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1. Deprenalin
2. Deprenil
3. Deprenyl
4. E 250
5. E-250
6. E250
7. Eldepryl
8. Emsam
9. Humex
10. Jumex
11. L-deprenyl
12. Selegiline
13. Selegiline Hydrochloride, (r)-isomer
14. Selegiline Hydrochloride, (r,s)-isomer
15. Selegiline Hydrochloride, (s)-isomer
16. Selegiline, (r)-isomer
17. Selegiline, (r,s)-isomer
18. Selegiline, (s)-isomer
19. Selegyline
20. Yumex
21. Zelapar
1. 14611-52-0
2. Eldepryl
3. Selegiline Hcl
4. Zelapar
5. L-deprenyl Hydrochloride
6. (-)-deprenyl Hydrochloride
7. L-deprenyl
8. Ensam
9. (r)-n-methyl-n-(1-phenylpropan-2-yl)prop-2-yn-1-amine Hydrochloride
10. R-(-)-deprenyl Hydrochloride
11. Jumex
12. R-(-)-deprenyl (hydrochloride)
13. R(-)-deprenyl Hydrochloride
14. (r)-(-)-deprenyl Hydrochloride
15. (-)-phenylisopropylmethylpropynylamine
16. Otrasel
17. 6w731x367q
18. Nsc-759259
19. Benzeneethanamine, N,alpha-dimethyl-n-2-propyn-1-yl-, Hydrochloride (1:1), (alphar)-
20. Dsstox_cid_24584
21. Dsstox_rid_80331
22. Jumex Hydrochloride
23. Dsstox_gsid_44584
24. Eldepryl Hydrochloride
25. Zydis Selegiline
26. (2r)-n-methyl-1-phenyl-n-prop-2-ynylpropan-2-amine;hydrochloride
27. Chebi:9087
28. (-)-deprenil Hydrochloride
29. (-)-e-250 Hydrochloride
30. Smr000449328
31. Selegiline Hydrochloride [usan]
32. Hsdb 7183
33. Fpf1100
34. Sr-01000597928
35. Plurimen
36. Seledat
37. Vivapryl
38. Xilopar
39. Ccris 8571
40. Unii-6w731x367q
41. Eldepryl (tn)
42. Prestwick_846
43. (r)-deprenyl Hcl
44. Selegiline Hydrochloride [usan:usp]
45. (-)-(r)-n,alpha-dimethyl-n-2-propynylphenethylamine Hydrochloride
46. (-)-n,alpha-dimethyl-n-2-propynylbenzeneethanamine Hydrochloride
47. Ncgc00016708-01
48. (-)-(r)-n,alpha-dimethyl-n-2-propynylphenethylamine Monohydrochloride
49. Cas-14611-52-0
50. R-(-)deprenyl Hydrochloride
51. Schembl41392
52. (-)-selegiline Hydrochloride
53. Mls000758294
54. Mls001423947
55. Mls002153281
56. Mls002222269
57. Chembl1200904
58. Dtxsid9044584
59. Hms1569p05
60. Fpf-1100
61. Selegiline Hydrochloride (jan/usp)
62. Tox21_110572
63. Tox21_301846
64. (r)-(-)-n,alpha-dimethyl-n-(2-propynyl)phenethylamine Hydrochloride
65. Mfcd00069299
66. Selegiline Hydrochloride [mi]
67. Selegiline Hydrochloride [jan]
68. Akos005166822
69. Benzeneethanamine, N,.alpha.-dimethyl-n-2-propynyl-, Hydrochloride, (r)-
70. Benzeneethanamine, N,alpha-dimethyl-n-2-propynyl-, Hydrochloride, (r)-
71. Tox21_110572_1
72. Ccg-100773
73. Ks-5098
74. Nc00023
75. Nc00605
76. Nsc 759259
77. Selegiline Hydrochloride [hsdb]
78. Selegiline Hydrochloride [mart.]
79. Selegiline Hydrochloride [vandf]
80. Ncgc00024994-06
81. Ncgc00255797-01
82. Selegiline Hydrochloride [usp-rs]
83. Selegiline Hydrochloride [who-dd]
84. Ac-18759
85. Hy-14199
86. Selegiline Hydrochloride [green Book]
87. Selegiline Hydrochloride [orange Book]
88. D00785
89. Selegiline Hydrochloride [ep Monograph]
90. Selegiline Hydrochloride [usp Monograph]
91. 611s520
92. Sr-01000597928-1
93. Sr-01000597928-5
94. Sr-01000597928-6
95. Q27108267
96. R-(-)-deprenyl Hydrochloride, Powder, >=98% (hplc)
97. Selegiline Hydrochloride 1.0 Mg/ml In Methanol (as Free Base)
98. (r)-(-)-n,alpha-dimethyl-n-(2-propynyl)phenethylamine Hcl
99. (r)-(-)-n-?-dimethyl-n-2-propynylbenzeneethanamine Hydrochloride
100. (r)-n-methyl-1-phenyl-n-prop-2-ynylpropan-2-amine Hydrochloride
101. (-)-(r)-n,.alpha.-dimethyl-n-2-propynylphenethylamine Hydrochloride
102. Selegiline Hydrochloride, European Pharmacopoeia (ep) Reference Standard
