The United States of America As Represented by the Department of Health

Ralph A Lessor

Kenner C Rice

Michael Francis Rafferty

Arthur E Jacobson

Patricia C Contreras

Mariena V Mattson

Thomas L O'Donohue

A derivative of phencyclidine (1) bearing an isothiocyanate moiety on the meta position of the aromatic ring (3; Metaphit as methanesulfonate and HCl salt) has been synthesized and identified as a rapid and specific site-directed acylating agent of the [.sup.3 H]-phencyclidine binding site in rat brain homogenates. Additional related compounds to Metaphit are Thiophit (oxalate salt), Ethylphit (HCl salt), and Isopropylphit (HCl salt).

Metaphit and related compounds as acylating agents for the

A derivative of phencyclidine (1) bearing an isothiocyanate moiety of the meta position of the aromatic ring (2; Metaphit) has been synthesized and identified as a rapid and specific site-directed acylating agent of the [.sup.3 H]-phencyclidine binding site in rat brain homogenates.

Metaphit, a specific acylating agent for the [.sup.3 H] phencyclidine

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Ralph A Lessor