Guanabenz |
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| Trade names | Wytensin |
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| AHFS/Drugs.com | Consumer Drug Information |
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| MedlinePlus | a686003 |
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| ATC code | |
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| Protein binding | 90% |
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| Elimination half-life | 6 hours |
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2-(2,6-dichlorobenzylidene)hydrazinecarboximidamide
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| ECHA InfoCard | 100.023.410 |
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| Formula | C8H8Cl2N4 |
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| Molar mass | 231.08 g·mol−1 |
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| 3D model (JSmol) | |
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Clc1cccc(Cl)c1\C=N\N=C(/N)N
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InChI=1S/C8H8Cl2N4/c9-6-2-1-3-7(10)5(6)4-13-14-8(11)12/h1-4H,(H4,11,12,14)/b13-4+ YKey:WDZVGELJXXEGPV-YIXHJXPBSA-N Y
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Guanabenz (pronounced GWAHN-a-benz, sold under the trade name Wytensin) is an alpha agonist that is selective to the alpha-2 adrenergic receptor. Guanabenz is used as an antihypertensive drug used in the treatment of high blood pressure (hypertension).[1][2]
The most common side effects during guanabenz therapy are dizziness, drowsiness, dry mouth, headache and weakness.[3]
Guanabenz can make one drowsy or less alert, therefore driving or operating dangerous machinery is not recommended.
Research
Guanabenz also has some anti-inflammatory properties in different pathological situations, including multiple sclerosis.[4]
Guanabenz was found in one study to exert an inhibitory effect by decreasing the abundance of the enzyme CH25H, a cholesterol hydroxylase linked to antiviral immunity. Therefore, it is suggested that the drug and similar compounds could be used to treat type I interferon-dependent pathologies and that the CH25H enzyme could be a therapeutic target to control these diseases,[5] including amyotrophic lateral sclerosis.
See also
References
- ^ Walker BR, Hare LE, Deitch MW (1982). "Comparative antihypertensive effects of guanabenz and clonidine". The Journal of International Medical Research. 10 (1): 6–14. doi:10.1177/030006058201000102. PMID 7037502. S2CID 2139809.
- ^ Bonham AC, Trapani AJ, Portis LR, Brody MJ (December 1984). "Studies on the mechanism of the central antihypertensive effect of guanabenz and clonidine". Journal of Hypertension Supplement. 2 (3): S543–S546. PMID 6599714.
- ^ "Guanabenz | The Merck Index Online". www.rsc.org. Retrieved 2023-04-17.
- ^ Way SW, Podojil JR, Clayton BL, Zaremba A, Collins TL, Kunjamma RB, et al. (March 2015). "Pharmaceutical integrated stress response enhancement protects oligodendrocytes and provides a potential multiple sclerosis therapeutic". Nature Communications. 6: 6532. Bibcode:2015NatCo...6.6532W. doi:10.1038/ncomms7532. PMC 4360920. PMID 25766071.
- ^ Perego J, Mendes A, Bourbon C, Camosseto V, Combes A, Liu H, et al. (January 2018). "Guanabenz inhibits TLR9 signaling through a pathway that is independent of eIF2α dephosphorylation by the GADD34/PP1c complex". Science Signaling. 11 (514) eaam8104. doi:10.1126/scisignal.aam8104. hdl:10773/27856. PMID 29363586. S2CID 13680678.
Sympatholytic (and closely related) antihypertensives (C02) |
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Sympatholytics (antagonize α-adrenergic vasoconstriction) | | Central | | α2-Adrenergic receptor agonists | |
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| Adrenergic release inhibitors | |
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| Imidazoline receptor agonists | |
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| Ganglion-blocking/nicotinic antagonists | |
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| Peripheral | | Indirect | | Monoamine oxidase inhibitors | |
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| VMAT inhibitors | |
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| Tyrosine hydroxylase inhibitors | |
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| Direct | | α1-Adrenergic receptor blockers | |
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| Non-selective α-adrenergic receptor blockers | |
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| Other antagonists | | Serotonin receptor antagonists | |
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| Endothelin receptor antagonists (for PHTooltip Pulmonary hypertension) |
- dual (Aprocitentan, Bosentan, Macitentan (+tadalafil), Riociguat)
- selective (Ambrisentan (+tadalafil), Sitaxentan, Sotatercept)
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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Adrenergic receptor modulators |
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| α1 | | Agonists | |
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| Antagonists |
- Abanoquil
- ADRIANA
- Ajmalicine
- Alfuzosin
- Anisodamine
- Anisodine
- Atiprosin
- Atypical antipsychotics (e.g., brexpiprazole, clozapine, olanzapine, quetiapine, risperidone)
- Benoxathian
- Beta blockers (e.g., adimolol, amosulalol, arotinolol, carvedilol, eugenodilol, labetalol)
- Buflomedil
- Bunazosin
- Butanserin
- Corynanthine
- Dapiprazole
- Domesticine
- Doxazosin
- Ergolines (e.g., acetergamine, ergotamine, dihydroergotamine, lisuride, nicergoline, terguride)
- Etoperidone
- Fenspiride
- Hydroxyzine
- Indoramin
- Ketanserin
- L-765,314
- mCPP
- Mepiprazole
- Metazosin
- Monatepil
- Moxisylyte
- MT-1207
- Naftopidil
- Nantenine
- Neldazosin
- Niaprazine
- Niguldipine
- Pardoprunox
- Pelanserin
- Perlapine
- Phendioxan
- Phenoxybenzamine
- Phentolamine
- Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione)
- Piperoxan
- Prazosin
- Quinazosin
- Quinidine
- Silodosin
- Spegatrine
- Spiperone
- Talipexole
- Tamsulosin
- Terazosin
- Tiodazosin
- Tolazoline
- Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin)
- Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, imipramine, trimipramine)
- Trimazosin
- Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine)
- Urapidil
- WB-4101
- Zolertine
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| α2 | | Agonists | |
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| Antagonists |
- 1-PP
- Adimolol
- Amesergide
- Aptazapine
- Atipamezole
- Atypical antipsychotics (e.g., asenapine, brexpiprazole, clozapine, lurasidone, olanzapine, paliperidone, quetiapine, risperidone, zotepine)
- Azapirones (e.g., buspirone, gepirone, ipsapirone, tandospirone)
- BRL-44408
- Buflomedil
- Cirazoline
- Efaroxan
- Esmirtazapine
- Fenmetozole
- Fipamezole
- Fluparoxan
- Idazoxan
- Ketanserin
- Lisuride
- mCPP
- Mianserin
- Mirtazapine
- NAN-190
- Pardoprunox
- Phentolamine
- Phenoxybenzamine
- Piperoxan
- Piribedil
- Rauwolscine
- Rotigotine
- Setiptiline
- Spegatrine
- Spiroxatrine
- Sunepitron
- Terguride
- Tolazoline
- Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine)
- Yohimbine
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| β | |
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- See also: Receptor/signaling modulators
- Dopaminergics
- Serotonergics
- Monoamine reuptake inhibitors
- Monoamine releasing agents
- Monoamine metabolism modulators
- Monoamine neurotoxins
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