103. Benzeneethanamine, N,?-dimethyl-n-2-propyn-1-yl-, Hydrochloride (1:1), (?r)-
104. Selegiline Hydrochloride, United States Pharmacopeia (usp) Reference Standard
Molecular Weight | 223.74 g/mol |
---|---|
Molecular Formula | C13H18ClN |
Hydrogen Bond Donor Count | 1 |
Hydrogen Bond Acceptor Count | 1 |
Rotatable Bond Count | 4 |
Exact Mass | 223.1127773 g/mol |
Monoisotopic Mass | 223.1127773 g/mol |
Topological Polar Surface Area | 3.2 Ų |
Heavy Atom Count | 15 |
Formal Charge | 0 |
Complexity | 195 |
Isotope Atom Count | 0 |
Defined Atom Stereocenter Count | 1 |
Undefined Atom Stereocenter Count | 0 |
Defined Bond Stereocenter Count | 0 |
Undefined Bond Stereocenter Count | 0 |
Covalently Bonded Unit Count | 2 |
1 of 6 | |
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Drug Name | Eldepryl |
Drug Label | ELDEPRYL (selegiline hydrochloride) is a levorotatory acetylenic derivative of phenethylamine. It is commonly referred to in the clinical and pharmacological literature as l-deprenyl.The chemical name is: (R)-(-)-N,2-dimethyl-N-2-propynylphenethylami... |
Active Ingredient | Selegiline hydrochloride |
Dosage Form | Capsule |
Route | Oral |
Strength | 5mg |
Market Status | Prescription |
Company | Somerset |
2 of 6 | |
---|---|
Drug Name | Selegiline hydrochloride |
PubMed Health | Selegiline (By mouth) |
Drug Classes | Antiparkinsonian |
Drug Label | Selegiline hydrochloride is a levorotatory acetylenic derivative of phenethylamine. It is commonly referred to in the clinical and pharmacological literature as l-deprenyl. The chemical name is: (R)-(-)-N,2-dimethyl-N-2-propynylphenethylamine hydroch... |
Active Ingredient | Selegiline hydrochloride |
Dosage Form | Tablet; Capsule |
Route | Oral |
Strength | 5mg |
Market Status | Prescription |
Company | Apotex; Stason; Dava Pharms; Mylan |
3 of 6 | |
---|---|
Drug Name | Zelapar |
PubMed Health | Selegiline |
Drug Classes | Antidepressant, Antiparkinsonian |
Drug Label | ZELAPAR Orally Disintegrating Tablets contain selegiline hydrochloride, a levorotatory acetylenic derivative of phenthylamine. Selegiline hydrochloride is described chemically as: (-)-(R)-N, -dimethyl-N-2-propynylphenethylamine hydrochloride and it... |
Active Ingredient | Selegiline hydrochloride |
Dosage Form | Tablet, orally disintegrating |
Route | Oral |
Strength | 1.25mg |
Market Status | Prescription |
Company | Valeant Pharm Intl |
4 of 6 | |
---|---|
Drug Name | Eldepryl |
Drug Label | ELDEPRYL (selegiline hydrochloride) is a levorotatory acetylenic derivative of phenethylamine. It is commonly referred to in the clinical and pharmacological literature as l-deprenyl.The chemical name is: (R)-(-)-N,2-dimethyl-N-2-propynylphenethylami... |
Active Ingredient | Selegiline hydrochloride |
Dosage Form | Capsule |
Route | Oral |
Strength | 5mg |
Market Status | Prescription |
Company | Somerset |
5 of 6 | |
---|---|
Drug Name | Selegiline hydrochloride |
PubMed Health | Selegiline (By mouth) |
Drug Classes | Antiparkinsonian |
Drug Label | Selegiline hydrochloride is a levorotatory acetylenic derivative of phenethylamine. It is commonly referred to in the clinical and pharmacological literature as l-deprenyl. The chemical name is: (R)-(-)-N,2-dimethyl-N-2-propynylphenethylamine hydroch... |
Active Ingredient | Selegiline hydrochloride |
Dosage Form | Tablet; Capsule |
Route | Oral |
Strength | 5mg |
Market Status | Prescription |
Company | Apotex; Stason; Dava Pharms; Mylan |
6 of 6 | |
---|---|
