacol. 2008 October; 40(Suppl 2): S91-S97. | |||||
| REF 35 | Drug repositioning: identifying and developing new uses for existing drugs. Nat Rev Drug Discov. 2004 Aug;3(8):673-83. | |||||
| REF 36 | Impact of physicochemical and structural properties on the pharmacokinetics of a series of alpha1L-adrenoceptor antagonists. Drug Metab Dispos. 2007 Aug;35(8):1435-45. | |||||
| REF 37 | In vitro alpha1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel alpha1A-adrenoceptor selective antagonists. Br J Pharmacol. 1999 May;127(1):252-8. | |||||
| REF 38 | SDZ NVI 085, an alpha 1A-adrenoceptor agonist with 5-HT2A receptor antagonist properties. Eur J Pharmacol. 1996 Feb 15;297(1-2):83-6. | |||||
| REF 39 | CN patent application no. 104151292, Indole derivative or a pharmaceutically acceptable salt thereof. | |||||
| REF 40 | Pharmacological properties of A-204176, a novel and selective alpha1A adrenergic agonist, in in vitro and in vivo models of urethral function. Life Sci. 2001 Nov 30;70(2):181-97. | |||||
| REF 41 | Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. J Med Chem. 1995 Sep 1;38(18):3415-44. | |||||
| REF 42 | Analogs of UK 14,304: Structural features responsible for alpha2 adrenoceptor activity, Bioorg. Med. Chem. Lett. 5(15):1745-1750 (1995). | |||||
| REF 43 | Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione ... J Med Chem. 2005 Apr 21;48(8):3076-9. | |||||
| REF 44 | The beta-adrenoceptor. Am J Respir Crit Care Med. 1998 Nov;158(5 Pt 3):S146-53. | |||||
| REF 45 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010051) | |||||
| REF 46 | Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. J Med Chem. 1995 Sep 15;38(19):3681-716. | |||||
| REF 47 | Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. J Med Chem. 1995 May 26;38(11):1998-2008. | |||||
| REF 48 | Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. | |||||
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