Method of inducing a histamine agonist action on H.sub.2 receptors

Information

  • Patent Grant
  • 5321039
  • Patent Number
    5,321,039
  • Date Filed
    Friday, September 6, 1991
    32 years ago
  • Date Issued
    Tuesday, June 14, 1994
    29 years ago
Abstract
The invention claims as drugs which are active as agonists of the histamine H.sub.3 receptor, the O-[2-(4(5-imidazolyl)-ethyl] isothiourea, 4-(4(5)-imidazolyl) butyramidine and S-[2-(4(5)-imidazolyl)-ethyl] isourea as well as their N-methyl derivatives, these compounds being useful for the preparation of drugs to be used as hypnotic, sleep-inducer, tranquillizer, sedative, anxiolytic, anti-asthmatic and anti-inflammatory agents, notably for the bronchi, the skin or the eyes, or as anti-gastric ulcer agents.
Description
Claims
  • 1. A method of inducing a histamine agonist action on H.sub.3 receptors of a subject, comprising the step of administering to said subject S-[2-(4(5)-imidazolyl)-ethyl] isothiourea in an amount sufficient to induce said action.
  • 2. The method according to claim 1, wherein the compound S-[2-(4(5)-imidazolyl)-ethyl] isothiourea is administered to said subject at a dosage of between 0.1 and 10 mg/kg.
  • 3. A method of inducing a hypnotic, sleep-inducing, tranquilizing, sedative or anxiolytic action in a subject, comprising the step of administering to said subject S-[2-(4(5)-imidazolyl)-ethyl] isothiourea in an amount sufficient to induce said action.
  • 4. The method according to claim 3, wherein the compound S-[2-(4(5)-imidazolyl)-ethyl] isothiourea is administered to said subject at a unit dosage of 5 to 60 mg.
  • 5. A method of inducing a histamine agonist action on H.sub.3 receptors of a subject, comprising the step of administering to said subject the N-methyl derivative of S-[2-(4(5)-imidazolyl)-ethyl] isothiourea in an amount sufficient to induce said action.
  • 6. The method according to claim 5, wherein the N-methyl derivative of S-[2-(4(5)-imidazolyl)-ethyl] isothiourea is administered to said subject at a dosage between 1 and 50 mg/kg.
  • 7. A method of inducing a hypnotic, sleep-inducing, tranquilizing, sedative or anxiolytic action in a subject, comprising the step of administering to said subject the N-methyl derivative of S-[2-(4(5)-imidazolyl)-ethyl] isothiourea.
  • 8. The method according to claim 7, wherein the N-methyl derivative of S-[2-(4(5)-imidazolyl)-ethyl] isothiourea is administered to said subject at a unit dose of 50 to 600 mg.
  • 9. A pharmaceutical composition having a hypnotic, sleep-inducing, tranquilizing, sedative, anxiolytic, anti-inflammatory or anti-gastric ulcer activity, comprising as active principle 0-[2-(4(5)-imidazolyl)-ethyl] isourea or its N-methyl derivative in an amount sufficient to induce said activity in a subject, and a pharmaceutically acceptable excipient or vehicle.
Priority Claims (1)
Number Date Country Kind
90 04861 Apr 1990 FRX
Parent Case Info

This application is a continuation-in-part of copending application Ser. No. 07/684,792, now abandoned, filed Apr. 15, 1991.

US Referenced Citations (5)
Number Name Date Kind
3759944 Black et al. Sep 1973
3818097 Black et al. Jun 1974
3891764 Black et al. Jun 1975
3954982 Black et al. May 1976
5047418 Howson Sep 1991
Foreign Referenced Citations (3)
Number Date Country
0420396 Apr 1991 EPX
2052692 May 1971 DEX
1296544 Nov 1972 GBX
Non-Patent Literature Citations (5)
Entry
Agents and Actions, vol. 18, 1/2 (1986), pp. 137-140.
Arch. Pharm., 319 Band, Dec. (1986) Heft 12, pp. 1057-1064.
Medicinal Chemistry, Chap. 6, (1985) pp. 93-118.
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Van der Werf, et al., Trends in Pharmacological Sciences, vol. 10, No. 4, . 159-182, Apr. 1989.
Continuation in Parts (1)
Number Date Country
Parent 684792 Apr 1991