Drug Name | Zelapar |
PubMed Health | Selegiline |
Drug Classes | Antidepressant, Antiparkinsonian |
Drug Label | ZELAPAR Orally Disintegrating Tablets contain selegiline hydrochloride, a levorotatory acetylenic derivative of phenthylamine. Selegiline hydrochloride is described chemically as: (-)-(R)-N, -dimethyl-N-2-propynylphenethylamine hydrochloride and it... |
Active Ingredient | Selegiline hydrochloride |
Dosage Form | Tablet, orally disintegrating |
Route | Oral |
Strength | 1.25mg |
Market Status | Prescription |
Company | Valeant Pharm Intl |
Monamine oxidase B inhibitor
O'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. 13th Edition, Whitehouse Station, NJ: Merck and Co., Inc., 2001., p. 1512
Selegiline is indicated for use with levodopa or levodopa and carbidopa combination in the treatment of idiopathic Parkinson's disease (paralysis agitans). /Included in US product labeling/ /Selegiline/
MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442
.... we report briefly on neurotoxicity associated with the immunodeficiency virus and discuss the effects of selegiline, a monoamine oxidase inhibitor which enhances dopamine availability in CNS on immunodeficiency virus-induced neurological disease. ... /MAO inhibitors may be potent mediators of the neuropathological deficits in immunodeficiency virus infection and factors which may accelerate the progression of the immunodeficiency virus --neurological disease./
PMID:14697901 Koutsilieri E et al; Neurotoxicology 25 (1-2): 267-70 (2004)
EXPTL Therapy: ... Twenty patients with mild-moderate pathological cerebral involution of atrophic and/or vascular origin, were treated with Selegiline (L-deprenyl), a monoamino-oxidase B inhibitor (10 mg/day for six months). Compared with a control group, Selegiline treated patients showed a statistically significant improvement in cognitive and behaviour capacities. At the end of investigation, "Mini Mental State" showed an improvement of 26.5% in Selegiline group and of 3.7% in control group (P < 0.01). "Echelle Clinique d'Aptitudes Intellectuelles" showed an improvement of 29.4% and of 10.8% respectively (P < 0.01). Selegiline treatment has shortened significantly the reaction times and has improved mnesic capacities. No side effects were observed during the study. /Selegiline/
PMID:12645393 Bettini R, Gorini M; Clin Ter 153 (6): 377-80 (2002)
For more Therapeutic Uses (Complete) data for SELEGILINE HYDROCHLORIDE (10 total), please visit the HSDB record page.
Pregnancy risk category: C /RISK CANNOT BE RULED OUT. Adequate, well controlled human studies are lacking, and animal studies have shown risk to the fetus or are lacking as well. There is a chance of fetal harm if the drug is given during pregnancy; but the potential benefits may outweigh the potential risk./
Physicians Desk Reference. 58th ed. Thomson PDR. Montvale, NJ 2004., p. 3176
Selegiline may decrease or inhibit salivary flow, thus contributing to the development of caries, periodontal disease, oral candidiasis, and discomfort.
MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2443
Therapeutic use may lead to increased tremor, bradykinesia, falling, dystonic symptoms, dyskinesias, hallucinations, confusion, sleep disturbance, headache, dry mouth, blurred vision, orthostatic hypotension, hypertension, poor appetite, urinary retention, and diaphoresis. Hypomanic behavior may be due to the l-amphetamine and l-amphetamine metabolites of selegiline.
