A histamine agonist is a drug which causes increased activity at one or more of the four histamine receptor subtypes.
H1 agonists promote wakefulness.[1]
H2: Betazole and Impromidine are examples of agonists used in diagnostics to increase histamine.
H3: Betahistine is a weak Histamine1 agonist and a very strong antagonist of the Histamine3 autoreceptor. Antagonizing H3 increases histaminergic tone.
See also
References
- ^ Sakai, N.; Nishino, S. (2013). "Wake-Promoting Medications". Encyclopedia of Sleep. Elsevier. pp. 627–633. doi:10.1016/b978-0-12-378610-4.00126-1. ISBN 978-0-12-378611-1.
Although centrally injected histamine or histaminergic H1 agonists promote wakefulness, the systemic administration of these compounds induces various unacceptable side effects via peripheral H1 receptor stimulation.
External links
|
|---|
| H1 | | Agonists | |
|---|
| Antagonists |
- Others: Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, brilaroxazine, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, ziprasidone, zotepine)
- Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione)
- Tetracyclic antidepressants (e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline)
- Tricyclic antidepressants (e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin (dothiepin), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine)
- Typical antipsychotics (e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene)
- Unknown/unsorted: Azanator
- Belarizine
- Elbanizine
- Flotrenizine
- GSK1004723
- Napactadine
- Tagorizine
- Trelnarizine
- Trenizine
|
|---|
|
|---|
| H2 | |
|---|
| H3 | |
|---|
| H4 | | Agonists |
- 4-Methylhistamine
- α-Methylhistamine
- Histamine
- L-Histidine
- OUP-16
- VUF-8430
|
|---|
| Antagonists | |
|---|
|
|---|
- See also
- Receptor/signaling modulators
- Monoamine metabolism modulators
- Monoamine reuptake inhibitors
|
|
|---|
| Types |
- ♦ Miscellaneous: Precursor
- Cofactor
|
|---|
| Classes | | Enzyme | see Enzyme inhibition |
|---|
| Ion channel | See Ion channel modulators |
|---|
Receptor & transporter | |
|---|
| Miscellaneous |
- Cofactor (see Enzyme cofactors)
- Precursor (see Amino acids)
|
|---|
|
|---|