Ellenhorn, M.J., S. Schonwald, G. Ordog, J. Wasserberger. Ellenhorn's Medical Toxicology: Diagnosis and Treatment of Human Poisoning. 2nd ed. Baltimore, MD: Williams and Wilkins, 1997., p. 659
In patients receiving levodopa, addition of selegiline hydrochloride may exacerbate levodopa-associated dyskinesias. This effect, which occurred in an average of 28% (range: 4-90%) of patients receiving the drug in clinical trials, usually occurs within 2 weeks after initiating selegiline therapy and generally is mitigated when the levodopa dosage is reduced ... . Involuntary movements, increased tremor, chorea, loss of balance, freezing, blepharospasm, increased bradykinesia, facial grimacing, speech problems, heavy leg, stiff neck, tardive dyskinesia, dystonic manifestations, festination, increased apraxia, and muscle cramping may occur in patients receiving selegiline. Bruxism, muscle twitching and myoclonic jerks have occurred in patients receiving levodopa and selegiline hydrochloride dosages exceeding 10 mg daily.
McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 2439
For more Drug Warnings (Complete) data for SELEGILINE HYDROCHLORIDE (12 total), please visit the HSDB record page.
Antidepressive Agents
Mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions. Several MONOAMINE OXIDASE INHIBITORS are useful as antidepressants apparently as a long-term consequence of their modulation of catecholamine levels. The tricyclic compounds useful as antidepressive agents (ANTIDEPRESSIVE AGENTS, TRICYCLIC) also appear to act through brain catecholamine systems. A third group (ANTIDEPRESSIVE AGENTS, SECOND-GENERATION) is a diverse group of drugs including some that act specifically on serotonergic systems. (See all compounds classified as Antidepressive Agents.)
Monoamine Oxidase Inhibitors
A chemically heterogeneous group of drugs that have in common the ability to block oxidative deamination of naturally occurring monoamines. (From Gilman, et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p414) (See all compounds classified as Monoamine Oxidase Inhibitors.)
Neuroprotective Agents
Drugs intended to prevent damage to the brain or spinal cord from ischemia, stroke, convulsions, or trauma. Some must be administered before the event, but others may be effective for some time after. They act by a variety of mechanisms, but often directly or indirectly minimize the damage produced by endogenous excitatory amino acids. (See all compounds classified as Neuroprotective Agents.)
Antiparkinson Agents
Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic antagonists. (See all compounds classified as Antiparkinson Agents.)
Selegiline and its metabolites are widely distributed into body tissues and cross the blood-brain barrier. Following IV administration of radiolabeled selegiline hydrochloride in mice, the parent drug and/or metabolites are rapidly and widely distributed to brain, liver, kidney, lung, heart, and brown fat. Following IV administration of radiolabeled selegiline hydrochloride in healthy adults, the highest accumulation of radioactivity occurred in the thalamus, basal ganglia, mesencephalon, and cingulate gyrus. /Selegiline/
McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 2441
Selegiline is excreted principally in urine as conjugated and unconjugated metabolites. About 20-63% of an orally administered dose of selegiline is excreted in urine as l-methamphetamine, 9-26% as l-amphetamine, and 1% as l-demethylselegiline. ... About 15% of a dose is excreted in feces within 72 hours following administration of selegiline. /SRP: This would usually result in a false positive drug test for d-methamphetamine if no d/l-isomer characterization was performed on the specimen./ /Selegiline/
McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 2441
Rapidly absorbed from the gastrointestinal tract.
MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442
... The mean peak plasma concentration (Cmax) is approximately 2 ug/L and the time to reach the peak is under an hour. The absolute bioavailability of selegiline is approximately 10%. It has an apparent volume of distribution of 1854 L. The oral clearance of selegiline (59 L/min) is many fold higher than the liver blood flow (1.5 L/min), indicating that extrahepatic processes are involved in the elimination of selegiline. ... /Selegiline/
PMID:9260033 Mahmood I; Clin Pharmacokinet 33 (2): 91-102 (1997)
... Selegiline is readily absorbed from the gastrointestinal tract and rapidly enters the brain and spinal cord following oral administration. The drug binds to brain regions with a high MAO-B content, such as the thalamus, the striatum, the cortex, and the brainstem. ... /Selegiline/
Gerlach M et al; Neurology 47 (6 Suppl 3): S137-45 (1996)
Selegiline is excreted principally in urine as conjugated and unconjugated metabolites. About 20-63% of an orally administered dose of selegiline is excreted in urine as l-methamphetamine, 9-26% as l-amphetamine, and 1% as l-demethylselegiline. /Selegiline/
McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 2441
Rapidly and completely metabolized to N-desmethyldeprenyl, l-methamphetamine, and l-amphetamine.
MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442
Selegiline is extensively metabolized, presumably through cytochrome p450 mediated oxygenation, to form l-desmethylselegiline and l-methamphetamine, which is further metabolized to l-amphetamine. Selegiline also is metabolized in the lungs to l-desmethylselegiline and l-methamphetamine and in the kidneys to l-methamphetamine, but the degree of metabolism in these tissues is minimal compared with that in the liver. /Selegiline/
McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 2441
... The pharmacokinetics of selegiline are highly variable. Following an oral dose of selegiline 10 mg, it is rapidly absorbed and metabolized to desmethylselegiline, levoamphetamine and levomethamphetamine. /Selegiline/
PMID:9260033 Mahmood I; Clin Pharmacokinet 33 (2): 91-102 (1997)
For more Metabolism/Metabolites (Complete) data for SELEGILINE HYDROCHLORIDE (6 total), please visit the HSDB record page.
Elimination: Selegiline: 39 (range, 16 to 69) hours. /Selegiline/
MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442
The mean half-lives of the 3 active metabolites that were found in serum and urine following a single dose of selegiline are as follows: N-desmethyldeprenyl, 2 hours; l-amphetamine, 17.7 hours; l-methamphetamine, 20.5 hours. /Selegiline/
MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442
The action of selegiline is thought to be related to its irreversible inhibition of monoamine oxidase type B (MAO B), the major form of the enzyme in the human brain. MAO B, which is involved in the oxidative deamination of dopamine in the brain, is inhibited when selegiline binds covalently and stoichiometrically to the isoalloxazine flavin adenine dinucleotide (FAD) at its active center. Administration of 10 mg of selegiline a day produces almost complete inhibition of MAO B in the brain. Selegiline becomes a nonselective inhibitor of all monamine oxidase (MAO) at higher doses, possibly at 20 to 40 mg a day. At these doses, tyramine-mediated hypertensive reaction with MAO A blockade ("cheese reactions") may occur. /Selegiline/
MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442
Selegiline (or its metabolites) may also act through other mechanisms to increase dopaminergic activity, including interfering with dopamine reuptake at the synapse. /Selegiline/
MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442
The mechanism of action of selegiline is complex and cannot be explained solely by its MAO-B inhibitory action. Pretreatment with selegiline can protect neurons against a variety of neurotoxins, such as 1-methyl-4-phenyl-1,2,3,6 tetrahydropyridine (MPTP), 6-hydroxydopamine, N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine (DSP-4), methyl-beta-acetoxyethyl-2-chloroethylamine (AF64A), and 5,6-dihydroxyserotonin, which damage dopaminergic, adrenergic, cholinergic, and sertoninergic neurons, respectively. Selegiline produces an amphetamine-like effect, enhances the release of dopamine, and blocks the reuptake of dopamine. It stimulates gene expression of L-aromatic amino acid decarboxylase, increases striatal phenylethylamine levels, and activates dopamine receptors. Selegiline reduces the production of oxidative radicals, up-regulates superoxide dismutase and catalase, and suppresses nonenzymatic and iron-catalyzed autooxidation of dopamine. Selegiline compensates for loss of target-derived trophic support, delays apoptosis in serum-deprived cells, and blocks apoptosis-related fall in the mitochondrial membrane potential. Most of the aforementioned properties occur independently of selegiline's efficacy to inhibit MAO-B. /Selegiline/
PMID:11813232 Ebadi M et al; J Neurosci Res 67 (3): 285-9 (2002)
Selegiline is a selective inhibitor of monoamine oxidase-B (MAO-B) at a dose of 10 mg/day and is given to patients with Parkinson's disease as an adjunct to levodopa therapy. By inhibiting MAO-B, selegiline increases the dopamine levels in the substantia nigra. Selegiline also blocks dopamine re-uptake from the synaptic cleft, thus increasing the dopamine concentrations in the brain. ... /Selegiline/
PMID:9260033 Mahmood I; Clin Pharmacokinet 33 (2): 91-102 (1997)
For more Mechanism of Action (Complete) data for SELEGILINE HYDROCHLORIDE (6 total), please visit the HSDB record page.